Synthesis and Biological Potential Assessment of 2-Substituted Quinazolin-4(3H)-ones as Inhibitors of Phosphodiesterase-I and Carbonic Anhydrase-II

Author(s): Syed Muhammad Saad, Muhammad Saleem, Shahnaz Perveen, Muhammad Tanveer Alam, Khalid Mohammed Khan, Muhammad Iqbal Choudhary

Journal Name: Medicinal Chemistry

Volume 11 , Issue 4 , 2015


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Abstract:

A library of twenty-five derivatives of 2-substituted quinazolin-4(3H)-ones 1-25 was synthesized and evaluated against phosphodiesterase-I (PDE) and carbonic anhydrase-II (CA). Compounds 17 (IC50 = 210.7 ± 2.62 µM), 16 (IC50 = 301.6 ± 1.18 µM), and 13 (IC50 = 458.13 ± 3.60 µM), selectively exhibited PDE inhibition while compounds 22 (IC50 = 61.33 ± 2.38 µM), 1 (IC50 = 108.30 ± 0.93 µM), and 21 (IC50 = 191.93 ± 2.72 µM), discriminatingly exhibited CA inhibition as compared to standards EDTA (IC50 = 277.69 ± 2.52 µM) and acetazolamide (IC50 = 0.12 ± 0.03µM), for PDE and CA inhibitions, respectively. However, compound 15 was found to be active against both enzymes with the IC50 values 344.33 ± 4.32 µM and 20.94 ± 0.58 µM, for PDE and CA inhibitions, respectively. Remaining compounds were found to be inactive against both the enzymes. Structure-activity relationship studies are discussed herein.

Keywords: 2-Substituted quinazolin-4(3H)-ones, NPP1/Phosphodiesterase-I, Carbonic Anhydrase-II, Structure-Activity Relationship.

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Article Details

VOLUME: 11
ISSUE: 4
Year: 2015
Published on: 03 December, 2014
Page: [336 - 341]
Pages: 6
DOI: 10.2174/1573406410666141203123926
Price: $65

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