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Synthesis of 2-substituted-4-aryl-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents with cardioprotective and ulcerogenic sparing effects

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Abstract

Several new 2-substituted-4-aryl-6-phenylpyridazin-3(2H)-ones were synthesized and evaluated for in vivo anti-inflammatory and analgesic activities and possible in vitro COX-2 selectivity. To critically evaluate the possibility of deleterious effects of newly synthesized agents on normal hemostasis, anti-platelet activity and whole blood clotting time were also assessed. The structures of the synthesized compounds were confirmed on the basis of spectral data and elemental analysis. The present study has led to the identification of 4-(4-methoxyphenyl)-2-(2-(4-phenylpiperazin-1-yl)-2-oxoethyl)-6-phenylpyridazin-3(2H)-one (17) as an ideal anti-inflammatory agent with good affinity and remarkable selectivity for COX-2 enzyme without any ulcerogenic and cardiovascular side effects. In addition, at lower doses all the pyridazinone derivatives do not seem to affect normal hemostatic balance.

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Acknowledgments

The authors are thankful to University Grants Commission, India, and Council of Scientific and Industrial Research, India, for providing financial support.

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  1. University Institute of Pharmaceutical Sciences, Sector-14, Panjab University, Chandigarh, 160014, India

    Deepika Sharma & Ranju Bansal

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  1. Deepika Sharma
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  2. Ranju Bansal
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Correspondence to Ranju Bansal.

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Sharma, D., Bansal, R. Synthesis of 2-substituted-4-aryl-6-phenylpyridazin-3(2H)-ones as potential anti-inflammatory and analgesic agents with cardioprotective and ulcerogenic sparing effects. Med Chem Res 25, 1574–1589 (2016). https://doi.org/10.1007/s00044-016-1588-9

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