Journal Title
Title of Journal: Med Chem Res
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Abbravation: Medicinal Chemistry Research
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Authors: Satheesh Krishna Balam Suresh Kumar Krishnammagari Jayaprakash Soora Harinath Siva Prasad Sthanikam Syama Sundar Chereddy Visweswara Rao Pasupuleti Nanda Kumar Yellapu Vasu Govardhana Reddy Peddiahgari Suresh Reddy Cirandur
Publish Date: 2014/08/06
Volume: 24, Issue: 3, Pages: 1119-1135
Abstract
Inhibition of 11βHSD1 enzymatic action is perceived as a potential target for the treatment of metabolic syndromes like cardiovascular diseases obesity and diabetes In an attempt to formulate potential organophosphorus compounds against 11βHSD1 enzyme inhibition we report novel 6bromo36methyl2pyridyl2alkyl/arylamino34dihydro2H132λ5benzoxazaphosphinin2ones 22a–22n as good in vitro inhibitors of HEK 293 cell lines The in vivo acute and subacute investigations sustain them as good antidiabetic compounds The computational docking studies performed on them also supported the binding mode of compounds 22a and 22h with 11βHSD1 protein The blood glucose level lowering effect of the target compounds 22a–22n screened on the streptozotocininduced diabetic rats revealed that the target compounds are potential by antidiabetic when compared to the potency of standard glibenclamide drug In addition the calculated QSAR parameters predicted ADMET properties evaluated bioactivity properties and toxicity risk studies authorize drug like properties to the synthesized compoundsWe thank University Grants Commission UGC New Delhi INDIA for providing financial support through UGCBSRRFSMS Research Fellowship In Sciences For Meritorious Students Fellowship F41/2011 BSRRFSMSBSK and for providing financial assistance through the Major Research Project F No 42281/2013 SR Dated 12032013 We also thank Dr V Koteswara Rao Post doctoral Fellow Kansas University Kansas USA for providing MOE software for QSAR and Molecular docking studies
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