Pharmacological Evaluation of Some New 6-Amino/Methyl 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 50 mg/kg, antihistaminic and cardiac activity were also studied. All the compounds exhibited significant anticonvulsant activity. Compounds 2-(2-hydroxy-3-piperazinopropylamino)-6-aminopyridine, 2-[2-hydroxy-3-(1-imidazolyl) propylamino]-6-aminopyridine, 2-[2-(1-imidazolyl)ethylamino]-6-methylpyridine and 2-[2-(methylamino)ethylamino]-6-methylpyridine were most active of the series against MES-induced seizures. Compounds 2-[2-(phenylamino)ethylamino]-6-aminopyridine, 2-[2-[bis(2-hydroxyethyl)amino]ethylamino]-6-aminopyridine, 2-[2-(diethylamino)ethylamino]-6-methylpyridine and 2-[2-hydroxy-3-(1-imidazolyl)propylamino]-6-methylpyridine exhibited significant decrease in the elevated motor activity at the dose of 50 mg/kg. Remarkable sympathetic blocking activity was observed with 2-(2-hydroxy-3-piperazinopropylamino)-6-aminopyridine, 2-(2-hydroxy-3-morpholinopropylamino)-6-methylpyridine and 2-(2-hydroxy-3-piperazinopropylamino)-6-methylpyridine only. Compounds 2-[2-(diethylamino)ethylamino]-6-aminopyridine, 2-[2-[bis(2-hydroxyethyl)amino]ethylamino]-6-aminopyridine, and 2-[2-(diethylamino)ethylamino]-6-methylpyridine 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
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Thomas Leonard
Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy Old Pallavara
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Sivakumar Ramaiah
Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy
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MURUGANANTHAM Nithyanantham
Department of Pharmaceutical Chemistry and Pharmacology, Vel's College of Pharmacy
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ANBALAGAN Navaneetharaman
Department of Pharmaceutical Chemistry, C. L. Baid Metha College of Pharmacy
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Gunasekaran Vedachalam
Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy
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RAVLEE Inguva
Department of Pharmaceutical Chemistry and Pharmacology, Vel's College of Pharmacy, Old Pallavaram
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Ravlee Inguva
Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy Old Pallavara
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Thomas Leonard
Department Of Medicinal Chemistry And Pharmacology Vel's Colleg Of Pharmacy Old Pallavaram
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Muruganantham Nithyanantham
Department Of Pharmaceutical Chemistry And Pharmacology Vel's College Of Pharmacy
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Anbalagan N
Department Of Pharmaceutical Chemistry C. L. Baid Metha College Of Pharmacy
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Anbalagan Navaneetharaman
Department Of Medicinal Chemistry And Pharmacology Vel's Colleg Of Pharmacy Old Pallavaram
関連論文
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- 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
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