2,4‐ and 2,5‐Disubstituted Arylthiazoles: Rapid Synthesis by C–H Coupling and Biological Evaluation

Abstract

Abstract Life‐threatening infections caused by bacteria that have developed resistance to common antibiotics, such as methicillin‐resistant Staphylococcus aureus (MRSA), have become a serious problem in hospitals and other areas all over the world. Thus, the development of an effective class of antibiotics against these bacteria is an urgent subject. Herein, we report a step‐economical and diversity‐oriented synthesis of a series of 2‐arylidenehydrazinyl‐4‐arylthiazole and 2‐arylidenehydrazinyl‐5‐arylthiazole analogues that utilizes C–H coupling methodologies. A library of 54 new congeners were synthesized and tested for their biological potential. Moreover, new knowledge regarding the structure–activity relationships (SARs) of these heterobiaryl compounds was collected.