Synthesis and Evaluation of Novel 4‐Substituted Styryl Quinazolines as Potential Antimicrobial Agents

Abstract

In an attempt to afford possible antibacterial and anti-human immunodeficiency virus (HIV) agents, a series of 22 novel styryl quinazoline-based heterocyclic entities were designed and synthesized. Various substituted aryl urea and thiourea cores were incorporated at position 4 of quinazoline, followed by styrylation of position 2, aiming at an augmented biological potential. The synthesized compounds were well characterized through IR, (1) H NMR, (13) C NMR and elemental analyses. All compounds were screened for their in vitro anti-HIV activity against the HIV-1 (IIIB) and HIV-2 (ROD) strains. The antibacterial activity was also evaluated against various pathogenic Gram-positive and Gram-negative bacterial strains.

Selectivity Studies Towards the Synthesis of Novel Biaryl Ureas by (Hetero)Nanocatalysis: Size Control and Support Effects

“…[1] For instance, the urea-type backbone is related to HIV-1 protease inhibition, [2] antitumor, [3] antitrypanossomal, [4] anda ntituberculosis activities. [1] For instance, the urea-type backbone is related to HIV-1 protease inhibition, [2] antitumor, [3] antitrypanossomal, [4] anda ntituberculosis activities.…”

“…The ureido scaffold has au biquitous presenceins everalfundamental biological processes. [1] For instance, the urea-type backbone is related to HIV-1 protease inhibition, [2] antitumor, [3] antitrypanossomal, [4] anda ntituberculosis activities. [5] This structural unit and some relateds ystems( e.g.,t hioureas,g lycolurilbased ones)f eatured ifferent properties,s uch as polarity, rigidity,a nd hydrogen-bonding capacity,w hich play ac entral role in molecular recognition, making these systems well suited to folding and self-assembly.…”

Design, synthesis, antimicrobial activity and anti-HIV activity evaluation of novel hybrid quinazoline–triazine derivatives

“…The development of hybrid molecules through the arrangement of dissimilar pharmacophores may provide compounds with attractive biological profiles 6 . Several observations indicate that s-triazine analogues are the widely studied heterocyclic compounds owing to their broad spectrum of biological activity, including antimicrobial [7][8][9][10] , antimycobacterial 11 , anticancer 12,13 , antimalarial 14 and anti-HIV (NNRTIs) properties 15 . The biological importance of quinazoline had already stimulated the medicinal chemists to consider it as a building block due to its broad range of pharmacological properties, such as antimicrobial [16][17][18] , anti-HIV and anti-TMV (Tobacco Mosaic Virus) 19,20 , antitubercular 21 , anticancer 22 , anti-inflammatory 23 , anticonvulsant 24 , antidepressant 25 , hypolipidemic 26 , antiulcer 27 , analgesic 28 and immunotropic activities 29 .…”

Design, Synthesis, Biological Evaluation, and Molecular Modeling of Coumarin–Piperazine Derivatives as Acetylcholinesterase Inhibitors

“…As part of our continuing pursuit focused to design new leads with potent biological activities and the therapeutic importance of coumarin and piperazine chemical groups/moieties, a series of coumarin–piperazine analogs were designed based on the structural features of ensaculin. The designed molecules were then synthesized and evaluated for their potency to inhibit h AChE enzyme.…”