On April 30, 2004, Moloney, Gerard P.; Garavelas, Agatha; Martin, Graeme R.; Maxwell, Miles; Glen, Robert C. published an article.Category: thiazole The title of the article was Synthesis and serotonergic activity of variously substituted (3-amido)phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor. And the article contained the following:
The synthesis and vascular 5-HT1B receptor activity of a novel series of substituted 3-amido phenylpiperazine and 4-(4-methyl-1-piperazinyl)-1-benzo[b]thiophene derivatives is described. Modifications to the amido linked sidechains of the 3-amidophenyl piperazine derivatives and to the 2-side-chain of the 1-benzo[b]thiophene derivatives have been explored. Several compounds were identified which exhibited affinity at the vascular 5-HT1B receptor of pKB > 7.0. From the 3-amidophenyl-piperazine series, N-[5-(4-chlorophenyl)-2-thiazolyl]-3-(4-methyl-1-piperazinyl)benzamide (I) and from the benzo[b]thiophene-4-piperazine series N-(2-ethylphenyl)-4-(4-methyl-1-piperazinyl)benzo[b]thiophene-2-carboxamide (II) were identified as a highly potent, silent (as judged by the inability of angiotensin II to unmask 5-HT1B receptor mediated agonist activity in the rabbit femoral artery) and competitive vascular 5-HT1B receptor antagonist. The affinity of compounds from these two series of compounds for the vascular 5-HT1B receptor is discussed as well as a proposed mode of binding to the receptor pharmacophore. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Category: thiazole
The Article related to 5-ht antagonists (type 5-ht1b), 5-ht1b receptors role: bsu (biological study, unclassified), biol (biological study) (antagonists), molecular modeling, pharmacophores, structure-activity relationship, serotoninergic antagonist and other aspects.Category: thiazole
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica