synthesis and anticonvulsant activity of some quinazolin-4-(3h)-one derivatives合成和抗惊厥的活动的一些quinazolin-4u2014u2014(3 h)u2014u2014衍生品.pdfVIP

Molecules 2008, 13, 2557-2569; DOI: 10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /molecules Article Synthesis and Anticonvulsant Activity of Some Quinazolin-4- (3H)-one Derivatives Hanan Georgey *, Nagwa Abdel-Gawad and Safinaz Abbas Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Eini Street, Cairo 11562, Egypt; E-mails: hamadido21@ (N. A-G.), safi_esab@ (S. A.) Tel.: 002-02 Fax: 002-02 * Author to whom correspondence should be addressed; E-mail: hanan-hanna@; Tel.:002-02 002-017-5600699. Received: 4 September 2008; in revised form: 18 September 2008 / Accepted: 15 October 2008 / Published: 16 October 2008 Abstract: A number of 3-substituted-2-(substituted-phenoxymethyl) quinazolin-4(3H)-one derivatives have been synthesized. Their structures have been elucidated on the basis of elemental analyses and spectroscopic studies (IR, 1H-NMR, MS). A preliminary evaluation of the anticonvulsant properties of the prepared compounds has indicated that some of them exhibit moderate to significant activity, compared to a diazepam standard. Keywords: Quinazolin-4-(3H)-ones; piperazines; chloroacetamide; anticonvulsant activity Introduction The quinazolin-4-(3H)-one ring system is considered an interesting moiety due to its wide ranging biological properties, which include antitumor [1-3], anti-HIV [4], selective estrogen beta modulator [5], anti-inflammatory [6-8], antibacterial [9-12], antidepressant [13] and CNS depressant activit