使用Biotage Isolera快速纯化液相制备色谱为设计新的抗

Gyrase ATPase domain, the pharmaceutical underexploited segment of DNA gyrase, the sole Type II topoisomerase present in Mycobacterium tuberculosis represents an attractive target for anti-tubercular drug discovery. Here we report, the development of a novel series of MTB DNA gyraseB inhibitor identified through a medium throughput screening (MTS) of BITS in-house chemical library (3000 compounds). The MTS hit was further remodeled by chemical synthesis to identify the most potent analogue 27 exhibiting an in vitro gyrB inhibitory IC50 of 0.15 lM. The series also demonstrated well correlating gyrase super coi领 activity and in vitro anti-mycobacterial potency against MTB H37Rv strain. Furthermore the compounds displayed good safety profile in their subsequent cytotoxicity and hERG toxicity
evaluations, to be worked out from a pharmaceutical point of view as potential anti-tubercular agents. Biotage 快速纯化制备液相色谱 Flash Isolera one Biotage 快速纯化制备液相色谱 Flash Isolera Prime Biotage 快速纯化制备液相色谱 Flash Isolera LS