Pharmacological Evaluation of Some New 2-Substituted Pyridine Derivatives

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概要

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• In the present study, a series of 2-substituted-pyridines were synthesized and characterized by IR, ^1H-NMR and Elemental Analysis. The compounds were assayed against seizures induced by maximal electro shock (MES) and pentylenetetrazole (scMet). Neurologic deficit was evaluated by the rotarod test. The decrease in the elevated motor activity by introceptive chemical stimuli (amphetamine antagonistic activity) was studied at the dose level of 25 and 50mg/kg, antihistaminic and cardiac activity were also studied. All the compounds exhibited significant anticonvulsant activity. Compounds 2-(2'-piperazino-ethanoxy) pyridine, 2-(3'-morpholino-2'-hydroxypropyloxy)-pyridine, 2-(3'-piperidino-2'-hydroxypropyloxy) pyridine and 2-(3'-piperazino-2'-hydroxypropyloxy)pyridine were most active of the series against MES-induced seizures. Compounds 2-(2'-piperazino-ethanoxy)pyridine, 2-(2'-phenylamino-ethanoxy)pyridine, 2-(3'-imidazolo-2'-hydroxypropyloxy)pyridine, 2-(3'-methylamino-2'-hydroxypropyloxy)pyridine and 2-(3'-piperidino-2'-hydroxypropyloxy)pyridine exhibited significant decrease in the elevated motor activity at the dose of 50mg/kg. Remarkable sympathetic blocking activity was observed with 2-(3'-piperazino-2'-hydroxypropyloxy)pyridine, 2-(3'-piperidino-2'-hydroxypropyloxy)pyridine and 2-(3'-imidazolo-2'-hydroxypropyloxy)pyridine only. Compounds 2-(2'-morpholino-ethanoxy)pyridine, 2-(2'-piperidino-ethanoxy)pyridine, 2-(2'-piperazino-ethanoxy)pyridine, 2-(2'-imidazolo-ethanoxy)pyridine, 2-(2'-diphenylamino-ethanoxy)pyridine, 2-(2'-diethanolamino-ethanoxy)pyridine, 2-(2'-phenylamino-ethanoxy)pyridine and 2-(2'-(4"-hydroxy)phenylamino-ethanoxy)pyridine exhibited significant blocking of histamine induced contraction on guinea pig ileum.

• 公益社団法人日本薬学会の論文
• 2003-02-01

著者

• Thomas Leonard

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

• 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

• NARENDAR Parasuraman

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

• PARTHIBAN Jeyaraman

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

• Parthiban Jeyaraman

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

• Thomas Leonard

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

• Narendar Parasuraman

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

• 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 1,8-Naphthyridine Derivatives
• 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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