Synthesis and pharmacological activity of N-(2,2-dimethyl-3,4-dihydro-2H-1-benzopyran-4-yl)-4H-1,2,4-benzothiadiazine-3-carboxamides 1,1-dioxides on rat uterus, rat aorta and rat pancreatic β-cells.
N-(2,2-Dimethyl-3,4-dihydro-2H-1-benzopyran-4-yl)-4H-1,2,4-benzothiadiazine-3-carboxamides 1,1-dioxides were prepared and evaluated on rat uterus, rat aortic rings and rat pancreatic β-cells. Pharmacological studies conducted on rat uterus indicated that several of these original hybrid compounds displayed a strong myorelaxant activity. The most active compounds hold a bromine atom at the 6-position of the dihydrobenzopyran ring. Moreover, the compounds failed to display a marked inhibitory effect on insulin secretion and vascular myogenic activity. These features suggest that the 6-bromo compounds could be relatively selective towards the uterine smooth muscle.
Laboratoire de Phytochimie et de Pharmacologie, Département de Chimie, Faculté des Sciences, Université de Jijel, B.P. 98 Ouled Aissa, 18000 Jijel, Algeria.
Smail
S
Khelili
Nadjib
N
Kihal
Mohamed
M
Yekhlef
Pascal
P
de Tullio
Philippe
P
Lebrun
Bernard
B
Pirotte
D000818:Animals; D001011:Aorta / Q000187:drug effects* / Q000502:physiology; D001581:Benzothiadiazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D060326:Chemistry Techniques, Synthetic; D005260:Female; D066298:In Vitro Techniques; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D050417:Insulin-Secreting Cells / Q000187:drug effects* / Q000378:metabolism; D009126:Muscle Relaxation / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects / Q000502:physiology; D051381:Rats; D014599:Uterus / Q000187:drug effects* / Q000502:physiology
D001581:Benzothiadiazines; D007328:Insulin