Aggarwal, Anup published the artcileDevelopment of a Novel Lead that Targets M. tuberculosis Polyketide Synthase 13, Quality Control of 903899-13-8, the publication is Cell (Cambridge, MA, United States) (2017), 170(2), 249-259.e25, database is CAplus and MEDLINE.
Widespread resistance to first-line TB drugs is a major problem that will likely only be resolved through the development of new drugs with novel mechanisms of action. The authors have used structure-guided methods to develop a lead mol. that targets the thioesterase activity of polyketide synthase Pks13, an essential enzyme that forms mycolic acids, required for the cell wall of Mycobacterium tuberculosis. The authors’ lead, TAM16, is a benzofuran class inhibitor of Pks13 with highly potent in vitro bactericidal activity against drug-susceptible and drug-resistant clin. isolates of M. tuberculosis. In multiple mouse models of TB infection, TAM16 showed in vivo efficacy equal to the first-line TB drug isoniazid, both as a monotherapy and in combination therapy with rifampicin. TAM16 has excellent pharmacol. and safety profiles, and the frequency of resistance for TAM16 is â?00-fold lower than INH, suggesting that it can be developed as a new antitubercular aimed at the acute infection.
Cell (Cambridge, MA, United States) published new progress about 903899-13-8. 903899-13-8 belongs to pyridine-derivatives, auxiliary class Pyridine,Boronic acid and ester,Alcohol,Boronic Acids,Boronic acid and ester, name is (6-Hydroxypyridin-3-yl)boronic acid, and the molecular formula is C5H6BNO3, Quality Control of 903899-13-8.
Referemce:
https://en.wikipedia.org/wiki/Pyridine,
Pyridine | C5H5N – PubChem