CNS depressant and anticonvulsant activities of some novel 3-[5-substituted 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones

作者: Varsha Jatav , Pradeep Mishra , Sushil Kashaw , JP Stables , None

DOI: 10.1016/J.EJMECH.2007.12.003

关键词:

摘要: Abstract A series of new 3-[5-substituted phenyl-1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3 H )-ones were synthesized and evaluated for anticonvulsant, sedative–hypnotic CNS depression activities. After i.p. injection to mice or rat at doses 30, 100, 300 mg/kg body weight 2-styryl quinazolin-4(3 derivatives examined in the maximal electroshock (MES) induced seizures subcutaneous pentylenetetrazole (scPTZ) seizure models mice. Rotorod method was employed determine neurotoxicity. Out 18 compounds only 4a , 4e 4p showed anticonvulsant activity one more test models. All except 4l 4q exhibited significant via actophotometer screen. Forced swim pool depressant resulted some potent compounds. It can be concluded that better activities than activity.

参考文章(10)
Roger D. Porsolt, Guy Anton, Nadine Blavet, Maurice Jalfre, Behavioural despair in rats: a new model sensitive to antidepressant treatments. European Journal of Pharmacology. ,vol. 47, pp. 379- 391 ,(1978) , 10.1016/0014-2999(78)90118-8
Jonathan R. Dimmock, Ramanan N. Puthucode, Jennifer M. Smith, Mark Hetherington, J. Wilson Quail, Uma Pugazhenthi, Terry Lechler, James P. Stables, (Aryloxy)aryl Semicarbazones and Related Compounds: A Novel Class of Anticonvulsant Agents Possessing High Activity in the Maximal Electroshock Screen Journal of Medicinal Chemistry. ,vol. 39, pp. 3984- 3997 ,(1996) , 10.1021/JM9603025
Melvin J. Yu, Jefferson R. McCowan, Norman R. Mason, Jack B. Deeter, Laurane G. Mendelsohn, Synthesis and X-ray crystallographic analysis of quinazolinone cholecystokinin/gastrin receptor ligands. Journal of Medicinal Chemistry. ,vol. 35, pp. 2534- 2542 ,(1992) , 10.1021/JM00092A003
M. J. Kornet, T. Varia, W. Beaven, Synthesis and anticonvulsant activity of 3‐amino‐4(3H)‐quinazolinones Journal of Heterocyclic Chemistry. ,vol. 20, pp. 1553- 1555 ,(1983) , 10.1002/JHET.5570200623
Patrick T. Flaherty, Thomas D. Greenwood, Amy L. Manheim, James F. Wolfe, Synthesis and evaluation of N-(phenylacetyl)trifluoromethanesulfonamides as anticonvulsant agents. Journal of Medicinal Chemistry. ,vol. 39, pp. 1509- 1513 ,(1996) , 10.1021/JM950761Q
James F. Wolfe, Terry L. Rathman, Mark C. Sleevi, James A. Campbell, Thomas D. Greenwood, Synthesis and anticonvulsant activity of some new 2-substituted 3-aryl-4(3H)-quinazolinones Journal of Medicinal Chemistry. ,vol. 33, pp. 161- 166 ,(1990) , 10.1021/JM00163A027
Yasuhisa Kurogi, Yasuhide Inoue, Kazuhiko Tsutsumi, Shizuo Nakamura, Kazushi Nagao, Hiroki Yoshitsugu, Yoshihiko Tsuda, Synthesis and hypolipidemic activities of novel 2-[4-[diethoxyphosphoryl)methyl]phenyl]quinazolines and 4(3H)-quinazolinones. Journal of Medicinal Chemistry. ,vol. 39, pp. 1433- 1437 ,(1996) , 10.1021/JM9506938
R. L. Krall, J. K. Penry, B. G. White, H. J. Kupferberg, E. A. Swinyard, Antiepileptic drug development: II. Anticonvulsant drug screening. Epilepsia. ,vol. 19, pp. 409- 428 ,(1978) , 10.1111/J.1528-1157.1978.TB04507.X
Ludmila Fišnerová, Bohumila Brunová, Zuzana Kocfeldová, Jana Tíkalová, Eva Maturová, Jaroslava Grimová, Synthesis and analgetic efficiency of some oxy and oxo derivatives of 4(3H)-quinazolinone Collection of Czechoslovak Chemical Communications. ,vol. 56, pp. 2373- 2381 ,(1991) , 10.1135/CCCC19912373
Varsha Jatav, Pradeep Mishra, S. K. Kashaw, Some novel 2-methyl-3-(1'3'4'-thiadiazoyl)-4-(3H)quinazolinones with anticonvulsant and CNS depressant activity Journal of the Indian Chemical Society. ,vol. 83, pp. 1165- 1170 ,(2006)