10252-83-2Relevant articles and documents
N-(1,3,4-oxadiazol-2-yl)benzamide analogs, bacteriostatic agents against methicillin- and vancomycin-resistant bacteria
Opoku-Temeng, Clement,Naclerio, George A.,Mohammad, Haroon,Dayal, Neetu,Abutaleb, Nader S.,Seleem, Mohamed N.,Sintim, Herman O.
, p. 797 - 805 (2018)
Various reports of multidrug-resistant bacteria that are immune to all available FDA-approved drugs demand the development of novel chemical scaffolds as antibiotics. From screening a chemical library, we identified compounds with antibacterial activity.
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.
VACCINE ADJUVANT
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Page/Page column 69, (2020/06/10)
Compounds useful as an adjuvant, e.g., formulas (I)-(VI) and uses thereof, for example, with immunogenic moieties or other adjuvants, are provided.