Synthesis, Anticonvulsant and Antihypertensive Activities of 8-Substituted Quinoline Derivatives(Medicinal Chemistry)

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概要

• 論文の詳細を見る

• A series of 8-substituted quinolines were synthesized and tested against seizures induced by maximal electro shock (MES), pentylenetetrazole (scMet) and antihypertensive activities. Neurologic deficit was evaluated by the rotarod test. Among the newly synthesized derivatives, several compounds with a 2-hydroxypropyloxyquinoline moiety displayed excellent anticonvulsant and antihypertensive activities. Compound 20 (8- (3'- (4"-phenylpiperazino) -2'-hydroxypropyloxy) quinoline) was potent in both series as an anticonvulsive agent. 13 (8- (3'-piperazino) -2'-hydroxypropyloxyquinoline) and 14 (8- (3'-imidazolo) -2'-hydroxypropyloxyquinoline) showed very good anticonvulsant activities in the propanol series of compound, whereas in the ethane series, 1 (8- (2'-piperazino-ethanoxy) quinoline) and 2 (8- (2'-imidazolo-ethanoxy) quinoline) were the most active as anticonvulsive agents. Compounds 20 (8- (3'-(4"-phenylpiperazino) -2'-hydroxypropyloxy) quinoline), 13 (8- (3'-piperazino) -2'-hydroxy-propyloxyquinoline) and 19 (8- (3'-(4"-ethylpiperazino) -2'-hydroxypropyloxy) quinoline) have shown excellent antihypertensive activity. They have significantly antagonized the pressor response elicited by adrenaline. These pharmacological results suggest that their anticonvulsant and antihypertensive effects may be correlated to the presence of β-blocking properties, and that those properties depend on the presence of aryloxypropanolamine.

• 公益社団法人日本薬学会の論文
• 2004-10-01

著者

• Leonard J

  Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy

• Leonard Joseph

  Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy

• Sivakumar Ramaiah

  Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy

• MURUGANANTHAM Nithyanantham

  Department of Pharmaceutical Chemistry and Pharmacology, Vel's College of Pharmacy

• ANBALAGAN Navaneetharaman

  Department of Pharmaceutical Chemistry, C. L. Baid Metha College of Pharmacy

• GUNASEKARAN Vedachalam

  Department of Pharmaceutical Chemistry and Pharmacology, Vel's College of Pharmacy

• Gunasekaran Vedachalam

  Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy

• Leonard Joseph

  Department Of Medicinal Chemistry And Pharmacology Vel's College Of Pharmacy

• Muruganantham Nithyanantham

  Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy

• Anbalagan N

  Department Of Pharmaceutical Chemistry C. L. Baid Metha College Of Pharmacy

• Anbalagan Navaneetharaman

  Department Of Medicinal Chemistry And Pharmacology Vel's Colleg Of Pharmacy Old Pallavaram

関連論文

• Synthesis and Pharmacological Activities of 2-(3'-substituted-2'-hydroxypropylamino)pyridines
• Synthesis, Anticonvulsant and Antihypertensive Activities of 8-Substituted Quinoline Derivatives(Medicinal Chemistry)
• Synthesis and Anticonvulsant Activity of Novel 1-Substituted-1,2-dihydro-pyridazine-3,6-diones(Medicinal Chemistry)
• Pharmacological Evaluation of Some New 6-Amino/Methyl Pyridine Derivatives
• Pharmacological Evaluation of Some New 2-Substituted Pyridine Derivatives

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