Publications (5) View all
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Article: Synthesis, anticonvulsant and antihypertensive activities of 8-substituted quinoline derivatives.
Nithyanantham Muruganantham, Ramaiah Sivakumar, Navaneetharaman Anbalagan, Vedachalam Gunasekaran, Joseph Thomas Leonard[show abstract] [hide abstract]
ABSTRACT: 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'-hydroxypropyloxyquinoline) 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 beta-blocking properties, and that those properties depend on the presence of aryloxypropanolamine.Biological & Pharmaceutical Bulletin 11/2004; 27(10):1683-7. · 1.66 Impact Factor -
Article: Synthesis and anticonvulsant activity of novel 1-substituted-1,2-dihydro-pyridazine-3,6-diones.
[show abstract] [hide abstract]
ABSTRACT: The synthesis and pharmacological evaluation of novel 1-substituted-1,2-dihydro-pyridazine-3,6-diones (4a--l, 5a--j) as potential anticonvulsant agents are described. The compounds were tested in vivo for the anticonvulsant activity. The compound which have maximum protection against MES induced seizures is 1-[3-(2-aminophenylamino)-2-hydroxypropyl)-1,2-dihydro-pyridazine-3,6-dione 4h (ED(50)=44.7 mg x kg(-1) i.p.) 1-[2-hydroxy-3-piperazin1-yl-propyl)-1,2-dihydro-pyridazine-3,6-dione 4c (ED(50)=72 mg x kg(-1) i.p.) and 1-[2-hydroxy-3-imidazol-1-yl-propyl)-1,2-dihydro-pyridazine-3,6-dione 4d (ED(50)=79 mg x kg(-1) i.p.) were also found to have maximum protection against MES induced seizures. Whereas all these compounds failed to protect the animals from subcutaneous pentylenetetrazole (Metrozol) seizure threshold test (sc-Met).Biological & Pharmaceutical Bulletin 11/2003; 26(10):1407-11. · 1.66 Impact Factor -
SourceAvailable from: pharm.or.jp
Article: Pharmacological evaluation of some new 2-substituted pyridine derivatives.
Parasuraman Narendar, Jeyaraman Parthiban, Navaneetharaman Anbalagan, Vedachalam Gunasekaran, Joseph Thomas Leonard[show abstract] [hide abstract]
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.Biological & Pharmaceutical Bulletin 03/2003; 26(2):182-7. · 1.66 Impact Factor -
SourceAvailable from: pharm.or.jp
Article: Pharmacological evaluation of some new 6-amino/methyl pyridine derivatives.
Inguva Ravlee, Ramaiah Sivakumar, Nithyanantham Muruganantham, Navaneetharaman Anbalagan, Vedachalam Gunasekaran, Joseph Thomas Leonard[show abstract] [hide abstract]
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-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.CHEMICAL & PHARMACEUTICAL BULLETIN 03/2003; 51(2):162-70. · 1.59 Impact Factor -
Article: Synthesis and pharmacological activities of 2-(3'-substituted-2'-hydroxypropylamino)pyridines.
Joseph Thomas Leonard, Navaneetharaman Anbalagan, Shanmugam Sadish Kumar, Sundararaj Kishore Gnanasam, Seshaiah Krishnan Sridhar[show abstract] [hide abstract]
ABSTRACT: In the present study, a series of 2-(3'-substituted-2'-hydroxypropylamino)pyridines were synthesized and characterized by IR, 1H-NMR and elemental analysis. The compounds were investigated for anticonvulsant (150, 300 mg/kg) and cardiac activity. 2-(3'-Diethylamino-2'-hydroxypropylamino)pyridine 3 was found to exhibit the highest anticonvulsant activity. 2-(3'-Dimethylamino-2'-hydroxypropylamino)pyridine 2 and 2-[3'-(4''-nitrophenylamino)-2'-hydroxypropylamino]pyridine 6 were found to exhibit negative ionotropic activity. 2-(3'-Dimethylamino-2'-hydroxypropylamino)pyridine 2, 2-[3'-(4''-nitrophenylamino)-2'-hydroxypropylamino]pyridine 6 and 2-(3'-piperidino-2'-hydroxypropylamino)pyridine 8 were found to antagonize exhibit beta-adrenergic activity.Biological & Pharmaceutical Bulletin 03/2002; 25(2):215-7. · 1.66 Impact Factor