Jitendra Maganbhai Gajera
Sardar Patel University
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Publication
Featured researches published by Jitendra Maganbhai Gajera.
Bioorganic & Medicinal Chemistry Letters | 2017
Nagarajan Muthukaman; Macchindra Tambe; Mahamadhanif S. Shaikh; Dnyandeo Pisal; Sanjay Deshmukh; Shital Tondlekar; Neelam Sarode; Lakshminarayana Narayana; Jitendra Maganbhai Gajera; Vidya Ganapati Kattige; Srinivasa Honnegowda; Vikas Karande; Abhay Kulkarni; Dayanidhi Behera; Satyawan Jadhav; Girish S. Gudi; Neelima Khairatkar-Joshi; Laxmikant Atmaram Gharat
A series of substituted tricyclic 4,4-dimethyl-3,4-dihydrochromeno[3,4-d]imidazole derivatives have been synthesized and their mPGES-1 biological activity has been disclosed in detail. Structure-activity relationship (SAR) optimization provided inhibitors with excellent mPGES-1 potency and low to moderate PGE2 release A549 cell potency. Among the mPGES-1 inhibitors studied, 7, 9 and 11l provided excellent selectivity over COX-2 (>200-fold) and >70-fold selectivity for COX-1 except 11l, which exhibited dual mPGES-1/COX-1 activity. Furthermore, the above tested mPGES-1 inhibitors demonstrated good metabolic stability in liver microsomes, high plasma protein binding (PPB) and no significant inhibition observed in clinically relevant CYP isoforms. Besides, selected mPGES-1 tool compounds 9 and 11l provided good in vivo pharmacokinetic profile and oral bioavailability (%F=33 and 85). Additionally, the representative mPGES-1 tool compounds 9 and 11l revealed moderate in vivo efficacy in the LPS-induced thermal hyperalgesia guinea pig pain model.
Organic Chemistry International | 2008
Jitendra Maganbhai Gajera; Shital Tondlekar; Laxmikant Atmaram Gharat
We have developed a novel and one-pot synthesis of 6-arylpyrimidine-4-ol by reacting commercially available alkyl 3-oxo-3-arylpropanoate with formamide in the presence of stoichiometric amount of ammonium acetate.
Journal of Heterocyclic Chemistry | 2006
D. I. Brahmbhatt; Jitendra Maganbhai Gajera; Chirag Patel; Vishwesh P. Pandya; Urvish R. Pandya
Archive | 2007
Laxmikant Atmaram Gharat; Jitendra Maganbhai Gajera; Aniket Vijaykumar Farande; Suresh Mahadev Kadam; Kasturaiah Chapala; Shailendra Nilkanth Bhadane
Archive | 2007
Laxmikant Atmaram Gharat; Jitendra Maganbhai Gajera; Mangesh Jagannath Pawar
Journal of Heterocyclic Chemistry | 2008
Jitendra Maganbhai Gajera; Balasubramanian Gopalan; Pravin Sabhajit Yadav; Sandip Damodar Patil; Laxmikant Atmaram Gharat
Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry | 2007
D. I. Brahmbhatt; Jitendra Maganbhai Gajera; V. P. Pandya; M. A. Patel
Archive | 2007
Laxmikant Atmaram Gharat; Neelima Khairatkar Joshi; Jitendra Maganbhai Gajera; Pravin Sabhajit Yadav
Archive | 2011
Laxmikant Atmaram Gharat; Jitendra Maganbhai Gajera; Neelima Khairatkar-Joshi; Malini Bajpai
Archive | 2008
Laxmikant Atmaram Gharat; Jitendra Maganbhai Gajera; Neelima Khairatkar-Joshi; Vidya G. Kattigf