Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis

Autor:	Rongfei Qin, Pengxu Wang, Bin Wang, Lei Fu, Sarah M. Batt, Gurdyal S. Besra, Chengwei Wu, Yanan Wang, Haihong Huang, Yu Lu, Gang Li
Rok vydání:	2021
Předmět:	Pharmacology Sulfonamides Organic Chemistry Antitubercular Agents General Medicine Microbial Sensitivity Tests Mycobacterium tuberculosis Thiophenes Molecular Docking Simulation Mice Structure-Activity Relationship Drug Discovery Tuberculosis Multidrug-Resistant Animals
Zdroj:	European journal of medicinal chemistry. 231
ISSN:	1768-3254
Popis:	A series of thiophene-benzenesulfonamide derivatives was designed and synthesized by exploring the structure-activity relationship of lead compounds 2,3-disubstituted thiophenes 25a and 297F as antituberculosis agents, which displayed potent antimycobacterial activity against drug-susceptible and clinically isolated drug-resistant tuberculosis. In particular, compound 17b, which had improved activity (minimum inhibitory concentration of 0.023 μg/mL) compared with the lead compounds, displayed good intracellular antimycobacterial activity in macrophages with a reduction of 1.29 log
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0b85873914ca4d495f9ce06dd1ac2311 https://pubmed.ncbi.nlm.nih.gov/35101648 Zobrazit plný text záznamu Full Text from ScienceDirect