10252-82-1Relevant articles and documents
Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis
Batt, Sarah M.,Besra, Gurdyal S.,Fu, Lei,Huang, Haihong,Li, Gang,Lu, Yu,Qin, Rongfei,Wang, Bin,Wang, Pengxu,Wang, Yanan,Wu, Chengwei
, (2022/02/01)
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 log10 CFU. A druggability evaluation indicated that compound 17b had favorable hepatocyte stability, low cytotoxicity, and low hERG channel inhibition. Moreover, compound 17b exhibited modest in vivo efficacy in an acute mouse model of tuberculosis. In addition, the molecular docking study elucidated the binding mode of compound 17b in the active site of DprE1. Therefore, compound 17b may be a promising antituberculosis lead for further research.
COMPOUNDS HAVING ANTIBACTERIAL ACTIVITY
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Page/Page column 106; 107, (2014/11/13)
The present invention relates to compounds of formula (I) and their uses. In particular, though not exclusively, it concerns heterocyclic compounds that inhibit the biogenesis of adhesive pili in Gram- negative bacteria, and their use in the prevention or
HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 35, (2010/11/25)
The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the