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Biomedical subjects

E Marmo

Publications and source records attributed to E Marmo.

At least 127 records · Page 7Linked to original sources
PubMed1983

N-monosubstituted urethanes and esters of 6-cis-dimethylamino-1,3,3-trimethyl-2-oxabicyclo-[2.2.2]octan-5-trans-ol with hypotensive and other activities.

The synthesis of 6-cis-dimethylamino-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-5-trans-ol (III) starting from 1,3,3-trimethyl-6-nitrimino-2-oxabicyclo[2.2.2]octane is described. Starting from aminoalcohol (III), a series of N-substituted urethanes (IV) and esters (V), as well as the rigid analogue of acetylcholine (VII), were prepared. A number of compounds (V) and particularly (IV) showed remarkable hypotensive and bradycardic activities in rats, whereas the p-aminobenzoate (V h) showed infiltration anesthesia in mice comparable to that of lidocaine. Antiarrhythmic activity in mice and antiacetylcholine activity in vitro are also reported.

Acetylcholine↗
PubMed1983

Research on heterocyclic compounds. XIV - Imidazothiazole and imidazobenzothiazole derivatives: synthesis and antiinflammatory activity.

A group of ethyl 6-methylimidazo[2,1-b]thiazole-5-carboxylates and 2-methylimidazo[2,1-b]benzothiazole-3-carboxylates was prepared by reaction of ethyl 2-chloroacetoacetate with some 2-aminothiazoles and 2-aminobenzothiazoles, respectively. Such reactions may sometimes afford a side product which was isolated and characterized. The ethyl esters were then converted into the corresponding acids by hydrolysis. Three of these acids were evaluated for antiinflammatory, analgesic, and antipyretic activities, as well as for ulcerogenic potential.

Animals↗
PubMed1983

Synthesis and pharmacological activity of some 1-alkylamino-3-(2'-methoxy-4'-diethylcarbamoyl-phenoxy)propan-2-ols.

The synthesis and pharmacological properties of some 1-alkylamino-3-(2'-methoxy-4'-diethylcarbamoylphenoxy)propan-2-ols, related to beta-adrenergic drugs, are described. The above compounds were found to possess beta 1 and beta 2-adrenolytic activity associated with local anesthetic and antiarrhythmic activities, which are clearly inferior to those of propranolol.

Adrenergic beta-Antagonists↗
PubMed1983

Derivatives of 4,5,6,7-tetrahydro-7,8,8-trimethyl-3-phenylamino-4,7-methano-2H-indazole with hypoglycemic and hypotensive activities.

By reaction of camphor enamine (I) with phenyl isothiocyanate, the N-phenyl thiocarboxamide (II) was obtained in excellent yield, and in turn gave 4,5,6,7-tetrahydro-7,8,8-trimethyl-3-phenylamino-4,7-methano-2H-indazole (III) in very good yield by reaction with hydrazine hydrate. A series of N-substituted ureas (IV) were synthesized in satisfactory yield by reaction of (III) with alkyl and aryl isocyanates. Ureas (IV) showed in general hypoglycemic and in some cases hypotensive activity in rats, whereas only hypotensive activity was present in the thiocarboxamide (II). Effects on heart rate, antiinflammatory and antipyretic activities in rats, infiltration anesthesia and antiarrhythmic activity in mice, as well as antiacetylcholine activity in vitro, are also reported.

Anesthesia, Intravenous↗
PubMed1983

Research on heterocyclic compounds. XV. Substitution influence on the pharmacological activity in a series of imidazo[1,2-a]pyridines.

We have taken into consideration a group of 28 imidazo [1,2-a]pyridine derivatives, some of which were already known, whereas the others have been synthesized and characterized to complete the series. Antiinflammatory, analgesic, antipyretic and ulcerogenic activities of such compounds were evaluated in comparison with indomethacin. The pharmacological data demonstrated the effects exerted on activity by the presence on the heterocyclic system of methyl substituents and/or an acidic moiety.

Animals↗
PubMed1983

Derivatives of 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane with hypotensive activity. I.

The synthesis of three series of glycinamides (IV), amides (V) and diamines (VI) starting from 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane is described. Some of compounds (IV), (V) and (VI) showed a moderate hypotensive activity in rats. Effects on heart rate in rats, infiltration anesthesia and antiarrhythmic activity in mice, as well as antiacetylcholine activity in vitro, are also reported.

Acetylcholine↗
PubMed1983

Derivatives of 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane with hypotensive activity. II.

The synthesis of a series of alkyl and aryl ureas (II) starting from 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane is described. Some of these compounds showed a moderate hypotensive activity in rats. Effects on heart rate in rats, infiltration anesthesia and antiarrhythmic activity in mice, as well as antiacetylcholine activity in vitro, are also reported.

Acetylcholine↗
PubMed1982

N-Phenyl-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-cis-amine derivatives with hypotensive and other activities.

The synthesis of N-phenyl-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-cis-amine (III) starting from 6-nitrimino-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octane, as well as of a series of amides (IV) and ureas (VI) derived from (III), is described. A number of compounds (IV) showed strong hypotensive and bradycardic activity in rats, whereas the urea (IVb) showed infiltration anesthesia in mice similar to that of lidocaine. Antiarrhythmic activity in mice and antiacetylcholine activity in vitro are also reported.

Acetylcholine↗
PubMed1982

N-Monosubstituted urethanes of 6-cis-dialkylamino-1,3,3-trimethyl-2-oxabicyclo [2.2.2] octan-5-trans-ols with hypotensive and other activities.

The synthesis of three series of N-monosubstituted urethanes of 6-cis-dialkylamino-1,3,3-trimethyl-2-oxabicyclo [2.2.2] octan-5-transols (IV), (V) and (VI) (dialkylamino = pyrrolidino, piperidino, morpholino) by reaction of the corresponding aminoalcohols with alkyl or aryl isocyanates, is described. A number of compounds (IV) and (V) showed remarkable hypotensive and bradycardic activity in rats, whereas (IV c) showed infiltration anesthesia and (IV n) antiarrhythmic activity in mice comparable to those of lidocaine. Antiacetylcholine activity in vitro is also reported.

Acetylcholine↗