Studies on the chemistry of thienoannelated O,N- and S,N-containing heterocycles. Part 19: Thieno[2,3-b][1,4]thiazines with calcium antagonistic and potassium opening activities

Citation
T. Erker et al., Studies on the chemistry of thienoannelated O,N- and S,N-containing heterocycles. Part 19: Thieno[2,3-b][1,4]thiazines with calcium antagonistic and potassium opening activities, ARCH PHARM, 333(2-3), 2000, pp. 58-62
Citations number
7
Categorie Soggetti
Pharmacology & Toxicology
Journal title
ARCHIV DER PHARMAZIE
ISSN journal
03656233 → ACNP
Volume
333
Issue
2-3
Year of publication
2000
Pages
58 - 62
Database
ISI
SICI code
0365-6233(200003)333:2-3<58:SOTCOT>2.0.ZU;2-O
Abstract
In this study novel substituted 6-benzyl-thieno[2,3-b] [1,4]thiazines with an urea moiety were synthesized. Structural modifications of the amino side chain were carried out with the aim of finding tissue specific compounds. The effects on papillary muscles, right atria, aortic strips, and terminal ilea were investigated. Compounds 10c and 10d showed the most potent negati ve inotropic effect. The calcium antagonism of all derivatives occurred in a non-competitive manner, which may indicate that they also have potassium channel opening activities.