Mukul R Jain

Summary

Affiliation: Zydus Research Centre
Country: India

Publications

  1. ncbi request reprint Design, synthesis, and biological evaluation of substituted-N-(thieno[2,3-b]pyridin-3-yl)-guanidines, N-(1H-pyrrolo[2,3-b]pyridin-3-yl)-guanidines, and N-(1H-indol-3-yl)-guanidines
    Rajesh H Bahekar
    Zydus Research Centre, Cadila Healthcare Ltd, Sarkhej Bavala N H 8A, Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem 15:3248-65. 2007
  2. ncbi request reprint In vitro PAI-1 inhibitory activity of oxalamide derivatives
    Mukul R Jain
    Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382210, Gujarat, India
    Eur J Med Chem 43:880-4. 2008
  3. ncbi request reprint Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands
    Saurin Raval
    Zydus Research Centre, Medicinal Chemistry, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad, Gujarat 382210, India
    Bioorg Med Chem Lett 18:3919-24. 2008
  4. ncbi request reprint Subtherapeutic dose of pioglitazone reduces expression of inflammatory adipokines in db/db mice
    Jogeswar Mohapatra
    Zydus Research Centre, Ahmedabad, India
    Pharmacology 84:203-10. 2009
  5. pmc Retinol-binding protein 4 : a possible role in cardiovascular complications
    Jogeswar Mohapatra
    Zydus Research Centre, Sarkhej Bavla Highway No 8A, Moraiya, Ahmedabad, Gujarat, India
    Br J Pharmacol 164:1939-48. 2011
  6. ncbi request reprint Involvement of adipokines in rimonabant-mediated insulin sensitivity in ob/ob mice
    Jogeswar Mohapatra
    Zydus Research Centre, Moraiya, Ahmedabad, Gujarat, India
    J Pharm Pharmacol 61:1493-8. 2009
  7. ncbi request reprint Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a CB1 receptor antagonist with in vivo antiobesity effect
    Brijesh Kumar Srivastava
    Department of Medicinal Chemistry, Zydus Research Centre, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382 210, India
    Bioorg Med Chem Lett 19:2546-50. 2009
  8. ncbi request reprint Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist
    Brijesh Kumar Srivastava
    Department of Medicinal Chemistry, Zydus Research Centre, Cadila Healthcare Ltd, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem Lett 18:3882-6. 2008
  9. ncbi request reprint Involvement of TACE in colon inflammation: a novel mechanism of regulation via SIRT-1 activation
    Manoranjan Sharma
    Dept of Pharmacology, Zydus Research Centre, Moraiya, Ahmedabad, Gujarat, India
    Cytokine 66:30-9. 2014
  10. ncbi request reprint Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents
    Kiran Shah
    Zydus Research Centre, Sarkhej Bavla N H 8A Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem Lett 22:5857-62. 2012

Collaborators

  • Brijesh Kumar Srivastava
  • Sunil Gupta
  • Abhijit Chatterjee
  • Saurin Raval
  • R Balaraman
  • Vishal Patel
  • Rajendra H Jani
  • Shvetank Bhatt
  • Shefalee K Bhavsar
  • Rajesh H Bahekar
  • Manoranjan Sharma
  • Jogeswar Mohapatra
  • Rakesh B Patel
  • Pankaj R Patel
  • Hiren M Patel
  • Shrikalp S Deshpande
  • Kartikkumar Navinchandra Patel
  • Dheerendra Pandey
  • Akshaya Wagh
  • Bhavin M Sonara
  • Kanaiyalal D Prajapati
  • Gourang B Shah
  • Shekhar Kadam
  • Vishwanath D Pawar
  • Kiran Shah
  • Aviseka Acharya
  • Vinay Mishra
  • Prabodha Swain
  • Kalapatapu V V M Sairam
  • Gaurav Pandya
  • Satinder Singh
  • Brijesh Kumar Srivastava
  • Hitesh Soni
  • Samadhan Govind Kshirsagar
  • Anil Argade
  • Amit Arvind Joharapurkar
  • Manoranjan M Sharma
  • Gaurang B Shah
  • Umar Malik
  • Anuj Singh
  • Pradip Jadav
  • Dipam Patel
  • Mubeen Sheikh
  • Amit Joharapurkar
  • Shilpesh Devada
  • Ramchandra Ranvir
  • Priya Ghumatkar
  • Maulik V Patel
  • Rajesh Sundar
  • Nisha Sadhwani
  • Neha Gandhi
  • Ajay Sharma
  • Satadru Jha
  • Jayendra Z Patel
  • Vishwanath Pawar
  • Rina Soni
  • Sandeep A Shedage
  • Prasenjit Mitra

Detail Information

Publications27

  1. ncbi request reprint Design, synthesis, and biological evaluation of substituted-N-(thieno[2,3-b]pyridin-3-yl)-guanidines, N-(1H-pyrrolo[2,3-b]pyridin-3-yl)-guanidines, and N-(1H-indol-3-yl)-guanidines
    Rajesh H Bahekar
    Zydus Research Centre, Cadila Healthcare Ltd, Sarkhej Bavala N H 8A, Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem 15:3248-65. 2007
    ..7mmol). Some of the test compounds (2c, 3c, and 4c) from each series were found to be equipotent to BL 11282 (standard aryl-imidazoline), which indicated that the guanidine group acts as a bioisostere of imidazoline ring system...
  2. ncbi request reprint In vitro PAI-1 inhibitory activity of oxalamide derivatives
    Mukul R Jain
    Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382210, Gujarat, India
    Eur J Med Chem 43:880-4. 2008
    ..In vitro PAI-1 inhibitory activities of oxalamide derivatives are evaluated by chromogenic assay. Few compounds have shown significant PAI-1 inhibitory activity...
  3. ncbi request reprint Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands
    Saurin Raval
    Zydus Research Centre, Medicinal Chemistry, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad, Gujarat 382210, India
    Bioorg Med Chem Lett 18:3919-24. 2008
    ..The 3-[3,5-dichloro-4-(4-hydroxy-3-isopropylphenoxy)-phenylamino]-4-hydroxy-cyclobut-3-ene-1,2-dione 21 has shown selectivity towards thyroid hormone receptor beta...
  4. ncbi request reprint Subtherapeutic dose of pioglitazone reduces expression of inflammatory adipokines in db/db mice
    Jogeswar Mohapatra
    Zydus Research Centre, Ahmedabad, India
    Pharmacology 84:203-10. 2009
    ..Anti-inflammatory effects of pioglitazone may precede its insulin-sensitizing effects in db/db mice...
  5. pmc Retinol-binding protein 4 : a possible role in cardiovascular complications
    Jogeswar Mohapatra
    Zydus Research Centre, Sarkhej Bavla Highway No 8A, Moraiya, Ahmedabad, Gujarat, India
    Br J Pharmacol 164:1939-48. 2011
    ..To understand the correlation, rimonabant, an anti-obesity drug, has been used to relieve the atherosclerotic predisposition...
  6. ncbi request reprint Involvement of adipokines in rimonabant-mediated insulin sensitivity in ob/ob mice
    Jogeswar Mohapatra
    Zydus Research Centre, Moraiya, Ahmedabad, Gujarat, India
    J Pharm Pharmacol 61:1493-8. 2009
    ..However, the precise role of adipokines in the insulin-sensitising effects of the CB1 antagonist rimonabant is not clear...
  7. ncbi request reprint Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a CB1 receptor antagonist with in vivo antiobesity effect
    Brijesh Kumar Srivastava
    Department of Medicinal Chemistry, Zydus Research Centre, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382 210, India
    Bioorg Med Chem Lett 19:2546-50. 2009
    ..Compound 3 has been identified as a hair growth stimulator and an antiobesity agent in animal models...
  8. ncbi request reprint Facile synthesis, ex-vivo and in vitro screening of 3-sulfonamide derivative of 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxylic acid piperidin-1-ylamide (SR141716) a potent CB1 receptor antagonist
    Brijesh Kumar Srivastava
    Department of Medicinal Chemistry, Zydus Research Centre, Cadila Healthcare Ltd, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem Lett 18:3882-6. 2008
    ..Primary ex-vivo pharmacological testing and in vitro screening of sulfonamide derivative 2 showed the loss of CB1 receptor antagonism...
  9. ncbi request reprint Involvement of TACE in colon inflammation: a novel mechanism of regulation via SIRT-1 activation
    Manoranjan Sharma
    Dept of Pharmacology, Zydus Research Centre, Moraiya, Ahmedabad, Gujarat, India
    Cytokine 66:30-9. 2014
    ..These results strongly emphasize the involvement of TACE in colon inflammation and inhibition of TACE directly or indirectly via SIRT-1 activation ameliorates colitis. ..
  10. ncbi request reprint Discovery of liver selective non-steroidal glucocorticoid receptor antagonist as novel antidiabetic agents
    Kiran Shah
    Zydus Research Centre, Sarkhej Bavla N H 8A Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem Lett 22:5857-62. 2012
    ..These preliminary results confirm discovery of potent and liver selective passive GR antagonist for the treatment of T2DM...
  11. ncbi request reprint Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole
    Brijesh Kumar Srivastava
    Department of Medicinal Chemistry, Zydus Research Centre, Cadila Healthcare Ltd, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem Lett 18:963-8. 2008
    ..Computer assisted conformational analysis gave a direct clue for the loss of CB1 antagonistic activity of the ligands without a fine docking simulation for the homology model...
  12. ncbi request reprint Selective inhibition of tumor necrosis factor-α converting enzyme attenuates liver toxicity in a murine model of concanavalin A induced auto-immune hepatitis
    Manoranjan Sharma
    Dept of Pharmacology, Zydus Research Centre, Moraiya, Ahmedabad, Gujarat, India
    Int Immunopharmacol 17:229-36. 2013
    ..These observations suggest that selective TACE inhibition is an effective approach for the treatment of both immune mediated hepatic inflammation and fibrosis. ..
  13. ncbi request reprint Ameliorative potential of aliskiren in experimental colitis in mice
    Rakesh B Patel
    Department of Pharmacology, Zydus Research Centre, Sarkhej Bavla National Highway 8A, Moraiya, Ahmedabad 382213, Gujarat, India
    Eur J Pharmacol 737:70-6. 2014
    ..p.) significantly diminished the elevated levels of TNF-α, IL-6 and renin mRNA in inflammed colon. These results indicate involvement of renin in colitis and inhibition of renin by aliskiren ameliorates colitis. ..
  14. ncbi request reprint Blockade of tumor necrosis factor-α converting enzyme (TACE) enhances IL-1β and IFN-γ via caspase-1 activation: a probable cause for loss of efficacy of TACE inhibitors in humans?
    Manoranjan Sharma
    Department of Pharmacology, Zydus Research Centre, Moraiya, Ahmedabad, Gujarat, India
    Eur J Pharmacol 701:106-13. 2013
    ..This novel finding might explain the possible cause behind the loss of efficacy of TACE inhibitors in human...
  15. ncbi request reprint Antithrombotic effects due to pharmacological modulation of thrombin-activatable fibrinolysis inhibitor in rats
    Hitesh Soni
    Zydus Research Centre, Ahmedabad, India
    Pharmacology 82:304-9. 2008
    ..These results provide evidence for a role of TAFI in arterial thrombosis in rats and suggest that TAFI inhibition could be explored as an attractive target for the development of new antithrombotic drugs...
  16. ncbi request reprint Cannabinoid receptor 1 antagonist treatment induces glucagon release and shows an additive therapeutic effect with GLP-1 agonist in diet-induced obese mice
    Kartikkumar Navinchandra Patel
    a Department of Pharmacology and Toxicology, Zydus Research Centre, Cadila Healthcare Limited, Sarkhej Bavla N H No 8A, Moraiya, Ahmedabad 382210, India
    Can J Physiol Pharmacol 92:975-83. 2014
    ..The hyperglucagonemia induced by rimonabant is partially responsible for enhancing the antiobesity effect of exendin-4. ..
  17. ncbi request reprint Anti-nociceptive and anti-allodynic activity of aliskiren in various pain models
    Rakesh B Patel
    Department of Pharmacology, Zydus Research Center, Sarkhej Bavla National Highway 8A, Moraiya, Ahmedabad 382 213, Gujarat, India
    Eur J Pharmacol 708:80-7. 2013
    ..This data suggests that aliskiren may have the potential to be used as an anti-nociceptive and anti-allodynic agent...
  18. ncbi request reprint Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model
    Brijesh Kumar Srivastava
    Zydus Research Centre, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382210, India
    J Med Chem 50:5951-66. 2007
    ....
  19. ncbi request reprint Effect of GLP-1 based therapies on diabetic dyslipidemia
    Vishal J Patel
    Department of Pharmacology and Toxicology, Zydus Research Centre, Sarkhej Bavla NH No 8A, Moraiya, Ahmedabad 382210, India
    Curr Diabetes Rev 10:238-50. 2014
    ..This review mainly deliberates the association of GLP-1 in lipid regulation via lipid absorption, hepatic cholesterol metabolism, reverse cholesterol transport and progression of atherosclerosis. ..
  20. pmc Pharmacokinetics, safety, and tolerability of saroglitazar (ZYH1), a predominantly PPARα agonist with moderate PPARγ agonist activity in healthy human subjects
    Rajendra H Jani
    Clinical R and D, Zydus Research Centre, Cadila Healthcare Limited, Sarkhej Bavla N H No 8A, Moriya, Ahmedabad, 382 213, Gujarat, India
    Clin Drug Investig 33:809-16. 2013
    ..The objective of this phase 1 study was to evaluate the pharmacokinetics, safety and tolerability of saroglitazar in healthy human subjects...
  21. ncbi request reprint Effect of saponins from Helicteres isora on lipid and glucose metabolism regulating genes expression
    Shefalee K Bhavsar
    Department of Pharmacology, L M College of Pharmacy, Navarangapura, Ahmedabad 380009, Gujarat, India
    J Ethnopharmacol 124:426-33. 2009
    ..We characterized saponins as active constituents from traditionally used antidiabetic plant Helicteres isora...
  22. pmc Evaluation of Cardioprotective Effect of 3,5,3'-Tri-iodo-L-thyronine in Isoproterenol-Induced Cardiotoxicity
    Vinay Mishra
    Department of Pharmacology and Toxicology, Zydus Research Center, Sarkhej Bavla N H No 8A, Moraiya, Ahmedabad 382213, India
    Int J Endocrinol 2011:908367. 2011
    ....
  23. ncbi request reprint Synthesis and antidiabetic activity of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines and thieno[2,3-b]pyridines
    Rajesh H Bahekar
    Zydus Research Centre, Cadila Healthcare Ltd, Sarkhej Bavala N H 8A, Moraiya, Ahmedabad, India
    Bioorg Med Chem 15:6782-95. 2007
    ..In general, compounds 2c and 3c were found to be equipotent at all the three different doses selected and with respect to BL 11282, both the test compounds were found to be more potent, at all the time points...
  24. ncbi request reprint Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones
    Brijesh Kumar Srivastava
    Zydus Research Centre, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382210, India
    Bioorg Med Chem Lett 17:5227-32. 2007
    ....
  25. ncbi request reprint Synthesis and in vitro antibacterial activities of novel oxazolidinones
    Brijesh Kumar Srivastava
    Zydus Research Centre, Department of Medicinal Chemistry, Sarkhej Bavla N H 8A, Moraiya, Ahmedabad 382210, Gujarat, India
    Eur J Med Chem 43:683-93. 2008
    ....
  26. ncbi request reprint Synthesis of 3,8,9-trisubstituted-1,7,9-triaza-fluorene-6-carboxylic acid derivatives as a new class of insulin secretagogues
    Rajesh H Bahekar
    Zydus Research Center, Cadila Healthcare Ltd, Sarkhej Bavala NH 8A, Moraiya, Ahmedabad, India
    Bioorg Med Chem 15:5950-64. 2007
    ..Some of the test compounds from each series were found to be equipotent to standard compound (Harmane), indicating that the pyridine ring systems of substituted-triaza-fluorenes act as bioisosteres of benzene ring in beta-carbolines...
  27. ncbi request reprint Synthesis and antidiabetic activity of 3,6,7-trisubstituted-2-(1H-imidazol-2-ylsulfanyl)quinoxalines and quinoxalin-2-yl isothioureas
    Rajesh H Bahekar
    Zydus Research Centre, Cadila Healthcare Ltd, Moraiya, Ahmedabad, India
    Arch Pharm (Weinheim) 340:359-66. 2007
    ....