440087-51-4Relevant articles and documents
New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold
Pajk, Stane,?ivec, Matej,?ink, Roman,Sosi?, Izidor,Neu, Margarete,Chung, Chun-Wa,Martínez-Hoyos, María,Pérez-Herrán, Esther,álvarez-Gómez, Daniel,álvarez-Ruíz, Emilio,Mendoza-Losana, Alfonso,Castro-Pichel, Julia,Barros, David,Ballell-Pages, Lluís,Young, Robert J.,Convery, Maire A.,Encinas, Lourdes,Gobec, Stanislav
, p. 252 - 257 (2016/05/02)
Tetrahydropyran derivative 1 was discovered in a high-throughput screening campaign to find new inhibitors of mycobacterial InhA. Following initial in-vitro profiling, a structure-activity relationship study was initiated and a focused library of analogs was synthesized and evaluated. This yielded compound 42 with improved antimycobacterial activity and low cytotoxicity. Additionally, the crystal structure of InhA in complex with inhibitor 1 was resolved, to reveal the binding mode and provide hints for further optimization.
3- Or 4-monosubstituted phenol derivatives useful as H3 ligands
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Page/Page column 24-25, (2010/02/14)
The invention relates to 3- or 4-monosubstituted phenol derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. Said 3- or 4-monosubstituted phenol derivatives are H3 ligands and are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.