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Drugs and Drug Candidates, Volume 4, Issue 3

2025 September - 16 articles

Cover Story: Building on our prior 1,3,5-tris-substituted benzene derivatives, we synthesized/tested simplified 1,3-bis[(4-(substituted-aminomethyl)phenyl)methyl]benzene and 1,3-bis[(4-(substituted-aminomethyl)phenoxy)methyl]benzene analogues against Plasmodium falciparum in vitro. The pharmacological results revealed significant antimalarial activity, with IC50 values in the submicromolar to micromolar range. Derivatives with notable G-quadruplex stabilization were not the most potent antimalarials. Moreover, these new compounds did not show promising stabilizing effects on the different G4 sequences. Therefore, no correlation arises between their antimalarial activity and the selectivity of their binding to G-quadruplexes. View this paper
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Articles (16)

  • Article
  • Open Access
2 Citations
2,374 Views
16 Pages

Design of a First-in-Class homoPROTAC to Induce ICP0 Degradation in Human Herpes Simplex Virus 1

  • Leyla Salimova,
  • Ali Sahin,
  • Ozge Ardicli,
  • Fatima Hacer Kurtoglu Babayev and ,
  • Zeynep Betul Sari,
  • Muhammed Emin Sari,
  • Muhammet Guzel Kurtoglu,
  • Sena Ardicli and
  • Huseyn Babayev
  • + 4 authors+ 0 author

Background/Objectives: Human Herpes Simplex Virus 1 (HSV-1) is a common pathogen that establishes lifelong latent infections. The emergence of drug resistance necessitates novel therapeutic strategies. This study introduces a novel antiviral approach...

(This article belongs to the Section In Silico Approaches in Drug Discovery)
  • Article
  • Open Access
2 Citations
1,503 Views
12 Pages

Background/Objectives: Malaria is a prominent vector-borne disease, with a high mortality rate, particularly in children under five years old. Despite the use of various insecticides for its control, the emergence of resistant mosquitoes poses a sign...

(This article belongs to the Section In Silico Approaches in Drug Discovery)
  • Review
  • Open Access
6,508 Views
24 Pages

Drugs, Mother, and Child—An Integrative Review of Substance-Related Obstetric Challenges and Long-Term Offspring Effects

  • Atziri Alejandra Jiménez-Fernández,
  • Joceline Alejandra Grajeda-Perez,
  • Sofía de la Paz García-Alcázar,
  • Mariana Gabriela Luis-Díaz and ,
  • Francisco Javier Granada-Chavez,
  • Emiliano Peña-Durán,
  • Jesus Jonathan García-Galindo and
  • Daniel Osmar Suárez-Rico
  • + 3 authors+ 0 author

Substance use during pregnancy is an increasingly important yet under-recognized threat to maternal and child health. This narrative review synthesizes the current evidence available on the epidemiology, pathophysiology, clinical management, and poli...

(This article belongs to the Section Clinical Research)
  • Article
  • Open Access
2,480 Views
32 Pages

Synthesis of New 1,3-bis[(4-(Substituted-Aminomethyl)Phenyl)methyl]benzene and 1,3-bis[(4-(Substituted-Aminomethyl)Phenoxy)methyl]benzene Derivatives, Designed as Novel Potential G-Quadruplex Antimalarial Ligands

  • Sandra Albenque-Rubio,
  • Jean Guillon,
  • Patrice Agnamey,
  • Céline Damiani and ,
  • Solène Savrimoutou,
  • Luisa Ronga,
  • Marie Hanot,
  • Tshering Zangmo,
  • Noël Pinaud and
  • Pascal Sonnet
  • + 12 authors+ 7 authors

Background: Based on our previously reported series of novel 1,3,5-tris[(4-(substituted-aminomethyl)phenyl)methyl]benzene and 1,3,5-tris[(4-(substituted-aminomethyl)phenoxy)methyl]benzene derivatives, we have now designed, synthesized, and tested a n...

(This article belongs to the Collection Anti-Parasite Drug Discovery)
  • Article
  • Open Access
1 Citations
2,064 Views
16 Pages

Background: Drug development for leishmaniases treatment follows a very selective process in order to propose drug candidates that possess all the qualities that meet the strict specifications of the pharmaceutical industry. Drug resistance is a limi...

(This article belongs to the Collection Anti-Parasite Drug Discovery)
  • Review
  • Open Access
1 Citations
5,020 Views
15 Pages

Bradykinin Receptors in Metabolic Disorders: A Comprehensive Review

  • Jéssica Branquinho,
  • Raquel Leão Neves,
  • Michael Bader and
  • João Bosco Pesquero

The kallikrein–kinin system and its B1 and B2 receptors are key regulators in metabolic disorders such as obesity, diabetes, and insulin resistance. Obesity, a chronic and multifactorial condition often associated with comorbidities like type 2...

(This article belongs to the Special Issue Drugs of the Kallikrein-Kinin System)
  • Review
  • Open Access
13 Citations
9,312 Views
31 Pages

Rheumatoid arthritis (RA) is a chronic systemic inflammatory disorder primarily targeting joints, leading to pain, swelling, and stiffness. RA results from the body’s own immune system attacking its own tissues. Currently, there are various tre...

(This article belongs to the Section Marketed Drugs)
  • Article
  • Open Access
1 Citations
2,191 Views
17 Pages

Background: Hypertension is a serious global health issue affecting over one billion adults and leading to severe complications if left unmanaged. Despite medical advancements, only a fraction of patients effectively have their hypertension under con...

(This article belongs to the Section In Silico Approaches in Drug Discovery)
  • Article
  • Open Access
1,428 Views
15 Pages

Background/Objective: Cerivastatin (Cer), a cholesterol-lowering statin, was withdrawn from the market due to fatal cases of rhabdomyolysis, particularly when co-administered with gemfibrozil (Gem), a strong CYP2C8 inhibitor. However, the pharmacokin...

(This article belongs to the Section Marketed Drugs)
  • Article
  • Open Access
2 Citations
2,904 Views
19 Pages

Identification of Pharmacophore Groups with Antimalarial Potential in Flavonoids by QSAR-Based Virtual Screening

  • Adriana de Oliveira Fernandes,
  • Valéria Vieira Moura Paixão,
  • Yria Jaine Andrade Santos,
  • Eduardo Borba Alves and ,
  • Ricardo Pereira Rodrigues,
  • Daniela Aparecida Chagas-Paula,
  • Aurélia Santos Faraoni,
  • Rosana Casoti,
  • Marcus Vinicius de Aragão Batista and
  • Tiago Branquinho Oliveira
  • + 7 authors+ 2 authors

Background/Objectives: Severe malaria, mainly caused by Plasmodium falciparum, remains a significant therapeutic challenge due to increasing drug resistance and adverse effects. Flavonoids, known for their wide range of bioactivities, offer a promisi...

(This article belongs to the Section In Silico Approaches in Drug Discovery)
  • Review
  • Open Access
34 Citations
16,036 Views
9 Pages

Suzetrigine represents a groundbreaking advancement in acute pain management as the first FDA-approved selective Nav1.8 inhibitor. This comprehensive review synthesizes data from clinical trials, pharmacological studies, and prescribing information t...

(This article belongs to the Section Marketed Drugs)
  • Article
  • Open Access
21 Citations
3,279 Views
27 Pages

A Multifaceted Exploration of Shirakiopsis indica (Willd) Fruit: Insights into the Neuropharmacological, Antipyretic, Thrombolytic, and Anthelmintic Attributes of a Mangrove Species

  • Mahathir Mohammad,
  • Md. Jahirul Islam Mamun,
  • Mst. Maya Khatun,
  • Md. Hossain Rasel and ,
  • M Abdullah Al Masum,
  • Khurshida Jahan Suma,
  • Mohammad Rashedul Haque,
  • Sayed Al Hossain Rabbi,
  • Md. Hemayet Hossain and
  • Safaet Alam
  • + 7 authors+ 2 authors

Background: Shirakiopsis indica (Willd.) (Family: Euphorbiaceae), a mangrove species found in the Asian region, is a popular folkloric plant. Locally, the plant is traditionally used to treat various types of ailments, especially for pain relief. The...

(This article belongs to the Section Drug Candidates from Natural Sources)
  • Article
  • Open Access
2 Citations
1,985 Views
10 Pages

Antimicrobial and Anti-Inflammatory Potentials of Silver Tungstate Nanoparticles, Cytotoxicity and Interference on the Activity of Antimicrobial Drugs

  • Washington de Souza Leal,
  • Juliane Zacour Marinho,
  • Isabela Penna Ceravolo,
  • Lucas Leão Nascimento and ,
  • Antonio Otávio de Toledo Patrocínio and
  • Marcus Vinícius Dias-Souza
  • + 1 author+ 0 author

Background: Bacterial resistance to antimicrobial drugs is a critical phenomenon that is hampering clinical treatments, raising the need for promising compounds that can be explored as pharmaceutical products. This study investigated the antimicrobia...

(This article belongs to the Section Medicinal Chemistry and Preliminary Screening)
  • Article
  • Open Access
2 Citations
1,767 Views
29 Pages

Ex Vivo Molecular Studies and In Silico Small Molecule Inhibition of Plasmodium falciparum Bromodomain Protein 1

  • David O. Oladejo,
  • Titilope M. Dokunmu,
  • Gbolahan O. Oduselu,
  • Daniel O. Oladejo and ,
  • Olubanke O. Ogunlana and
  • Emeka E. J. Iweala
  • + 1 author+ 0 author

Background: Malaria remains a significant global health burden, particularly in sub-Saharan Africa, accounting for high rates of illness and death. The growing resistance to frontline antimalarial therapies underscores the urgent need for novel drug...

(This article belongs to the Section In Silico Approaches in Drug Discovery)
  • Review
  • Open Access
2 Citations
4,081 Views
38 Pages

The methods utilized in the drug discovery pipeline routinely combine machine learning and deep learning algorithms to enhance the outputs. The generation of a drug target, through virtual screening and computational analysis of databases used for ta...

(This article belongs to the Section In Silico Approaches in Drug Discovery)
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Drugs Drug Candidates - ISSN 2813-2998