Design, synthesis, structure-activity relationship, and in vivo activity of azabicyclic aryl amides as α7 nicotinic acetylcholine receptor agonists was written by Walker, Daniel P.;Wishka, Donn G.;Piotrowski, David W.;Jia, Shaojuan;Reitz, Steven C.;Yates, Karen M.;Myers, Jason K.;Vetman, Tatiana N.;Margolis, Brandon J.;Jacobsen, E. Jon;Acker, Brad A.;Groppi, Vincent E.;Wolfe, Mark L.;Thornburgh, Bruce A.;Tinholt, Paula M.;Cortes-Burgos, Luz A.;Walters, Rodney R.;Hester, Matthew R.;Seest, Eric P.;Dolak, Lester A.;Han, Fusen;Olson, Barbara A.;Fitzgerald, Laura;Staton, Brian A.;Raub, Thomas J.;Hajos, Mihaly;Hoffmann, William E.;Li, Kai S.;Higdon, Nicole R.;Wall, Theron M.;Hurst, Raymond S.;Wong, Erik H. F.;Rogers, Bruce N.. And the article was included in Bioorganic & Medicinal Chemistry in 2006.Safety of Benzothiazole-5-carboxylic acid This article mentions the following:
A novel set of azabicyclic aryl amides have been identified as potent and selective agonists of the α7 nAChR. A two-pronged approach was taken to improve the potential hERG liability of previously disclosed α7 nAChR agonist, PNU-282,987, while maintaining the compound’s other desirable pharmacol. properties. The first approach involved further exploration of the aryl carboxylic acid fragment of PNU-282,987, while the second approach focused on modification of the azabicyclic amine portion of PNU-282,987. The best compounds from each series are characterized by rapid brain penetration, good oral bioavailability in rat, and demonstrate in vivo efficacy in a rat P50 auditory sensory gating assay. At least one analog from each series shows an improved hERG safety profile over PNU-282,987. In the experiment, the researchers used many compounds, for example, Benzothiazole-5-carboxylic acid (cas: 68867-17-4Safety of Benzothiazole-5-carboxylic acid).
Benzothiazole-5-carboxylic acid (cas: 68867-17-4) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Safety of Benzothiazole-5-carboxylic acid
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica