On June 15, 2011, Capek, Petr; Zhang, Yan; Barlow, Deborah J.; Houseknecht, Karen L.; Smith, Garry R.; Dickerson, Tobin J. published an article.Recommanded Product: 16296-68-7 The title of the article was Enhancing the Pharmacokinetic Properties of Botulinum Neurotoxin Serotype A Protease Inhibitors through Rational Design. And the article contained the following:
Botulinum neurotoxin (BoNT), the etiol. agent that causes the neuroparalytic disease botulism, has become a highly studied drug target in light of the potential abuse of this toxin as a weapon of bioterrorism. In particular, small mol. inhibitors of the light chain metalloprotease of BoNT serotype A have received significant attention and a number of small mol. and biol. inhibitors have been reported. However, all small mols. reported have been identified from either primary screens or medicinal chem. follow-up studies, and the pharmacokinetic profiles of these compounds have not been addressed. In this study, we have removed the pharmacol. liabilities of one of the best compounds reported to date, 2,4-dichlorocinnamate hydroxamic acid, and in the process uncovered a related class of benzothiophene hydroxamic acids that are significantly more potent inhibitors of the BoNT/A light chain, while also possessing greatly improved ADME properties, with the best compound showing the most potent inhibition of BoNT/A light chain reported (Ki = 77 nM). Using a strategy of incorporating traditional drug development filters early into the discovery process, potential liabilities in BoNT/A lead compounds have been illuminated and removed, clearing the path for advancement into further pharmacol. optimization and in vivo efficacy testing. The experimental process involved the reaction of 5-Chlorobenzo[b]thiophene-3-carbaldehyde(cas: 16296-68-7).Recommanded Product: 16296-68-7
The Article related to botulinum neurotoxin serotype a protease inhibitor chlorocinnamate benzothiophene hydroxamate, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenothiophenes and other aspects.Recommanded Product: 16296-68-7
Referemce:
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem