Design, Synthesis, and Evaluation of Novel 3-, 4-substituted, and 3,4-di Substituted Quinazoline Derivatives as Antimicrobial Agents

Farag A El-Essawy,Nader M Boshta,Abdulrahman I Alharthi,Nancy E Wahba,Mshari A Alotaibi

doi:10.37358/rc.20.2.7951

Abstract

A novel series of 3-, 4-substituted, and 3,4-di substituted quinazoline derivatives were prepared via various cyclized regents and most of the newly prepared compounds evaluated for their antimicrobial activities in vitro against Gram-positive, Gram-negative bacterial strains and fungi strains. The structures of the quinazoline derivatives have been confirmed using spectroscopic analyses (IR, NMR, and EI-MS). Some of the synthesized derivatives displayed a moderate antimicrobial activity in comparison with reference drugs, for example compounds 13d, 15a, 17b, 18b, 18d, 25, and 29a-c. Among the synthesized compounds, the pyrimidoqunazoline derivative 6c elicited the highest activity.

Highlights

A novel series of 3, 4-substituted, and 3,4-di substituted quinazoline derivatives were prepared via various cyclized regents and most of the newly prepared compounds evaluated for their antimicrobial activities in vitro against Gram-positive, Gram-negative bacterial strains and fungi strains
Pyrimidine, Triazole and pyrazole scaffolds attracted medicinal chemistry very much due to their biological and chemotherapeutic importance [14-23]. On this context and our research interest in the area of drug discovery as well as the synthesis of novel heterocyclic systems, [24-27] we became interested in the design and synthesis a series of novel quinazoline derivatives
Since many analogues of this ring system showed marked biological activity [30], we have investigated the synthesis of this scaffold, and we present our results