On March 13, 2014, Lazerwith, Scott E.; Lew, Willard; Zhang, Jennifer; Morganelli, Philip; Liu, Qi; Canales, Eda; Clarke, Michael O.; Doerffler, Edward; Byun, Daniel; Mertzman, Michael; Ye, Hong; Chong, Lee; Xu, Lianhong; Appleby, Todd; Chen, Xiaowu; Fenaux, Martijn; Hashash, Ahmad; Leavitt, Stephanie A.; Mabery, Eric; Matles, Mike; Mwangi, Judy W.; Tian, Yang; Lee, Yu-Jen; Zhang, Jingyu; Zhu, Christine; Murray, Bernard P.; Watkins, William J. published an article.Category: chlorides-buliding-blocks The title of the article was Discovery of GS-9669, a Thumb Site II Non-Nucleoside Inhibitor of NS5B for the Treatment of Genotype 1 Chronic Hepatitis C Infection. And the article contained the following:
Investigation of thiophene-2-carboxylic acid HCV NS5B site II inhibitors, guided by measurement of cell culture medium binding, revealed the structure-activity relationships for intrinsic cellular potency. The pharmacokinetic profile was enhanced through incorporation of heterocyclic ethers on the N-alkyl substituent. Hydroxyl groups were incorporated to modulate protein binding. Intrinsic potency was further improved through enantiospecific introduction of an olefin in the N-acyl motif, resulting in the discovery of the phase 2 clin. candidate GS-9669. The unexpected activity of this compound against the clin. relevant NS5B M423T mutant, relative to the wild type, was shown to arise from both the N-alkyl substituent and the N-acyl group. The experimental process involved the reaction of trimethyloxosulphonium chloride(cas: 5034-06-0).Category: chlorides-buliding-blocks
The Article related to gs9669 clin candidate synthesis hepatitis c infection treatment, Heterocyclic Compounds (One Hetero Atom): Thiophenes and other aspects.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics