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Proceedings, 2017, MMCS 2017

The 1st Molecules Medicinal Chemistry Symposium

Barcelona, Spain | 8 September 2017

Issue Editor: Diego Muñoz-Torrero, University of Barcelona, Spain

Number of Papers: 44
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Cover Story (view full-size image): This issue of Proceedings gathers papers presented at the 1st Molecules Medicinal Chemistry Symposium (MMCS), which was held in Barcelona, Spain, on 8 September 2017. It collects contributions in the [...] Read more.
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2 pages, 163 KiB  
Editorial
Introduction to the 1st Molecules Medicinal Chemistry Symposium (MMCS), Barcelona, 8 September 2017
by Diego Muñoz-Torrero and Kelly Chibale
Proceedings 2017, 1(6), 1098; https://doi.org/10.3390/proceedings1061098 - 4 Dec 2017
Viewed by 1388
Abstract
The Medicinal Chemistry section of the MDPI journal Molecules organized, for the first time, the [...]
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(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)

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1 pages, 133 KiB  
Abstract
Preparation of Antimicrobial Nitrogen Heterocycles Using Sustainable Processes
by Concepción C. González, Jorge Juan Cabrera Trujillo, Emy André-Joyaux, Antonio J. Herrera and Nieves R. Paz
Proceedings 2017, 1(6), 201; https://doi.org/10.3390/proceedings1060201 - 6 Dec 2017
Viewed by 1732
Abstract
Libraries of compounds containing heteroaromatic rings and other nitrogen heterocycles were [...]
Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 149 KiB  
Abstract
Antimycobacterial Activity of New 1,4-Benzoxazine-2-One Derivatives and Its 2-(Arylamino)-4-Oxobut-2-Enoate, Ring-Open Analogues
by Daniele Zampieri, Marco Bernecich, Maria Grazia Mamolo, Adriana Sanna and Alessandro De Logu
Proceedings 2017, 1(6), 209; https://doi.org/10.3390/proceedings1060209 - 18 Oct 2017
Viewed by 1463
Abstract
Menaquinone is one of the essential components of the electron transport chain in many pathogens and consequently enzymes in its biosynthesis pathway are potential drug targets for the development of novel antibacterial agents. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 239 KiB  
Abstract
Discovery of Biphenyl-Substituted Diarylpyrimidines as New Non-Nucleoside HIV-1 Reverse Transcripttase Inhibitors
by Kaijun Jin, Ge Meng, Fen-Er Chen, Erik De Clercq and Christophe Pannecouque
Proceedings 2017, 1(6), 220; https://doi.org/10.3390/proceedings1060220 - 19 Oct 2017
Viewed by 1392
Abstract
Reverse transcriptase (RT), the key enzyme in the HIV life cycle of HIV, is one of the main targets for the antiretroviral chemotherapy. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
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2 pages, 163 KiB  
Abstract
Computational Approach to Structural and Conformational Characterization of Viral Surface Glycoproteins of HIV-2
by Patrícia Serra, Andreia Martins, Nuno Taveira and Rita C. Guedes
Proceedings 2017, 1(6), 228; https://doi.org/10.3390/proceedings1060228 - 19 Oct 2017
Viewed by 1601
Abstract
The efficacy of some of the available antiretroviral drugs is very limited against HIV-2 and, most importantly, none of the current drugs effectively prevents entry into the cells. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 170 KiB  
Abstract
Synthesis and Anticandidal Activity of New Imidazole Derivatives
by Derya Osmaniye, Betül Kaya Çavuşoğlu, Begüm Nurpelin Sağlık, Yusuf Özkay and Zafer Asım Kaplancıklı
Proceedings 2017, 1(6), 230; https://doi.org/10.3390/proceedings1060230 - 19 Oct 2017
Viewed by 1314
Abstract
During the last few years, there has been an increased awareness of morbidity and mortality related to invasive and systemic fungal disease because of resistant fungi and immunocompromised infections, for instance, AIDS. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 183 KiB  
Abstract
Designing Novel Hydrazinecarbothioamides as Potential HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors
by Hong Yin, Zhengyong Wan, Ge Meng, Fen-Er Chen, Erik De Clercq and And Christophe Pannecouque
Proceedings 2017, 1(6), 274; https://doi.org/10.3390/proceedings1060274 - 18 Oct 2017
Cited by 2 | Viewed by 1492
Abstract
Reverse transcriptase (RT), the key enzyme in the HIV life cycle of HIV, is one of the main targets for the antiretroviral chemotherapy. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
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2 pages, 168 KiB  
Abstract
Synthesis and In Vitro Antiparasitic Activity of Novel Arylamine Mannich Base-Type Derivatives against Trypanosoma cruzi and Leishmania spp.
by Rocio Paucar-Bernabé, Rubén Martín-Escolano, Elsa Moreno-Viguri, Manuel Sánchez-Moreno and Silvia Pérez-Silanes
Proceedings 2017, 1(6), 636; https://doi.org/10.3390/proceedings1060636 - 18 Oct 2017
Viewed by 1517
Abstract
Chagas disease and Leishmaniasis are trypanosomatid diseases considered as neglected tropical diseases by the WHO. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 200 KiB  
Abstract
Synthesis of 2-(5-(2-((5-(Cyclohexylamino)-1,3,4-Thiadiazol-2-yl)thio)ethyl)-1,3,4-Oxadiazol-2-yl) Derivatives and Their Antimicrobial Activity
by Serkan Levent, Betül Kaya Çavuşoğlu, Yusuf Özkay and Zafer Asım Kaplancıklı
Proceedings 2017, 1(6), 637; https://doi.org/10.3390/proceedings1060637 - 19 Oct 2017
Viewed by 1328
Abstract
The rate of invasive fungal infections has increased since the 1980s, particularly in the vast populace of immunocompromised patients as well as those hospitalized with serious underlying disease [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 135 KiB  
Abstract
Antimicrobial Peptides Derived from the Genome Mining of Animals Living in Pathogenic Environments
by José Manuel Pérez de la Lastra, C. Garrido-Orduña, C. L. Borges, A. A. Borges and A. Boto
Proceedings 2017, 1(6), 638; https://doi.org/10.3390/proceedings1060638 - 18 Oct 2017
Cited by 1 | Viewed by 1500
Abstract
Antimicrobial peptides (AMPs) have been used on animals for millions of years. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 197 KiB  
Abstract
Synthesis and Antimicrobial Activity of Newly Synthesized 2-((5-(4-(5(6)fluoro-1H-benzo[d]imidazol-2-yl)phenyl)-1,3,4-oxadiazol-2-yl)thio)-Derivatives
by Abdullah Burak Karaduman, Ulviye Acar Çevik, Derya Osmaniye, Yusuf Özkay and Sinem Ilgın
Proceedings 2017, 1(6), 639; https://doi.org/10.3390/proceedings1060639 - 18 Oct 2017
Viewed by 1329
Abstract
Benzimidazole derivatives have a great deal of interest in terms of antimicrobial therapy. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 137 KiB  
Abstract
Identification of a Novel Anti-Mycobacterial Series
by Esther Porras and Carlos Alemparte
Proceedings 2017, 1(6), 641; https://doi.org/10.3390/proceedings1060641 - 20 Oct 2017
Viewed by 1285
Abstract
Tuberculosis (TB) is the biggest global killer in history. One of the main objectives for fighting TB is to find a shorter treatment and also to target multidrug-resistant (MDR) and extensively drug-resistant XDR strains. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 131 KiB  
Abstract
Antimicrobial: Arginine and Lysine Conjugated Rhamnolipids
by Anderson Ramos, Aurora Pinazo, Ana M. Marqués, Angeles Manresa and Lourdes Pérez
Proceedings 2017, 1(6), 642; https://doi.org/10.3390/proceedings1060642 - 7 Nov 2017
Viewed by 1677
Abstract
The rapid increase of multiple drug resistant bacteria and fungi poses a serious threat to society. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 150 KiB  
Abstract
QSAR Analysis of Antibacterial and Antifungal Activity of Novel 2-Morpholinoquinoline Analogs
by Strahinja Kovačević, Milica Karadžić, Lidija Jevrić and Sanja Podunavac-Kuzmanović
Proceedings 2017, 1(6), 643; https://doi.org/10.3390/proceedings1060643 - 18 Oct 2017
Viewed by 1392
Abstract
The present study is focused on the chemometric QSAR analysis of antifungal and antibacterial activity of novel 2-morpholinoquinoline analogs and their molecular structure described by in silico molecular descriptors. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 139 KiB  
Abstract
Trichomonacidal Activity of 3,3′-Diindolylmethane (DIM) Is Additive to Metronidazole (MTZ) In Vitro, Supporting Future Oral/Topical Use
by Alexandra Ibáñez-Escribano, Leyre Pernaute Lau, Juan José Nogal-Ruiz, Alicia Gómez-Barrio, Jose Antonio Escario and Michael A. Zeligs
Proceedings 2017, 1(6), 645; https://doi.org/10.3390/proceedings1060645 - 19 Oct 2017
Viewed by 1609
Abstract
New, safe, well tolerated, and versatile anti-trichomonal agents for oral and topical use are needed to combat spreading resistance of Trichomonas vaginalis to metronidazole (MTZ). [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 168 KiB  
Abstract
Design, Synthesis Molecular Docking Study and Antifungal Activity Evaluation of New Benzimidazole-Triazole Derivatives
by Büşra Korkut, Ulviye Acar Çevik, Yusuf Özkay and Özlem Atlı
Proceedings 2017, 1(6), 647; https://doi.org/10.3390/proceedings1060647 - 19 Oct 2017
Cited by 2 | Viewed by 1383
Abstract
Lanosterol 14α-demethylase (CYP51) is an essential enzyme in the fungal life cycle and also an important target for antifungal drug development. Selective inhibition of the enzyme would cause depletion of ergosterol and accumulation of lanosterol and result in the growth inhibition of the [...] Read more.
Lanosterol 14α-demethylase (CYP51) is an essential enzyme in the fungal life cycle and also an important target for antifungal drug development. Selective inhibition of the enzyme would cause depletion of ergosterol and accumulation of lanosterol and result in the growth inhibition of the fungal cell [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 162 KiB  
Abstract
Design, Synthesis and Structure—Activity Relationships of a Phenotypic Small Library against Protozoan Infections
by Elisa Uliassi, Lorna Piazzi, Federica Belluti, Marcel Kaiser, Reto Brun, Sheraz Gul, Bernhard Ellinger, Carolina B. Moraes, Lucio H. Freitas-Junior, Chiara Borsari, Maria Paola Costi and Maria Laura Bolognesi
Proceedings 2017, 1(6), 648; https://doi.org/10.3390/proceedings1060648 - 19 Oct 2017
Cited by 2 | Viewed by 1802
Abstract
Protozoan infections (Plasmodium spp., Leishmania spp., and Trypanosoma spp.) remain one of the most pressing global health concerns, affecting billions of people and producing unsustainable economic burdens [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 121 KiB  
Abstract
Aryl Sulfonamides as a New Antitubercular Series: Discovery, Optimization and Target Identification
by Arancha Pérez García
Proceedings 2017, 1(6), 649; https://doi.org/10.3390/proceedings1060649 - 19 Oct 2017
Viewed by 1572
Abstract
Tuberculosis (TB) remains a major global health problem. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 198 KiB  
Abstract
In Vitro Primary Screening of a Synthetic Series of Chromenoazoldiones against Trypanosoma cruzi
by Cristina Fonseca-Berzal, Paula Morales, José A. Escario, Nadine Jagerovic and Alicia Gómez-Barrio
Proceedings 2017, 1(6), 650; https://doi.org/10.3390/proceedings1060650 - 17 Oct 2017
Viewed by 1508
Abstract
Similarities between parasites and cancer have prompted parasitologists to take advantage of several approaches enabled by cancer research to identify antiparasitic agents [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 168 KiB  
Abstract
Docking Study on T. cruzi Trypanothione Reductase and Iron-Superoxide Dismutase Isoforms of a Series of Imidazole-Based Derivatives as an Approach towards the Design of New Potential Inhibitors
by Iván Beltrán-Hortelano, María Font, Silvia Galiano and Silvia Pérez-Silanes
Proceedings 2017, 1(6), 651; https://doi.org/10.3390/proceedings1060651 - 18 Oct 2017
Viewed by 1371
Abstract
Chagas disease (CD) or American trypanosomiasis is a widespread parasitic disease throughout the world. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 123 KiB  
Abstract
Machine-Learning QSAR Model for Predicting Activity against Malaria Parasite’s Ion Pump PfATP4 and In Silico Binding Assay Validation
by Angela Lopez-Del Rio, Laura Llorach-Parés, Alexandre Perera-Lluna, Conxita Avila, Alfons Nonell-Canals and Melchor Sanchez-Martinez
Proceedings 2017, 1(6), 652; https://doi.org/10.3390/proceedings1060652 - 18 Oct 2017
Cited by 1 | Viewed by 1988
Abstract
Malaria is a mosquito-borne infectious disease caused by parasitic protozoans of the genus Plasmodium. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 139 KiB  
Abstract
Edelfosine (ET-18-OCH3) a Promising Alkylphospholipid against Resistant Trichomonas vaginalis
by Alexandra Ibáñez-Escribano, Jose Antonio Escario, Faustino Mollinedo and Alicia Gómez-Barrio
Proceedings 2017, 1(6), 653; https://doi.org/10.3390/proceedings1060653 - 19 Oct 2017
Viewed by 1438
Abstract
Edelfosine (ET-18-OCH3) is an alkylphospholipid with an analogous structure to miltefosine. Both molecules are active against kinetoplastids (Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei). [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 152 KiB  
Abstract
Lipopeptide Antibiotics Derived from Polymyxin B with a Broad Spectrum of Activity: Membrane Interaction
by Yolanda Cajal, Roser Segovia, Angeles Manresa, Ariadna Grau-Campistany and Francesc Rabanal
Proceedings 2017, 1(6), 654; https://doi.org/10.3390/proceedings1060654 - 17 Oct 2017
Viewed by 1857
Abstract
Antimicrobial peptides offer a new class of therapeutic agents to which bacteria may not be able to develop genetic resistance, since they act on the lipid component of the cell membranes [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 178 KiB  
Abstract
Activity of 2-benzyl-1-(2-hydroxyethyl)-5-nitroindazolin-3-one on Trypanosoma cruzi Bloodstream Trypomastigotes (Y strain): In Vitro and In Vivo Studies
by Cristina Fonseca-Berzal, Cristiane França da Silva, Marcos Meuser Batista, Francisca Hildemagna Guedes-da-Silva, Mariane Vasconcelos, Kelly C. Demarque, José A. Escario, Vicente J. Arán, Maria de Nazaré C. Soeiro and Alicia Gómez-Barrio
Proceedings 2017, 1(6), 655; https://doi.org/10.3390/proceedings1060655 - 17 Oct 2017
Cited by 1 | Viewed by 1489
Abstract
Benznidazole and nifurtimox, the currently available drugs for the specific treatment of Chagas disease, show limited effectiveness and high toxicity that prompt the identification of therapeutic alternatives. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 188 KiB  
Abstract
Synthesis, Anticandidal Activity and Molecular Docking Study of Some New Imidazole Derivatives
by Begüm Nurpelin Sağlık, Ayşen Işık, Ulviye Acar Çevik, Yusuf Özkay and Serkan Levent
Proceedings 2017, 1(6), 656; https://doi.org/10.3390/proceedings1060656 - 19 Oct 2017
Viewed by 1244
Abstract
The azole pharmacophore is still regarded as a viable lead structure for the synthesis of more effective antifungal agents [1–3]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 261 KiB  
Abstract
Antimicrobial Activity of Amino Acid Analogues and Their Derivatives
by Dácil Hernández, Carlos Saavedra, Carmen Carro, Alicia Boto and José M. Pérez de Lastra
Proceedings 2017, 1(6), 657; https://doi.org/10.3390/proceedings1060657 - 19 Oct 2017
Viewed by 1420
Abstract
Libraries of compounds containing unnatural amino acids or amino acid analogues were prepared from inexpensive substrates using sustainable processes [1–3]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 164 KiB  
Abstract
Synthesis and Antimicrobial Activity Evaluation of New Benzimidazole—Thiazole Derivatives
by Zafer Asim Kaplancikli, Serkan Levent, Derya Osmaniye and Yusuf Özkay
Proceedings 2017, 1(6), 658; https://doi.org/10.3390/proceedings1060658 - 19 Oct 2017
Viewed by 1372
Abstract
Antibiotic resistance which was expedited by the use of antimicrobial drugs has been a significant global challenge for public health [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 159 KiB  
Abstract
Biological Evaluation of Arylamine Mannich Base Derivatives with Potent In Vivo Activity as Potent Antichagasic Agents
by Rocio Paucar-Bernabé, Elsa Moreno-Viguri, Rubén Martín-Escolano, Mery Santivañez-Veliz, Amaya Azqueta, Nuria Cirauqui, Manuel Sánchez-Moreno and Silvia Pérez-Silanes
Proceedings 2017, 1(6), 659; https://doi.org/10.3390/proceedings1060659 - 18 Oct 2017
Viewed by 1581
Abstract
Chagas disease (CD) is a neglected tropical disease caused by the parasite Trypanosoma cruzi [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 153 KiB  
Abstract
Design, Synthesis and Activity of New Polymyxins
by Francesc Rabanal, Roser Segovia, Aina Coll, Judith Solé, Maria Garcia-Subirats, Angeles Manresa and Yolanda Cajal
Proceedings 2017, 1(6), 662; https://doi.org/10.3390/proceedings1060662 - 20 Oct 2017
Viewed by 1826
Abstract
Antibiotic resistance is a daunting challenge for public health systems worldwide. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 199 KiB  
Abstract
Novel Imidazole Derivatives as Antifungal Agents: Synthesis, Biological Evaluation, ADME Prediction and Molecular Docking Studies
by Yusuf Özkay, Derya Osmaniye, Serkan Levent and Begüm Nurpelin Sağlık
Proceedings 2017, 1(6), 663; https://doi.org/10.3390/proceedings1060663 - 19 Oct 2017
Cited by 2 | Viewed by 1490
Abstract
The incidence of infection from opportunistic and pathogenic fungi has continued to rise in recent years. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 151 KiB  
Abstract
Sustainable Multi-Target Drugs for Neglected Tropical Diseases Caused by Trypanosomatids: Dream or Reality?
by Maria Laura Bolognesi
Proceedings 2017, 1(6), 664; https://doi.org/10.3390/proceedings1060664 - 26 Oct 2017
Viewed by 1506
Abstract
The development of nifurtimox-eflornithine combination therapy (NECT) has been a major and emboldening advance towards more effective and simple medications in the field of neglected tropical diseases (NTD) caused by Trypanosomatids. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 154 KiB  
Abstract
Design of Potential Antimalarial Agents Based on a Homology Model of Plasmodium falciparum Glucose-6-Phosphate Dehydrogenase
by Caterina Pont, Nelson Alencar, Irene Sola, María Linares, Luca Di Palma, Carla Barbaraci, Cristina Sampedro, Jordi Juárez-Jiménez, Paloma Abad, Susana Pérez-Benavente, Jerónimo Lameira, José M. Bautista, F. Javier Luque and Diego Muñoz-Torrero
Proceedings 2017, 1(6), 665; https://doi.org/10.3390/proceedings1060665 - 18 Oct 2017
Viewed by 1798
Abstract
There currently exists a dire need for safe and inexpensive new antimalarial drugs, which are effective against multiple life cycle stages of Plasmodium falciparum, and act through mechanisms that differ from those of the available drugs to prevent drug resistance. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 115 KiB  
Abstract
Multicomponent Reactions with Heterocycles: A Source of Novel Scaffolds for Antiparasitic and Antiviral Agents
by Rodolfo Lavilla
Proceedings 2017, 1(6), 666; https://doi.org/10.3390/proceedings1060666 - 19 Oct 2017
Viewed by 1470
Abstract
We disclose a reaction discovery approach, based on novel multicomponent reactions (MCRs) upon heterocyclic substrates, especially azines, that yields a variety of scaffolds amenable to straightforward diversification. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 116 KiB  
Abstract
Cell-Based Medicinal Chemistry Optimization of High Throughput Screening Hits towards Orally Active Antimalarial and Antituberculosis Agents
by Kelly Chibale
Proceedings 2017, 1(6), 667; https://doi.org/10.3390/proceedings1060667 - 4 Dec 2017
Viewed by 1329
Abstract
It has recently been demonstrated, from a number of antimalarial and antituberculosis drug discovery programmes, that phenotypic whole cell screening can uncover cell permeable and active drug leads with potentially novel modes of action. In this regard, several series of antiplasmodial and antimycobacterial [...] Read more.
It has recently been demonstrated, from a number of antimalarial and antituberculosis drug discovery programmes, that phenotypic whole cell screening can uncover cell permeable and active drug leads with potentially novel modes of action. In this regard, several series of antiplasmodial and antimycobacterial actives were identified by phenotypic whole cell high-throughput screening of small molecule libraries. Following validation, hit molecules demonstrating good in vitro antiplasmodial and antimycobacterial activity against the respective causative agents, Plasmodium falciparum and Mycobacterium tuberculosis, with low cytotoxicity were prioritized for hit to lead and lead optimization medicinal chemistry progression. This talk will describe the drug discovery process that led to the identification of lead candidates with good oral in vivo pharmacokinetics. Target identification aspects will also be presented. Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 132 KiB  
Abstract
Structure Guided Design of Xanthomonas oryzae pv. oryzae Topoisomerase I Inhibitors
by Lakindu Samaranayake P. K. and Inoka C. Perera
Proceedings 2017, 1(6), 668; https://doi.org/10.3390/proceedings1060668 - 23 Oct 2017
Viewed by 1804
Abstract
Topoisomerase inhibitors initiate the cell killing process by either stabilizing or increasing the amount of the covalent complex formed between the enzyme and cleaved DNA. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 111 KiB  
Abstract
Current Pipeline of Antimalarial Therapies
by Benoît Laleu
Proceedings 2017, 1(6), 669; https://doi.org/10.3390/proceedings1060669 - 18 Oct 2017
Viewed by 1355
Abstract
Malaria is a devastating disease affecting millions of people each year yet, surprisingly, apart from the Artemisinin Combination Therapies (ACTs) there are relatively few effective treatments for Plasmodium falciparum and only one complete treatment for Plasmodium vivax. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 159 KiB  
Abstract
Lipid-Oligonucleotide Conjugates Forming G-Quadruplexes (Lipoquads) as Potent Inhibitors of HIV Entry
by Sébastien Lyonnais, Santiago Grijalvo, Carmen Alvarez-Fernández, Eric Fleta, Javier Martínez, Andreas Meyerhans, Sonsoles Sánchez-Palomino, Gilles Mirambeau and Ramon Eritja
Proceedings 2017, 1(6), 670; https://doi.org/10.3390/proceedings1060670 - 19 Oct 2017
Cited by 2 | Viewed by 1496
Abstract
Molecules that block virus entry by interfering with the actions of viral fusion proteins are of primary concern in the search for antiviral drugs. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 158 KiB  
Abstract
Structure-Activity Relationship of Arg10-Teixobactin: A Recently Discovered Antimicrobial Peptide
by Fernando Albericio, Shimaa A. H. Abdel Monaim, Yahya E. Jad, Gerardo A. H. Acosta, Estelle J. Ramchuran, Ayman El-Faham, Thavendran Govender, Hendrik G. Kruger and Beatriz G. de la Torre
Proceedings 2017, 1(6), 671; https://doi.org/10.3390/proceedings1060671 - 18 Oct 2017
Viewed by 1753
Abstract
The emergence of multidrug resistant bacteria has a direct impact on global public health due to the reduced potency of existing antibiotics against pathogens [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 138 KiB  
Abstract
Design and Synthesis of Cysteine Protease Inhibitors
by Florenci V. Gonzalez
Proceedings 2017, 1(6), 672; https://doi.org/10.3390/proceedings1060672 - 18 Oct 2017
Viewed by 1689
Abstract
We have been preparing new dipeptidyl inhibitors against parasitic cysteine proteases cruzain (related to Chagas disease) and rhodesain (related to Sleeping Sickness disease), and against human cathepsins. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 221 KiB  
Abstract
The Search for New Antimicrobial Agents, by Site-Selective Peptide Modification
by Alicia Boto, C. González, D. Hernández, I. Romero-Estudillo, N. Rodriguez-Paz and J. M. Pérez de la Lastra
Proceedings 2017, 1(6), 673; https://doi.org/10.3390/proceedings1060673 - 19 Oct 2017
Viewed by 1583
Abstract
Antimicrobial peptides (AMPs) have been used by animals and plants for millions of years for defence against pathogens, and present important advantages as potential drugs, such as a broad spectrum of activity, no induction of resistances, and synergic action with conventional antibiotics [1]. [...] Read more.
Antimicrobial peptides (AMPs) have been used by animals and plants for millions of years for defence against pathogens, and present important advantages as potential drugs, such as a broad spectrum of activity, no induction of resistances, and synergic action with conventional antibiotics [1]. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
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2 pages, 164 KiB  
Abstract
Nitrosyl [2Fe-2S] Ferredoxin Mimetics as New Nitric Oxide Donating Antibacterial Agents
by Nataliya Sanina, Galina Kozub, Tat’yana Kondrat’eva, Viktoriya Mumyatova and Alexei Terent’ev
Proceedings 2017, 1(6), 674; https://doi.org/10.3390/proceedings1060674 - 19 Oct 2017
Cited by 1 | Viewed by 1327
Abstract
Nitric oxide (NO) therapy is the newest approach to the treatment of socially important diseases all over the world. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 121 KiB  
Abstract
Highly Sensitive Bioluminescence Imaging Models for Chagas Disease Drug Discovery
by John M. Kelly, Amanda F. Francisco, Shiromani Jayawardhana, Martin C. Taylor and Michael D. Lewis
Proceedings 2017, 1(6), 676; https://doi.org/10.3390/proceedings1060676 - 17 Oct 2017
Viewed by 1470
Abstract
Chagas disease is caused by the insect-transmitted protozoan Trypanosoma cruzi, and is the most important parasitic infection in Latin America. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
2 pages, 165 KiB  
Abstract
Antibiotic Translocation and Membrane Barrier: New Insights to Combat Bacterial Resistance Jean-Marie Pagès UMR_MD1, TMCD2, Aix-Marseille Univ, IRBA, Marseille, France
by Jean-Marie Pagès
Proceedings 2017, 1(6), 677; https://doi.org/10.3390/proceedings1060677 - 16 Oct 2017
Viewed by 1419
Abstract
The increasing prevalence of antibacterial resistance is a worrying health concern. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
1 pages, 118 KiB  
Abstract
Diversity-Oriented Synthesis and Chemical Genetics of Peptidomimetics to Address Lead Discovery of Anti-Infective Agents
by Elena Lenci, Irene Stefanini, Antonio Guarna, Gloria Menchi, Duccio Cavalieri and Andrea Trabocchi
Proceedings 2017, 1(6), 678; https://doi.org/10.3390/proceedings1060678 - 18 Oct 2017
Cited by 1 | Viewed by 1383
Abstract
Modern advances in Chemical Biology include the improvement of screening methods, the introduction of bioinformatic methods to unravel biological pathways, and the generation of highquality chemical libraries. [...] Full article
(This article belongs to the Proceedings of Proceedings of the 1st Molecules Medicinal Chemistry Symposium, Barcelona, Spain)
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