Biomedical subjects
Publications and source records attributed to G Carenini.
A report is given of the synthesis and pharmacological investigation of some cyclohexylphenoxymethylmorpholines of general formula: Formula: (see text). The compound in which R = H and bearing the cyclohexyl group at the ortho position showed a pharmacological profile typical of drugs with antidepressant activity and was studied in detail in comparison with viloxazine and imipramine.
The effect of variation of the cycloaliphatic residue position on pharmacological activity was studied in two series of cyclohexylphenoxy derivatives (A and B). (Formula: See text) The ortho derivatives generally exhibit remarkably strong activity; (A) has an imipramine-like pharmacological profile; (B) with Y = H is more active than naphazoline and xylomethazoline as vasoconstrictor. The meta and para substituted derivatives and all (B) derivatives with R = CH3 exhibited no definite or interesting pharmacological activities.
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The paper describes the synthesis and the pharmacological evaluation of some derivatives of prenylamine, all with a cycloaliphatic ring within or instead of the isopropylamine moiety. Their general formulas are: (C6H5)2CH-CH2-CH2-NH-CH-CH2-R CH2 (I) (C6H5)2CH-CH2-CH2-NH-R' (II) where R contains and R' is a cycloaliphatic ring. Several compounds and particularly those of formula (I), and of formula (II), where the alicyclic ring had a bulky substituent in para were more active than prenylamine as coronary vasodilators on isolated guinea-pig heart (Langendorff). The most interesting derivative was M.G. 8926 [N-(3,3-diphenylpropyl)-alpha-methyl-beta-cyclohexylethylamine], which was more active than prenylamine on Langendorff's heart and in enhancing the pressor response to catecholamines and inhibiting the isoprenaline induced hypotension. Moreover, it had almost the same effects as prenylamine as spasmolytic, local and general anesthetic, on heart rate and arterial pressure and against coronary spasm from pitressin.
Seventeen acids with diphenylyl and cyclohexylphenyl groups were esterified with the hydroxyl group at position 21 of prednisolone and triamcinolone acetonide. Some of these esters showed marked activity against carrageenin edema and Selye spots in the rat, especially on local application.
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