Biomedical subjects
Publications and source records attributed to M Carissimi.
The synthesis and pharmacological investigation of 2-(2-thienyl)morpholine and some of its derivatives substituted on the nitrogen are described. The non-substituted compound showed interesting antidepressive properties with a pharmacological profile similar to that of imipramine.
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.
Derivatives of some primary amines and their N-benzyl derivatives containing a 4-cyclohexylphenyl or a 4-phenylcyclohexyl group were prepared. Pharmacological study showed clear analgesic activity in the phenylquinone test which was more accentuated for the 4-phenylcyclohexyl derivatives. All the compounds proved devoid of sympathomimetic activity on the cardiovascular system and without anorexic effect. Some of the compounds showed some antireserpine activity.
The effect of replacing the basic aliphatic residue of orciprenaline [(A); R = isopropylamino] and salbutamol [(B); R = tert.butylamino] with: a) a heterocyclic amine; b) a basic residue containing a phenylcyclohexane radical had been studied. The synthesis of the compounds is outlined. They were tested in vitro for relaxation of histamine-induced spasm of tracheal chains and on the isolated Langendorff heart, and in vivo according to the Konzett and Rössler technique and for their action on the cardiovascular system. In all tests the new derivataives were less active than the reference substances; the only exception was (A) where R = 4-phenylpiperidine (M.G. 6604), which was almost as active as orciprenaline in the Konzett and Rössler test, had one third of its activity on isolated trachea and showed absolutely no influence on heart rate in vitro or in vivo. Its effect was not inhibited by beta-blocking agents; it therefore showed an antihistaminic profile.
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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 synthesis of N6,O2'-dipivaloyl-cyclic AMP is described with some pharmacological tests made in comparison with the dibutyryl homolog. The two compounds proved equally active in increasing glycemia in the rabbit whereas the dipivaloyl derivative is less effective in counteracting contractions induced by imidazole in the isolated guinea-pig trachea.
The preparation of some derivatives of lidoflazine bearing a phenylcyclohexane residue in place of the m.xylene is described. Study of the coronary dilating activity on the isolated heart showed that this activity is markedly increased by the modification. Acute toxicity in rats is also strongly increased.
The paper describes the preparation and study of the pharmacological properties of a series of derivatives with the general formula. (see article) where R is a cyclohexyl or cyclohexenyl radical and R1 is a hydrogen, methyl or cyclohexyl. The compounds with a single cycloaliphatic radical ortho to the basic chain, and in particular the one with a cyclohexyl (exaprolol), were found to be particularly active in blocking the beta-adrenergic receptors, as antiarrhythmics and local anesthetics, while the introduction of a second radical or the shift of the cycloaliphatic radical to meta or para position caused the said pharmacological activities to disappear almost entirely, with the exception of the local anesthetic action.
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.
Some derivatives of oxacillin were prepared containing in place of the phenyl group a cyclohexyl, cyclohexylphenyl, phenylcyclohexyl or diphenylyl moiety. In the same compounds a methylene bridge between the carboxy group and the heterocyclic ring was inserted. The results of in vitro evaluation of antibacterial activity are given.
Some penicillins with structures similar to that of ampicillin and cyclacillin bearing the phenylcyclohexane grouping were prepared. In vitro tests of antibacterial activity showed that the introduction of this residue led to reduced activity in comparison with that of the parent compound.
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