Cardiovascular activity of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. Part 10(3): Dialkylamino-, pyrrolidyl- and morpholyl-alkyl-derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide, 7- or 5,7-halogen substituted.
A series of dialkylamino, pyrrolidyl and morpholyl-alkyl-derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide, 7- or 5,7-halogen substituted in the benzenoid moiety, was prepared and their cardiovascular activity studied. Most of the substances in question were capable of inducing a significant decrease in mean arterial blood pressure; some of them tended to increase pulse pressure or to cause bradycardia, an effect which was noted particularly in the case of compound 10 which reduced heart-rate by 85%. The structure/activity relationship of these substances, of the 6- and 6,7-halogen substituted isomers and of their corresponding non-substituted progenitors is examined.
Parenti
C
C
Dipartimento di Scienze Farmaceutiche, Universitá di Modena, Italy.
Costantino
L
L
Di Bella
M
M
Raffa
L
L
Baggio
G G
GG
D000818:Animals; D001581:Benzothiadiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D002317:Cardiovascular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002621:Chemistry; D003499:Cyclic S-Oxides / Q000138:chemical synthesis / Q000494:pharmacology; D004562:Electrocardiography; D006339:Heart Rate / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism
D001581:Benzothiadiazines; D002317:Cardiovascular Agents; D003499:Cyclic S-Oxides