Journal Title
Title of Journal: Med Chem Res
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Abbravation: Medicinal Chemistry Research
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Authors: Pran Kishore Deb Rajwinder Kaur Balakumar Chandrasekaran Madhu Bala Dilshad Gill Venkat Rao Kaki Raghuram Rao Akkinepalli Raghuprasad Mailavaram
Publish Date: 2013/11/09
Volume: 23, Issue: 6, Pages: 2780-2792
Abstract
A series of new 2substitutedN13thiazole2ylacetamide 3–7 and Nbenzodthiazol2yl2substitutedacetamide 10–13 derivatives have been synthesized and evaluated in vivo rat paw edema for their antiinflammatory activities and in silicodocking studies to recognize the hypothetical binding motif of the title compounds with the cyclooxygenase isoenzyme COX2 employing GLIDE software Schrodinger Inc The compounds 10–13 were found to have good antiinflammatory activities around 84–93 of the standard indomethacin The binding mode of the title compounds has been proposed based on the docking studies Further the predicted ADME properties of all the tested compounds were found to be in the ranges as predicted by QikProp for 95 of known oral drugs and also satisfy the Lipinski’s rule of fiveThe author PKD is thankful to CSIR New Delhi for awarding the Senior Research Fellowship Sanction No 09/135/0534/2008/EMRI 18/03/2008 The authors thankfully acknowledge the Chairman UIPS Chandigarh for providing the facilities Authors are also thankful to Dr Kanwaljit Chopra Pharmacology Division and Dr Maninder Karan Vasisht Pharmacognosy Division UIPS PU for valuable help during pharmacological studies Authors profusely thank to Avtar Singh SAIF CIL PU for carrying out the NMR studies Author PKD is thankful to Pharmaceutical Chemistry Division School of Pharmacy IMU Malaysia for providing the facilities to carry out the docking studies Authors are also thankful to Mr Raghurangaswamy Executive Director Schrodinger India for providing the evaluation license 14 Jun–16 July 2013 to carry out the molecular modeling studies
Keywords:
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