923605-07-6Relevant articles and documents
Synthesis and biological evaluation of 2,4,5-trisubstituted thiazoles as antituberculosis agents effective against drug-resistant tuberculosis
Karale, Uttam B.,Krishna, Vagolu Siva,Krishna, E. Vamshi,Choudhari, Amit S.,Shukla, Manjulika,Gaikwad, Vikas R.,Mahizhaveni,Chopra, Sidharth,Misra, Sunil,Sarkar, Dhiman,Sriram, Dharmarajan,Dusthackeer, V.N. Azger,Rode, Haridas B.
, p. 315 - 328 (2019/06/14)
The dormant and resistant form of Mycobacterium tuberculosis presents a challenge in developing new anti-tubercular drugs. Herein, we report the synthesis and evaluation of trisubstituted thiazoles as antituberculosis agents. The SAR study has identified a requirement of hydrophobic substituent at C2, ester functionality at C4, and various groups with hydrogen bond acceptor character at C5 of thiazole scaffold. This has led to the identification of 13h and 13p as lead compounds. These compounds inhibited the dormant Mycobacterium tuberculosis H37Ra strain and M. tuberculosis H37Rv selectively. Importantly, 13h and 13p were non-toxic to CHO cells. The 13p showed activity against multidrug-resistant tuberculosis isolates.
PIM KINASE INHIBITORS AND METHODS OF THEIR USE
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Page/Page column 104, (2009/10/22)
The present invention relates to new compounds of Formulas (I) and (II), their tautomers, stereoisomers and polymorphs, and pharmaceutically acceptable salts, esters, metabolites or prodrugs thereof, compositions of the new compounds together with pharmac
