[Heteropolycyclic systems. VII. 4-Dialkylaminoalkyl-2,3,3a,4-tetrahydro-1H-pyrrolo[2,1c] [1,2,4]benzothiadiazine-5,5-dioxides and their benzene-substituted derivatives. Cardiovascular effects in the anesthetized rat].
A series of 4-dimethylaminoethyl and 4-diethylaminoethyl derivatives of 2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c] [1,2,4] benzothiadiazine-5,5-dioxide substituted or unsubstituted in the benzene ring was prepared and subjected to preliminary investigation using the cardiovascular system of the anesthesized rat. Introduction of a basic group in the alkyl chain on N4 gives compounds with good hypotensive activity, this being most pronounced for (III, IV a and XIV) and an increase in differential pressure, marked for (V a, X, XII). These effects are sometimes accompanied by some bradycardizing activity, most marked for (V a) and (X). The results therefore confirm that derivatives of tetrahydropyrrolbenzothiazine have cardiovascular activity. Structure-activity relationships are discussed.
D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006439:Hemodynamics / Q000187:drug effects*; D008722:Methods; D051381:Rats; D013329:Structure-Activity Relationship; D013829:Thiadiazines / Q000138:chemical synthesis* / Q000494:pharmacology; D013843:Thiazines / Q000138:chemical synthesis*; D013997:Time Factors
D013829:Thiadiazines; D013843:Thiazines
Sistemi eteropoliciclici. Nota VII - 4-Dialchilaminoalchil-2,3,3a,4-tetraidro-1H-pirrolo[2,1-c] [1,2,4]benzotiadiazin-5,5-diossido e loro derivati bz-sostituiti. Effetti cardiovascolari nel ratto anestetizzato.