[Crystalline form of progesterone in silicone elastomers].
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Biomedical subjects
Publications and source records attributed to R Cameroni.
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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.
A series of 4-propylderivatives of 2,3,3a,4-tetrahydro-1H-pyrrolo[2,1-c] [1,2,4]benzothiadizine-5,5-dioxide substituted or unsubstituted in the benzene ring was synthesized. Derivatives of these compounds together with those of the corresponding 4-methyl and 4-ethyl derivatives prepared previously were tested for cardiovascular effects in the anesthesized rat. All the compounds studied showed hypotensive activity which was particularly intense for compounds (X), (XIX), (XXII), (XXV), and produced an increase in differential pressure marked for (XXV) and (XXVIII) which was often accompanied by pronounced bradycardia (XVII), (XVIII) and (XIX). The results prove that derivatives of 2,3,3a,4-tetrahydro-1H-pyrrolo-[2,1-c][1,2,4]benzothiadiazine-5,5-dioxide have hypotensive and bradycardizing activity. Structure-activity relationships are discussed.
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The preparation of some 4-alkyl derivatives of 2,3,3a,4--tetrahydro-1H-pyrrolo(2,1-c)(1,2,4)benzothiadiazin-5,5-dioxode and bz-substituted derivatives by the action of alkyl iodides on the LiAlH4 reduction products of the corresponding 2,3-dihydro-1H-pyrrolo(2,1-c)(1,2,4)benzothiadiazin-5,5-dioxide is described. It was found that some of the substances synthesized exist in polymorphous forms and it was possible to isolate these.
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