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Synthesis of thioether derivatives of quinazoline-4-one-2-thione and evaluation of their antiplatelet aggregation activity

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Abstract

A series of 2-(arylmethylthio)-3-phenylquinazolin-4-one derivatives have been synthesized and their antiplatelet aggregation activities were assessed against ADP and arachidonic acid-induced platelet aggregation in human plasma. Among the tested thioethers, derivative 2, 3, 5 and 16 were the most potent compounds with satisfactory IC50 for inhibition of platelet aggregation induced by ADP. Analysis of global physicochemical parameters shows some correlations between activities and molecular volume and also surface area of the studied derivatives.

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Authors and Affiliations

  1. Department of Medicinal Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Vali Asr Avenue, Niayesh Junction, P.O. Box 14155-6153, Tehran, Iran

    Zahra Eskandariyan, Marjan Esfahani Zadeh, Kamaleddin Haj Mohammad Ebrahim Tehrani, Vida Mashayekhi & Farzad Kobarfard

  2. Phytochemistry Research Center, Shahid Beheshti University of Medical Sciences, Vali Asr Avenue, Niayesh Junction, P.O. Box 14155-6153, Tehran, Iran

    Farzad Kobarfard

Authors
  1. Zahra Eskandariyan
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  2. Marjan Esfahani Zadeh
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  3. Kamaleddin Haj Mohammad Ebrahim Tehrani
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  4. Vida Mashayekhi
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  5. Farzad Kobarfard
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Correspondence to Farzad Kobarfard.

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Eskandariyan, Z., Esfahani Zadeh, M., Haj Mohammad Ebrahim Tehrani, K. et al. Synthesis of thioether derivatives of quinazoline-4-one-2-thione and evaluation of their antiplatelet aggregation activity. Arch. Pharm. Res. 37, 332–339 (2014). https://doi.org/10.1007/s12272-013-0192-5

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  • DOI: https://doi.org/10.1007/s12272-013-0192-5

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