Synthesis and evaluation of novel 4-substituted styryl quinazolines as potential antimicrobial agents

Arch Pharm (Weinheim). 2012 Dec;345(12):964-72. doi: 10.1002/ardp.201200291. Epub 2012 Sep 27.

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.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Gram-Negative Bacteria / drug effects
  • Gram-Negative Bacteria / growth & development
  • Gram-Positive Bacteria / drug effects
  • Gram-Positive Bacteria / growth & development
  • HIV-1 / drug effects
  • HIV-1 / physiology
  • HIV-2 / drug effects
  • HIV-2 / physiology
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Quinazolines / chemical synthesis*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology
  • Virus Replication / drug effects

Substances

  • Anti-Bacterial Agents
  • Anti-HIV Agents
  • Quinazolines
  • styrylquinazoline