Development of a more highly selective M1 antagonist from the continued optimization of the MLPCN Probe ML012 was written by Melancon, Bruce J.;Lamers, Alexander P.;Bridges, Thomas M.;Sulikowski, Gary A.;Utley, Thomas J.;Sheffler, Douglas J.;Noetzel, Meredith J.;Morrison, Ryan D.;Scott Daniels, J.;Niswender, Colleen M.;Jones, Carrie K.;Jeffrey Conn, P.;Lindsley, Craig W.;Wood, Michael R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Category: thiazole This article mentions the following:
This Letter describes the continued optimization of an MLPCN probe mol. (ML012) through an iterative parallel synthesis approach. After exploring extensive modifications throughout the parent structure, we arrived at a more highly M1-selective antagonist, compound (I; VU0415248). Muscarinic subtype selectivity across all five human and rat receptors for I, along with rat selectivity for the lead compound (ML012), is presented. In the experiment, the researchers used many compounds, for example, 2-Acetamido-4-methylthiazole-5-sulfonyl chloride (cas: 69812-29-9Category: thiazole).
2-Acetamido-4-methylthiazole-5-sulfonyl chloride (cas: 69812-29-9) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica