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CLC number: R914.5; TQ460.7+2

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Journal of Zhejiang University SCIENCE B 2007 Vol.8 No.7 P.526~532

http://doi.org/10.1631/jzus.2007.B0526


Synthesis and anticonvulsant activity of some potent 5,6-bis aryl 1,2,4-triazines


Author(s):  MALLIKARJUNA B.P., SURESH KUMAR G.V., SASTRY B.S., NAGARAJ, MANOHARA K.P.

Affiliation(s):  Department of Medicinal Chemistry, St. Johns Pharmacy College, Bangalore-560040, Karnataka, India; more

Corresponding email(s):   gvsureshkumar@yahoo.com

Key Words:  5, 6-Bis aryl 1, 2, 4-triazines, Synthesis, Anticonvulsant activity


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MALLIKARJUNA B.P., SURESH KUMAR G.V., SASTRY B.S., NAGARAJ, MANOHARA K.P.. Synthesis and anticonvulsant activity of some potent 5,6-bis aryl 1,2,4-triazines[J]. Journal of Zhejiang University Science B, 2007, 8(7): 526~532.

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author="MALLIKARJUNA B.P., SURESH KUMAR G.V., SASTRY B.S., NAGARAJ, MANOHARA K.P.",
journal="Journal of Zhejiang University Science B",
volume="8",
number="7",
pages="526~532",
year="2007",
publisher="Zhejiang University Press & Springer",
doi="10.1631/jzus.2007.B0526"
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%T Synthesis and anticonvulsant activity of some potent 5,6-bis aryl 1,2,4-triazines
%A MALLIKARJUNA B.P.
%A SURESH KUMAR G.V.
%A SASTRY B.S.
%A NAGARAJ
%A MANOHARA K.P.
%J Journal of Zhejiang University SCIENCE B
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%P 526~532
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%D 2007
%I Zhejiang University Press & Springer
%DOI 10.1631/jzus.2007.B0526

TY - JOUR
T1 - Synthesis and anticonvulsant activity of some potent 5,6-bis aryl 1,2,4-triazines
A1 - MALLIKARJUNA B.P.
A1 - SURESH KUMAR G.V.
A1 - SASTRY B.S.
A1 - NAGARAJ
A1 - MANOHARA K.P.
J0 - Journal of Zhejiang University Science B
VL - 8
IS - 7
SP - 526
EP - 532
%@ 1673-1581
Y1 - 2007
PB - Zhejiang University Press & Springer
ER -
DOI - 10.1631/jzus.2007.B0526


Abstract: 
In the present research, a series of 285%29&ck%5B%5D=abstract&ck%5B%5D=keyword'>2f4a8b>5,286-Bis aryl 1%29&ck%5B%5D=abstract&ck%5B%5D=keyword'>2f4a8b>6-Bis aryl 1,2,4-triazines 285%29&ck%5B%5D=abstract&ck%5B%5D=keyword'>2f4a8b>5a~285%29&ck%5B%5D=abstract&ck%5B%5D=keyword'>2f4a8b>5f were synthesized by condensation of various benzils 4a~4f with aminoguanidine bicarbonate and were screened in vivo, for their anticonvulsant and neurotoxicity studies. Compounds 285%29&ck%5B%5D=abstract&ck%5B%5D=keyword'>2f4a8b>5a, 285%29&ck%5B%5D=abstract&ck%5B%5D=keyword'>2f4a8b>5b and 285%29&ck%5B%5D=abstract&ck%5B%5D=keyword'>2f4a8b>5d were found to be potent molecules of this series, when compared with the reference drugs phenytoin sodium, diazepam and lamotrigine. The structures of these compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopic data.

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Reference

[1] Chang, B.S., Lowenstein, D.H., 2003. Mechanisms of disease: epilepsy. N. Eng. J. Med., 349(13):1257-1262.

[2] Danny, D.S., René, H.L., Jill, L.S., Alan, V., 1992. Comparative anticonvulsant potency and pharmacokinetics of (+)- and (−)-enantiomers of stiripentol. Epilepsy Res., 1(11):29-36.

[3] Dimmock, J.R., Sidhu, K.K., Tumber, D.F., 1995a. Some aryl semicarbazones possessing anticonvulsant activitie. Eur. J. Med. Chem., 30(4):287-301.

[4] Dimmock, J.R., Vashishtha, S.C., Stables, J.P., 1995b. Evaluation of the semicarbazones, thiosemicarbazones and bis-carbohydrazones of some aryl alicycylic ketones for anticonvulsant and other biological propertie. Eur. J. Med. Chem., 30(4):303-314.

[5] Duncan, J.S., 2002. The promise of new antiepileptic drugs. Br. J. Clin. Pharmacol., 53(2):123-131.

[6] Erickson, J.G., 1952. 3-Amino-as-triazines. J. Am. Chem. Soc., 74(18):4706.

[7] Fisher, R.S., 1989. Animal models of the epilepsies. Brain Research Reviews, 14(3):245-278.

[8] Grundmann, C., Kreutzberger, A., 1954. 1,3,5-Triazine. J. Am. Chem. Soc., 76(2):632-633.

[9] Hosford, D.A., Wang, Y., 1997. Utility of the lethargic (lh/lh) mouse model of absence seizures in predicting the effects of lamotrigine, vigabatrin, tiagabine, gabapentin, and topiramate against human absence seizures. Epilepsia, 38(4):408-414.

[10] Kubicki, M., Codding, P.W., 2001. Hydrogen bonding patterns in 3,5-diamino-6-aryl triazines. Journal of Molecular Structure, 570(1-3):53-60.

[11] McNamara, J.O., 2001. Drugs Effective in the Therapy of the Epliepsies. In: Hardman, L.G., Limbird, L.E. (Eds.), Goodman and Gilman’s the Pharmacological Basis of Therapeutics. McGraw Hill, New York, p.521-547.

[12] Pandeya, S.N., Yogeswari, P., Stables, J.P., 2000. Synthesis and anticonvulsant activity of 4-bromophenyl substituted aryl semicarbazones. Eur. J. Med. Chem., 35(10):879-886.

[13] Pastalos, P.N., 1999. Synthesis of some oxime ether derivatives of 1-(2-naphthyl)-2-(1,2,4-triazol-1-yl)ethanone and their anticonvulsant and antimicrobial activities. Curr. Opin. CPNS Invest. Drugs, 1(64):549-555.

[14] Petroff, O.A., Rothman, D.L., Behar, K.L., Mattson, R.H., 1995. Initial observations on effect of vigabatrin on in vivo 1H spectroscopic measurements of γ-aminobutyric acid, glutamate, and glutamine in human brain. Epilepsia, 36(5):457-464.

[15] Porsolt, R.D., Anton, G., Blavet, N., Jalfre, M., 1978. Behavioural despair in rats: a new model sensitive to antidepressant treatments. Eur. J. Pharmacol., 47(4):379-391.

[16] Richard, W.A., Peter, B.R., Theodre, J.F., 1972. Antimalarial activities of some 3,5-diamino-as-triazine derivatives. J. Med. Chem., 15(4):859-871.

[17] Sander, J.W.A.S., 1993. Some aspects of prognosis in the epilepsies: a review. Epilepsia, 34(6):1007-1016.

[18] Sawyer, D.A., Copp, F.C., 1992. Synthesis of novel triazoles as potent anticonvulsants. Chem. Abstr., 108:1125.

[19] Smith, Q.E., 1960. Pharmacological Screening Tests Progress in Medicinal Chemistry. 1: Butterworths. London, p.1-33.

[20] Stephani, U., 1989. The natural history of myoclonic astatic epilepsy the natural history of myoclonic astatic epilepsy. Epilepsia, 47(Suppl. 1):S53-S55.

[21] Taylor, C.P., 1996. Voltage-gated Na+ channels as targets for anticonvulsant, analgesic and neuroprotective drugs. Curr. Pharm. Des., 2(4):375-379.

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