Synthesis, Biological Evaluation, and Molecular Modeling Studies of New 8-methyl-4-oxo-1,4-dihydroquinoline-3-carbohydrazides as Potential Anti-HIV Agents.

ABSTRACT:

Background

The development of a highly safe and potent scaffold is a significant challenge in anti-HIV drug discovery.

Objectives

This study aimed at developing a novel series of anti-HIV agents based on HIV integrase inhibitor pharmacophores.

Methods

A novel series of 8-methyl-4-oxo-1,4-dihydroquinoline-3-carbohydrazide derivatives featuring various substituted benzoyl and N-phenyl carboxamide and carbothioamide moieties were designed and synthesized.

Results

According to the biological evaluation, all the developed compounds were effective against HIV at concentrations lower than 150 µM, associated with no significant cytotoxicity (CC₅₀ > 500 µM).

Conclusions

Compound 8b, possessing a 4-fluorobenzoyl group, was the most potent compound, with

SUBMITTER: Alemi M 

PROVIDER: S-EPMC9420234 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature