Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Kalapatapu V.V.M. Sairam"'
Publikováno v:
International Journal of Molecular Sciences, Vol 8, Iss 9, Pp 894-919 (2007)
Flavoprotein monoamine oxidase is located on the outer membrane ofmitochondria. It catalyzes oxidative deamination of monoamine neurotransmitters such asserotonin, norepinephrine and dopamine and hence is a target enzyme for antidepressantdrugs. MAO
Externí odkaz:
https://doaj.org/article/fab3a679f20343d7920a7716c17739d5
Autor:
Suresh Giri, Ranjit C. Desai, Prashant K. Deshmukh, Mukul R. Jain, Sameer Agarwal, Amit B. Patil, Umesh Aware, Priyanka Priyadarsiny, Poonam Giri, Brijesh Darji, Kalapatapu V.V.M. Sairam, Harilal Patel, Santosh Sasane
Publikováno v:
ACS Medicinal Chemistry Letters. 7:51-55
TGR5 is a G protein-coupled receptor (GPCR), activation of which promotes secretion of glucagon-like peptide-1 (GLP-1) and modulates insulin secretion. The 2-thio-imidazole derivative 6g was identified as a novel, potent, and selective TGR5 agonist (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::daaa34afb099c04011bf2aff9981f2ea
https://doi.org/10.1021/acsmedchemlett.5b00323
https://doi.org/10.1021/acsmedchemlett.5b00323
Design, synthesis and biological evaluation of novel aminomethyl-piperidones based DPP-IV inhibitors
Autor:
Dipam Patel, Rajesh Bahekar, Amit Joharapurkar, Praveen Kumar Singh, Pradip Jadav, Shailesh R. Shah, Kalapatapu V.V.M. Sairam, Mukul R. Jain
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:1918-1922
A series of novel aminomethyl-piperidones were designed and evaluated as potential DPP-IV inhibitors. Optimized analogue 12v ((4S,5S)-5-(aminomethyl)-1-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-4-(2,5-difluorophenyl)piperidin-2-one) showed excellent in vit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91e791b15adc4657672790a178c9f937
https://doi.org/10.1016/j.bmcl.2014.03.009
https://doi.org/10.1016/j.bmcl.2014.03.009
Autor:
Mukul R. Jain, Amit Joharapurkar, Kalapatapu V.V.M. Sairam, Rajesh Bahekar, Pradip Jadav, Shailesh R. Shah, Dipam Patel, Mubeen Shaikh, Kiran Shah
Publikováno v:
Medicinal Chemistry. 9:660-671
A series of peptidomimetic containing bidentate pTyr mimetics (9a-w) are reported as potent and selective PTP1B inhibitors. Compounds (9p and 9q) showed excellent selectivity towards PTP1B over various PTPs, including TCPTP (in vitro), which confirms
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afeba8e29bd88ae919d6e1580d319555
https://doi.org/10.2174/1573406411309050005
https://doi.org/10.2174/1573406411309050005
Autor:
Vishal B. Unadkat, Kalapatapu V.V.M. Sairam, Jignesh K. Joshi, Vrajesh Pandya, Nirav Joshi, Hiteshkumar Soni, Harilal Patel, Haresh Ajani, Pankaj R. Patel, Bhavesh Sharma, Ganes Chakrabarti, Jigar S. Patel, Jeevan Kumar, Tushar Jarag, Balaji Chaugule, Akshyaya Rath, Mukul R. Jain, Bhavesh Parmar
Publikováno v:
European Journal of Medicinal Chemistry. 58:136-152
A novel series of potent and efficacious factor Xa inhibitors which possesses sulfoximine moiety as novel S4 binding element in anthranilamide chemotype has been identified. Lead optimization at this novel P4 group led to many potent factor Xa inhibi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c56d4fe8f15287f7d9f01b7d6254273
https://doi.org/10.1016/j.ejmech.2012.10.005
https://doi.org/10.1016/j.ejmech.2012.10.005
Autor:
Kishan Patel, Kaushil Patel, Kalapatapu V.V.M. Sairam, Shailesh R. Shah, Mukul R. Jain, Pradip Jadav, Rajendra Chopade, Rajesh Bahekar, Amit Joharapurkar, Shruti Bhardwaj, Dipam Patel, Kiran Shah, Mubeen Shaikh
Publikováno v:
Letters in Drug Design & Discovery. 9:867-873
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c0f420351ec9c82746212382fe110467
https://doi.org/10.2174/157018012803307932
https://doi.org/10.2174/157018012803307932
Autor:
Amit Joharapurkar, Dipam Patel, Rajesh Bahekar, Mubeen Sheikh, Kalapatapu V.V.M. Sairam, Kiran Shah, Mukul R. Jain, Pradip Jadav
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5857-5862
Series of benzyl-phenoxybenzyl amino-phenyl acid derivatives (8a–q) are reported as non-steroidal GR antagonist. Compound 8g showed excellent h-GR binding and potent antagonistic activity (in vitro). The lead compound 8g exhibited significant oral
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e4dda973b5491343037b85dcaeccfbe
https://doi.org/10.1016/j.bmcl.2012.07.078
https://doi.org/10.1016/j.bmcl.2012.07.078
Autor:
Dipam Patel, Kalapatapu V.V.M. Sairam, Amit Joharapurkar, Samadhan Kshirsagar, Rajesh Bahekar, Mubeen Shaikh, Pradip Jadav, Mukul R. Jain, Shailesh R. Shah
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:3516-3521
Pyrrolidine based peptidomimetics are reported as potent and selective DPP-IV inhibitors for the treatment of T2DM. Compounds 16c and 16d showed excellent in vitro potency and selectivity towards DPP-IV and the lead compound 16c showed sustained anti
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5afcabfd7800319373f211a103def8eb
https://doi.org/10.1016/j.bmcl.2012.03.078
https://doi.org/10.1016/j.bmcl.2012.03.078
Autor:
Dipam Patel, Amit Joharapurkar, Mubeen Shaikh, Nirav Dhanesha, Shailesh R. Shah, Prashant Kapadnis, Kalapatapu V.V.M. Sairam, Pradip Jadav, Rajesh Bahekar, Mukul R. Jain
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1111-1117
A novel series of pTyr mimetics containing triaryl-sulfonamide derivatives (5a–r) are reported as potent and selective PTP1B inhibitors. Some of the test compounds (5o and 5p) showed excellent selectivity towards PTP1B over various PTPs, including
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92b7a45f3328d2febacd046a152dd48e
https://doi.org/10.1016/j.bmcl.2011.11.122
https://doi.org/10.1016/j.bmcl.2011.11.122
Autor:
Dipam Patel, Pradip Jadav, Yernaidu Siriki, Rajesh Bahekar, Amit Joharapurkar, Debdutta Bandyopadhyay, Mubeen Shaikh, Samadhan Kshirsagar, Harilal Patel, Brijesh Darji, Kalapatapu V.V.M. Sairam, Shailesh R. Shah, Mukul R. Jain, Pankaj R. Patel
Publikováno v:
ChemMedChem. 6:1011-1016
The worldwide incidence of metabolic syndromes such as obesity and diabetes are increasing at an alarming rate. Patients that suffer from obesity-induced type 2 diabetes (informally known as diabesity) are at increased risk of cardiovascular disease;
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ae2a2abb335a80a8e4217f55ae33c224
https://doi.org/10.1002/cmdc.201100077
https://doi.org/10.1002/cmdc.201100077