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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. 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 field of medicinal chemistry of anti-infective agents, focusing on novel drug structural classes, therapeutic approaches, biological targets, and resistance mechanisms, which could pave the way for the development of optimized therapies against bacterial, protozoan, viral, and fungal infections.

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Introduction to the 1st Molecules Medicinal Chemistry Symposium (MMCS), Barcelona, 8 September 2017

by

Diego Muñoz-Torrero

and

Proceedings 2017, 1(6), 1098; https://doi.org/10.3390/proceedings1061098 - 04 Dec 2017

Viewed by 863

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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Open AccessAbstract

Preparation of Antimicrobial Nitrogen Heterocycles Using Sustainable Processes

by

Concepción C. González

,

Jorge Juan Cabrera Trujillo

,

Emy André-Joyaux

,

Antonio J. Herrera

and

Proceedings 2017, 1(6), 201; https://doi.org/10.3390/proceedings1060201 - 06 Dec 2017

Viewed by 1279

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)

Open AccessAbstract

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

,

and

Alessandro De Logu

Proceedings 2017, 1(6), 209; https://doi.org/10.3390/proceedings1060209 - 18 Oct 2017

Viewed by 878

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)

Open AccessAbstract

Discovery of Biphenyl-Substituted Diarylpyrimidines as New Non-Nucleoside HIV-1 Reverse Transcripttase Inhibitors

by

,

,

,

and

Christophe Pannecouque

Proceedings 2017, 1(6), 220; https://doi.org/10.3390/proceedings1060220 - 19 Oct 2017

Viewed by 824

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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Open AccessAbstract

Computational Approach to Structural and Conformational Characterization of Viral Surface Glycoproteins of HIV-2

by

Patrícia Serra

,

Andreia Martins

,

and

Proceedings 2017, 1(6), 228; https://doi.org/10.3390/proceedings1060228 - 19 Oct 2017

Viewed by 1048

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)

Open AccessAbstract

Synthesis and Anticandidal Activity of New Imidazole Derivatives

by

,

Betül Kaya Çavuşoğlu

,

Begüm Nurpelin Sağlık

,

and

Zafer Asım Kaplancıklı

Proceedings 2017, 1(6), 230; https://doi.org/10.3390/proceedings1060230 - 19 Oct 2017

Viewed by 833

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)

Open AccessAbstract

Designing Novel Hydrazinecarbothioamides as Potential HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors

by

,

,

,

,

and

And Christophe Pannecouque

Proceedings 2017, 1(6), 274; https://doi.org/10.3390/proceedings1060274 - 18 Oct 2017

Cited by 1 | Viewed by 874

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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Open AccessAbstract

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 964

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)

Open AccessAbstract

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

,

Betül Kaya Çavuşoğlu

,

and

Zafer Asım Kaplancıklı

Proceedings 2017, 1(6), 637; https://doi.org/10.3390/proceedings1060637 - 19 Oct 2017

Viewed by 817

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)

Open AccessAbstract

Antimicrobial Peptides Derived from the Genome Mining of Animals Living in Pathogenic Environments

by

José Manuel Pérez de la Lastra

,

C. Garrido-Orduña

,

,

and

Proceedings 2017, 1(6), 638; https://doi.org/10.3390/proceedings1060638 - 18 Oct 2017

Cited by 1 | Viewed by 849

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)

Open AccessAbstract

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

,

,

and

Proceedings 2017, 1(6), 639; https://doi.org/10.3390/proceedings1060639 - 18 Oct 2017

Viewed by 846

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)

Open AccessAbstract

Identification of a Novel Anti-Mycobacterial Series

by

and

Carlos Alemparte

Proceedings 2017, 1(6), 641; https://doi.org/10.3390/proceedings1060641 - 20 Oct 2017

Viewed by 832

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)

Open AccessAbstract

Antimicrobial: Arginine and Lysine Conjugated Rhamnolipids

by

,

,

Ana M. Marqués

,

Angeles Manresa

and

Proceedings 2017, 1(6), 642; https://doi.org/10.3390/proceedings1060642 - 07 Nov 2017

Viewed by 1084

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)

Open AccessAbstract

QSAR Analysis of Antibacterial and Antifungal Activity of Novel 2-Morpholinoquinoline Analogs

by

Strahinja Kovačević

,

Milica Karadžić

,

and

Sanja Podunavac-Kuzmanović

Proceedings 2017, 1(6), 643; https://doi.org/10.3390/proceedings1060643 - 18 Oct 2017

Viewed by 839

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)

Open AccessAbstract

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 930

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)

Open AccessAbstract

Design, Synthesis Molecular Docking Study and Antifungal Activity Evaluation of New Benzimidazole-Triazole Derivatives

by

,

Ulviye Acar Çevik

,

and

Proceedings 2017, 1(6), 647; https://doi.org/10.3390/proceedings1060647 - 19 Oct 2017

Cited by 2 | Viewed by 789

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)

Open AccessAbstract

Design, Synthesis and Structure—Activity Relationships of a Phenotypic Small Library against Protozoan Infections

by

,

,

Federica Belluti

,

,

,

,

Bernhard Ellinger

,

Carolina B. Moraes

,

Lucio H. Freitas-Junior

,

,

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 1237

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)

Open AccessAbstract

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 1000

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)

Open AccessAbstract

In Vitro Primary Screening of a Synthetic Series of Chromenoazoldiones against Trypanosoma cruzi

by

Cristina Fonseca-Berzal

,

,

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 991

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)

Open AccessAbstract

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

,

,

and

Silvia Pérez-Silanes

Proceedings 2017, 1(6), 651; https://doi.org/10.3390/proceedings1060651 - 18 Oct 2017

Viewed by 822

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)

Open AccessAbstract

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

,

,

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 1148

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)

Open AccessAbstract

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 908

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)

Open AccessAbstract

Lipopeptide Antibiotics Derived from Polymyxin B with a Broad Spectrum of Activity: Membrane Interaction

by

,

,

Angeles Manresa

,

Ariadna Grau-Campistany

and

Francesc Rabanal

Proceedings 2017, 1(6), 654; https://doi.org/10.3390/proceedings1060654 - 17 Oct 2017

Viewed by 1293

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)

Open AccessAbstract

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 914

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)

Open AccessAbstract

Synthesis, Anticandidal Activity and Molecular Docking Study of Some New Imidazole Derivatives

by

Begüm Nurpelin Sağlık

,

,

Ulviye Acar Çevik

,

and

Proceedings 2017, 1(6), 656; https://doi.org/10.3390/proceedings1060656 - 19 Oct 2017

Viewed by 779

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)

Open AccessAbstract

Antimicrobial Activity of Amino Acid Analogues and Their Derivatives

by

Dácil Hernández

,

Carlos Saavedra

,

,

and

José M. Pérez de Lastra

Proceedings 2017, 1(6), 657; https://doi.org/10.3390/proceedings1060657 - 19 Oct 2017

Viewed by 817

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)

Open AccessAbstract

Synthesis and Antimicrobial Activity Evaluation of New Benzimidazole—Thiazole Derivatives

by

Zafer Asim Kaplancikli

,

,

and

Proceedings 2017, 1(6), 658; https://doi.org/10.3390/proceedings1060658 - 19 Oct 2017

Viewed by 798

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)

Open AccessAbstract

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

,

,

,

Manuel Sánchez-Moreno

and

Silvia Pérez-Silanes

Proceedings 2017, 1(6), 659; https://doi.org/10.3390/proceedings1060659 - 18 Oct 2017

Viewed by 1018

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)

Open AccessAbstract

Design, Synthesis and Activity of New Polymyxins

by

Francesc Rabanal

,

,

,

,

Maria Garcia-Subirats

,

Angeles Manresa

and

Proceedings 2017, 1(6), 662; https://doi.org/10.3390/proceedings1060662 - 20 Oct 2017

Viewed by 1238

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)

Open AccessAbstract

Novel Imidazole Derivatives as Antifungal Agents: Synthesis, Biological Evaluation, ADME Prediction and Molecular Docking Studies

by

,

,

and

Begüm Nurpelin Sağlık

Proceedings 2017, 1(6), 663; https://doi.org/10.3390/proceedings1060663 - 19 Oct 2017

Cited by 1 | Viewed by 879

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)

Open AccessAbstract

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 916

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)

Open AccessAbstract

Design of Potential Antimalarial Agents Based on a Homology Model of Plasmodium falciparum Glucose-6-Phosphate Dehydrogenase

by

,

,

,

,

,

Carla Barbaraci

,

Cristina Sampedro

,

Jordi Juárez-Jiménez

,

,

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 1221

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)

Open AccessAbstract

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 974

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)

Open AccessAbstract

Cell-Based Medicinal Chemistry Optimization of High Throughput Screening Hits towards Orally Active Antimalarial and Antituberculosis Agents

by

Proceedings 2017, 1(6), 667; https://doi.org/10.3390/proceedings1060667 - 04 Dec 2017

Viewed by 820

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)

Open AccessAbstract

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 1049

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)

Open AccessAbstract

Current Pipeline of Antimalarial Therapies

by

Proceedings 2017, 1(6), 669; https://doi.org/10.3390/proceedings1060669 - 18 Oct 2017

Viewed by 796

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)

Supplementary material:
Supplementary File 1 (PDF, 492 KiB)

Open AccessAbstract

Lipid-Oligonucleotide Conjugates Forming G-Quadruplexes (Lipoquads) as Potent Inhibitors of HIV Entry

by

Sébastien Lyonnais

,

Santiago Grijalvo

,

Carmen Alvarez-Fernández

,

,

Javier Martínez

,

Andreas Meyerhans

,

Sonsoles Sánchez-Palomino

,

Gilles Mirambeau

and

Proceedings 2017, 1(6), 670; https://doi.org/10.3390/proceedings1060670 - 19 Oct 2017

Cited by 1 | Viewed by 964

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)

Open AccessAbstract

Structure-Activity Relationship of Arg₁₀-Teixobactin: A Recently Discovered Antimicrobial Peptide

by

Fernando Albericio

,

Shimaa A. H. Abdel Monaim

,

,

Gerardo A. H. Acosta

,

Estelle J. Ramchuran

,

,

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 1193

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)

Open AccessAbstract

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 1011

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)

Open AccessAbstract

The Search for New Antimicrobial Agents, by Site-Selective Peptide Modification

by

,

,

,

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 1041

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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Open AccessAbstract

Nitrosyl [2Fe-2S] Ferredoxin Mimetics as New Nitric Oxide Donating Antibacterial Agents

by

Nataliya Sanina

,

,

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 835

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)

Open AccessAbstract

Highly Sensitive Bioluminescence Imaging Models for Chagas Disease Drug Discovery

by

,

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 979

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)

Open AccessAbstract

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 914

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)

Open AccessAbstract

Diversity-Oriented Synthesis and Chemical Genetics of Peptidomimetics to Address Lead Discovery of Anti-Infective Agents

by

,

Irene Stefanini

,

,

,

Duccio Cavalieri

and

Andrea Trabocchi

Proceedings 2017, 1(6), 678; https://doi.org/10.3390/proceedings1060678 - 18 Oct 2017

Cited by 1 | Viewed by 896

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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