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Volume 76
Issue 3
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Article

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

by
Fadi M. AWADALLAH
Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Eini street 11562 Cairo, Egypt
Sci. Pharm. 2008, 76(3), 415-438; https://doi.org/10.3797/scipharm.0804-20
Submission received: 19 April 2008 / Accepted: 5 August 2008 / Published: 9 August 2008
Versions Notes

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

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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. https://doi.org/10.3797/scipharm.0804-20

AMA Style

AWADALLAH FM. Synthesis, Pharmacophore Modeling, and Biological Evaluation of Novel 5H-Thiazolo[3,2-a]pyrimidin-5-one Derivatives as 5-HT2A Receptor Antagonists. Scientia Pharmaceutica. 2008; 76(3):415-438. https://doi.org/10.3797/scipharm.0804-20

Chicago/Turabian Style

AWADALLAH, Fadi M. 2008. "Synthesis, Pharmacophore Modeling, and Biological Evaluation of Novel 5H-Thiazolo[3,2-a]pyrimidin-5-one Derivatives as 5-HT2A Receptor Antagonists" Scientia Pharmaceutica 76, no. 3: 415-438. https://doi.org/10.3797/scipharm.0804-20

APA Style

AWADALLAH, F. M. (2008). Synthesis, Pharmacophore Modeling, and Biological Evaluation of Novel 5H-Thiazolo[3,2-a]pyrimidin-5-one Derivatives as 5-HT2A Receptor Antagonists. Scientia Pharmaceutica, 76(3), 415-438. https://doi.org/10.3797/scipharm.0804-20

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