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Sci. Pharm. 2008, 76(3), 415-438; doi:10.3797/scipharm.0804-20 (registering DOI)

Synthesis, Pharmacophore Modeling, and Biological Evaluation of Novel 5H-Thiazolo[3,2-a]pyrimidin-5-one Derivatives as 5-HT2A Receptor Antagonists

Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Eini street 11562 Cairo, Egypt
Received: 19 April 2008 / Accepted: 5 August 2008 / Published: 9 August 2008
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Abstract

Novel 5H-thiazolo[3,2-a]pyrimidin-5-one derivatives linked through an ethylene bridge to various phenylpiperazine groups were prepared for evaluation as 5-HT2A receptor antagonists. The target compounds 11a–p were prepared through the initial synthesis of the 2-chloroethyl intermediates 10a–d which were then reacted with the appropriate phenylpiperazines. All compounds were tested for their antagonistic activity on 5-HT2Areceptors using inhibition of 5-hydroxytryptophan(5-HTP)-induced head twitches in mice. Pharmacophore modeling study, based on a hypothetical pharmacophore template generated from a set of diverse known active ligands, revealed good fitting of the designed compounds to the generated hypothetical pharmacophore.
Keywords: Arylpiperazines; 5-HT2A antagonists; Thiazolo[3,2-a]pyrimidines; Inhibition of 5-HTP induced head twitches Arylpiperazines; 5-HT2A antagonists; Thiazolo[3,2-a]pyrimidines; Inhibition of 5-HTP induced head twitches
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

AWADALLAH, F.M. Synthesis, Pharmacophore Modeling, and Biological Evaluation of Novel 5H-Thiazolo[3,2-a]pyrimidin-5-one Derivatives as 5-HT2A Receptor Antagonists. Sci. Pharm. 2008, 76, 415-438.

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