ABSTRACT
A series of 2-substituted thiazol-4-ylethanamines have been synthesized and tested for their histaminergic H1-receptor activities. The compounds with 2-phenyl substitution, regardless of the different physicochemical properties of the meta-substituents at the phenyl ring, showed weak H1-agonistic activity with pD2 values ranging from 4.35 to 5.36. When the phenyl group was replaced by a benzyl group, the resulting compounds all exhibited weak H1-antagonistic activity (pA2: 4.14-4.82).
Subject(s)
Histamine Agonists/chemical synthesis , Thiazoles/chemical synthesis , Animals , Dose-Response Relationship, Drug , Guinea Pigs , Histamine Agonists/pharmacology , Ileum/drug effects , In Vitro Techniques , Ligands , Male , Muscle Contraction/drug effects , Muscle, Smooth/drug effects , Structure-Activity Relationship , Thiazoles/pharmacologyABSTRACT
We synthetized pyridobenzoxazocynone that differs in the enlarged eight-membered heterocyclic system from the basic structure of pyridobenzoxazepinones a known class of non-nucleoside HIV-1 reverse transcriptase inhibitors. Pyridobenzoxazocynone hydrochloride was found to inhibit HIV-1 reverse transcriptase activity. At concentration 0.35 microM the enzyme activity decreased by 64 +/- 14%. Higher concentrations of pyridobenzoxazocynone hydrochloride completely abolished the enzyme activity expressed as radioactivity of acid insoluble products. These results suggest that pyridobenzoxazocynones may represent a new class of HIV-1 reverse transcriptase inhibitors.
Subject(s)
HIV Reverse Transcriptase/antagonists & inhibitors , Oxazocines/chemical synthesis , Pyridines/chemical synthesis , Reverse Transcriptase Inhibitors/chemical synthesis , Gene Products, pol/antagonists & inhibitors , Humans , Molecular Structure , Oxazocines/pharmacology , Pyridines/pharmacology , Reverse Transcriptase Inhibitors/pharmacologyABSTRACT
Selected 1-aryl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline derivatives were synthesized and evaluated as beta-adreno-receptor agents. Some of the compounds showed week agonistic or antagonistic activity on these receptors.
Subject(s)
Adrenergic beta-Agonists/chemical synthesis , Adrenergic beta-Antagonists/chemical synthesis , Isoquinolines/chemical synthesis , Tetrahydroisoquinolines , Adrenergic beta-1 Receptor Agonists , Adrenergic beta-1 Receptor Antagonists , Adrenergic beta-2 Receptor Agonists , Adrenergic beta-2 Receptor Antagonists , Adrenergic beta-Agonists/pharmacology , Adrenergic beta-Antagonists/pharmacology , Animals , Bronchodilator Agents/chemical synthesis , Bronchodilator Agents/pharmacology , Female , Guinea Pigs , Heart/drug effects , In Vitro Techniques , Isoproterenol/pharmacology , Isoquinolines/pharmacology , Male , Muscle, Smooth/drug effects , Propranolol/pharmacology , Trachea/drug effectsABSTRACT
The synthesis and biological activity of new 10-13 membered oxygen-nitrogen heterocyclic systems condensed with two aromatic rings is reported. The structure-activity relationship of these new compounds in X-ray investigation has been studied. Pharmacological investigations have shown that the compounds exhibit weak neuroleptic activity.
Subject(s)
Antipsychotic Agents/chemical synthesis , Heterocyclic Compounds/chemical synthesis , Animals , Antipsychotic Agents/pharmacology , Behavior, Animal/drug effects , Cerebral Cortex/drug effects , Cerebral Cortex/metabolism , Dopamine D2 Receptor Antagonists , Heterocyclic Compounds/pharmacology , In Vitro Techniques , Male , Rats , Receptors, Dopamine D1/antagonists & inhibitors , Receptors, Muscarinic/drug effects , Receptors, Muscarinic/metabolism , Structure-Activity Relationship , X-Ray DiffractionABSTRACT
The synthesis and biological activity of a series of 4,5-dihydro-1H-2,4-benzodiazepine is reported. The structure-activity relationship of these new compounds was studied based on X-ray investigations. Pharmacological investigations have shown that the compounds exert depressive action on the central nervous system and exhibit weak neuroleptic activity.
Subject(s)
Antipsychotic Agents/chemical synthesis , Animals , Antipsychotic Agents/chemistry , Body Temperature/drug effects , Crystallization , Dextroamphetamine/pharmacology , Female , Lethal Dose 50 , Magnetic Resonance Spectroscopy , Male , Mice , Rats , Spectrophotometry, Infrared , Stereotyped Behavior/drug effects , X-Ray DiffractionSubject(s)
Antipsychotic Agents/pharmacology , Motor Activity/drug effects , Oxazocines/pharmacology , Stereotyped Behavior/drug effects , Animals , Antipsychotic Agents/chemical synthesis , Chemical Phenomena , Chemistry , Female , Male , Mice , Motor Activity/physiology , Oxazocines/chemical synthesis , Rats , Stereotyped Behavior/physiologySubject(s)
Azepines/pharmacology , Blood Circulation/drug effects , Central Nervous System/drug effects , Morpholines/pharmacology , Oxazocines/pharmacology , Piperazines/pharmacology , Azepines/chemical synthesis , Humans , Morpholines/chemical synthesis , Oxazocines/chemical synthesis , Piperazine , Piperazines/chemical synthesisSubject(s)
Blood Pressure/drug effects , Motor Activity/drug effects , Oxadiazoles/chemical synthesis , Oxazines/chemical synthesis , Animals , Chemical Phenomena , Chemistry , Drug Evaluation, Preclinical , Female , Male , Mice , Mice, Inbred BALB C , Oxazines/pharmacology , Rabbits , Rats , Rats, Inbred Strains , Tranquilizing Agents , Vasodilator AgentsSubject(s)
2,4-Dichlorophenoxyacetic Acid/analogs & derivatives , 2,4-Dichlorophenoxyacetic Acid/chemical synthesis , 2,4-Dichlorophenoxyacetic Acid/pharmacology , Animals , Antihypertensive Agents , Blood Pressure/drug effects , Body Temperature/drug effects , Chemical Phenomena , Chemistry , Depression, Chemical , Guinea Pigs , Humans , Ileum/drug effects , Mice , Mice, Inbred BALB C , Motor Activity/drug effects , Muscle, Smooth/drug effects , Rabbits , Rats , Rats, Inbred Strains , Sleep/drug effects , Stereotyped Behavior/drug effects , Tranquilizing AgentsSubject(s)
Psychotropic Drugs/chemical synthesis , Amphetamine/pharmacology , Animals , Benzoates/chemical synthesis , Benzoates/pharmacology , Chemical Phenomena , Chemistry , Diazonium Compounds/chemical synthesis , Diazonium Compounds/pharmacology , Drug Interactions , Lethal Dose 50 , Male , Mice , Mice, Inbred BALB C , Motor Activity/drug effects , Rats , Rats, Inbred StrainsABSTRACT
Anthelminthic activity of new esters of 3,4,5-trimethoxybenzoic acid containing rests of the title heterocyclic amines has been determined. 3-(Perhydroazepinyl)-propyl ester 6 acts on enchytraeids in vitro 56-fold stronger than piperazine adipate, 2-(perhydroazepinyl)-ethyl ester 5 is the most effective in a therapy of mice infested with nematodes.
Subject(s)
Anthelmintics/chemical synthesis , Azepines/chemical synthesis , Oxazocines/chemical synthesis , Animals , Anthelmintics/pharmacology , Anthelmintics/toxicity , Mice , Nematode Infections/drug therapyABSTRACT
New derivatives with the expected pharmacological activity of heterocyclic systems mentioned above having ether (1-6) and ester (7-10) groups were obtained.
