In 2022,Naidu, B. Narasimhulu; Patel, Manoj; McAuliffe, Brian; Ding, Bo; Cianci, Christopher; Simmermacher, Jean; Jenkins, Susan; Parker, Dawn D.; Sivaprakasam, Prasanna; Khan, Javed A.; Kish, Kevin; Lewis, Hal; Hanumegowda, Umesh; Krystal, Mark; Meanwell, Nicholas A.; Kadow, John F. published an article in Journal of Medicinal Chemistry. The title of the article was 《Design, Synthesis, and Preclinical Profiling of GSK3739936 (BMS-986180), an Allosteric Inhibitor of HIV-1 Integrase with Broad-Spectrum Activity toward 124/125 Polymorphs》.Category: pyridine-derivatives The author mentioned the following in the article:
The design, synthesis, and optimization of pyridine-based I [R = Ph, 4-MeC6H4, 4-ClC6H4, etc.] and II [R1 = 3-(4-fluorophenyl)propyl, 2-(4-fluorophenyl)ethylamino, 3-(4-fluorophenyl)propoxy, etc.] allosteric integrase inhibitors were reported. Optimization was conducted with a specific emphasis on the inhibition of the 124/125 polymorphs such that the designed compounds showed excellent potency in-vitro against majority of the 124/125 variants. In vivo profiling of promising preclin. lead I [R = 4-FC6H4] showed that it exhibited a good pharmacokinetic (PK) profile in preclin. species, which resulted in a low predicted human efficacious dose. However, findings in rat toxicol. studies precluded further development of I [R = 4-FC6H4]. The results came from multiple reactions, including the reaction of 2-(2-Hydroxyethyl)pyridine(cas: 103-74-2Category: pyridine-derivatives)
2-(2-Hydroxyethyl)pyridine(cas: 103-74-2) belongs to pyridine. Pyridine derivatives lend themselves to many roles in the spirited field of supramolecular chemistry – whether as the ligand backbone of metal-organic polymers or presiding over the key electronic stations of nanodevices. In biochemistry, pyridine-containing cofactors are necessary nutrients on which our lives depend. Category: pyridine-derivatives