14446-47-0Relevant articles and documents
Reversible inactivation of bovine plasma amine oxidase by cysteamine and related analogs
Jeon, Heung Bae,Jang, Yujin
, p. 442 - 446 (2010)
Cysteamine (1) was reported many years ago to reversibly inhibit lentil seedling amine oxidase, through the formation of a complex with thioacetaldehyde, the turnover product of 1. Herein, cysteamine (1) and its analogs 2-(methylamino)ethanethiol (3) and 3-aminopropanethiol (6) were found to be reversible inhibitors of bovine plasma amine oxidase (BPAO), but 2-(methylthio)ethylamine (7) was determined to be a weak irreversible inhibitor of BPAO. Based on our results, indicating the necessity of a sulfhydryl-amine for reversible inactivation of BPAO, the failure of inhibited BPAO to recover activity after gel filtration, the first-order kinetics of activity recovery upon dialysis, and 2,4,6-trihydroxyphenylalanine quinine (TPQ) cofactor transformation which indicated from the results of phenylhydrazine titration and substrate protection, we propose a mechanism for the reversible inactivation of BPAO by 1 involving the formation of a cofactor adduct, thiazolidine, between BPAO and 1.
PROCESS FOR THE PREPARATION OF TENELIGLIPTIN AND ITS NOVEL INTERMEDIATES
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Page/Page column 26, (2016/01/26)
The present invention relates to a novel process for the preparation of Teneligliptin or its pharmaceutically acceptable salts and its hydrates thereof. The invention also relates to novel intermediates used in the synthesis of Teneligliptin and their preparation.
Synthesis of 2,3,4,7-tetrahydro[1,4]thiazepines from thiazolidines and β-enaminonitriles
Calvo, Luis A.,González-Ortega, Alfonso,Marcos, Rocío,Pérez, Mónica,Sa?udo, M. Carmen
, p. 3691 - 3700 (2008/09/20)
A wide library of 2,3,4,7-tetrahydro[1,4]thiazepines have been prepared by simple heating of thiazolidine and β-enaminonitrile derivatives in acetonitrile. The procedure, whose yields depend on the nature and position of the substituents, gave good results if the substituents were not very bulky but it is less effective when starting from 2-substituted thiazolidines.