Synthetic studies to help elucidate the metabolism of the preclinical candidate TBAJ-876-a less toxic and more potent analogue of bedaquiline was written by Choi, Peter J.;Conole, Daniel;Sutherland, Hamish S.;Blaser, Adrian;Tong, Amy S. T.;Cooper, Christopher B.;Upton, Anna M.;Palmer, Brian D.;Denny, William A.. And the article was included in Molecules in 2020.Related Products of 51834-97-0 This article mentions the following:
Bedaquiline is a novel drug approved in 2012 by the FDA for treatment of drug-resistant tuberculosis (TB). Although it shows high efficacy towards drug-resistant forms of TB, its use has been limited by the potential for significant side effects. In particular, bedaquiline is a very lipophilic compound with an associated long terminal half-life and shows potent inhibition of the cardiac potassium hERG channel, resulting in QTc interval prolongation in humans that may result in cardiac arrhythmia. To address these issues, we carried out a drug discovery program to develop an improved second generation analog of bedaquiline. From this medicinal chem. program, a candidate (TBAJ-876) has been selected to undergo further preclin. evaluation. During this evaluation, three major metabolites arising from TBAJ-876 were observed in several preclin. animal models. We report here our synthetic efforts to unequivocally structurally characterize these three metabolites through their independent directed synthesis. In the experiment, the researchers used many compounds, for example, 5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0Related Products of 51834-97-0).
5-Hydroxy-2-methoxylpyridine (cas: 51834-97-0) belongs to pyridine derivatives. In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Related Products of 51834-97-0