Pharmacological Evaluation of Some New 2-Substituted Pyridine Derivatives.

Abstract

In the present study, a series of 2-substituted-pyridines were synthesized and characterized by IR, 1 H-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-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 50 mg/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.

Synthesis, Anticonvulsant and Antihypertensive Activities of 8-Substituted Quinoline Derivatives

“…The increase in the carbon atom number at the 4th position of piperazine influenced the activity remarkably. In the propanol series (12)(13)(14)(15)(16)(17)(18)(19)(20), only compounds 13, 14, 19 and 20 were found to have a high degree of protection against MES-induced convulsions. 4-phenylpiperazino substituted compounds at the 3Ј position showed higher protection than the other substitutions at piperazine compounds.…”

“…We have already reported the potential anticonvulsant activity and the b-blocking activity of propanolamine, aminopropane and aminoethane from our laboratory. [14][15][16][17][18][19][20] To explore the heteroaryl and propanolamine/aminoethane combination, it was envisaged that chemical entities with both quinoline and aryloxypropanolamine/aminoethane moieties would result in compounds with interesting biological activities.…”

Anticonvulsant Activity of a Combined Pharmacophore of Pyrazolo-pyridines with Lesser Toxicity in Mice

“…Numerous currently used drugs in various diseases contain the pyridinyl pharmacophore that incited the scientists worldwide to investigate different derivatives possessing pyridine nucleus for anticonvulsant activity. The results obtained were found to be very encouraging [4][5][6][7] and the research to get better agents is ongoing.…”

Synthesis and characterization of some heterocyclic schiff bases: potential anticonvulsant agents

“…Pyridines and its derivatives have already been reported with anticonvulsant (Kaminski et al, 2006) (Narendar et al, 2003), cardiotonic (Bekhit and Baraka, 2005), antihypertensive (Ludden et al, 1979), b-adrenergic blocking (Ferrarinia et al, 2000) activities. Pyridine and amino-pyridines are well known class of compounds for its potassium channel blocking action.…”