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. doi 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. doi 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. doi 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. doi 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. doi 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. doi 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
  10. doi 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

Collaborators

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

Detail Information

Publications22

  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. doi 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. doi 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. doi 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. doi 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. doi 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. doi 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...
  10. doi 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...
  11. doi 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...
  12. doi 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...
  13. doi 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. ..
  14. 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
    ....
  15. doi 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...
  16. doi 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...
  17. 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
    ....
  18. 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
    ....
  19. 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
    ....
  20. 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...
  21. 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
    ....
  22. 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...