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Your search keyword '"Chandrasena, Gamini"' showing total 5 results
Start Over Author "Chandrasena, Gamini" Journal journal of medicinal chemistry
5 results on '"Chandrasena, Gamini"'

1. Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139

Author

Hopper, Allen T., primary, Juhl, Martin, additional, Hornberg, Jorrit, additional, Badolo, Lassina, additional, Kilburn, John Paul, additional, Thougaard, Annemette, additional, Smagin, Gennady, additional, Song, Dekun, additional, Calice, Londye, additional, Menon, Veena, additional, Dale, Elena, additional, Zhang, Hong, additional, Cajina, Manuel, additional, Nattini, Megan E., additional, Gandhi, Adarsh, additional, Grenon, Michel, additional, Jones, Ken, additional, Khayrullina, Tanzilya, additional, Chandrasena, Gamini, additional, Thomsen, Christian, additional, Zorn, Stevin H., additional, Brodbeck, Robb, additional, Poda, Suresh Babu, additional, Staal, Roland, additional, and Möller, Thomas, additional

Published
2021
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2. 3-Arylimino-2-indolones Are Potent and Selective Galanin GAL3 Receptor Antagonists

Author

Konkel, Michael J., primary, Lagu, Bharat, additional, Boteju, Lakmal W., additional, Jimenez, Hermogenes, additional, Noble, Stewart, additional, Walker, Mary W., additional, Chandrasena, Gamini, additional, Blackburn, Thomas P., additional, Nikam, Sham S., additional, Wright, Jon L., additional, Kornberg, Brian E., additional, Gregory, Tracy, additional, Pugsley, Thomas A., additional, Akunne, Hyacinth, additional, Zoski, Kim, additional, and Wise, Lawrence D., additional

Published
2006
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3. Design and Synthesis of N-[(4-Methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a Novel Peroxisome Proliferator-Activated Receptor α/γ Dual Agonist with Efficacious Glucose and Lipid-Lowering Activities

Author

Devasthale, Pratik V., primary, Chen, Sean, additional, Jeon, Yoon, additional, Qu, Fucheng, additional, Shao, Chunning, additional, Wang, Wei, additional, Zhang, Hao, additional, Cap, Michael, additional, Farrelly, Dennis, additional, Golla, Rajasree, additional, Grover, Gary, additional, Harrity, Thomas, additional, Ma, Zhengping, additional, Moore, Lisa, additional, Ren, Jimmy, additional, Seethala, Ramakrishna, additional, Cheng, Lin, additional, Sleph, Paul, additional, Sun, Wei, additional, Tieman, Aaron, additional, Wetterau, John R., additional, Doweyko, Arthur, additional, Chandrasena, Gamini, additional, Chang, Shu Y., additional, Humphreys, W. Griffith, additional, Sasseville, Vito G., additional, Biller, Scott A., additional, Ryono, Denis E., additional, Selan, Fred, additional, Hariharan, Narayanan, additional, and Cheng, Peter T. W., additional

Published
2004
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4. 3-Arylimino-2-indolones Are Potent and Selective Galanin GAL3 Receptor Antagonists

Author

J. Konkel, Michael, Lagu, Bharat, W. Boteju, Lakmal, Jimenez, Hermogenes, Noble, Stewart, W. Walker, Mary, Chandrasena, Gamini, P. Blackburn, Thomas, S. Nikam, Sham, L. Wright, Jon, E. Kornberg, Brian, Gregory, Tracy, A. Pugsley, Thomas, Akunne, Hyacinth, Zoski, Kim, and D. Wise, Lawrence

Abstract

A series of 3-imino-2-indolones are the first published, high-affinity antagonists of the galanin GAL3 receptor. One example, 1,3-dihydro-1-phenyl-3-[[3-(trifluoromethyl)phenyl]imino]-2H-indol-2-one (9), was shown to have high affinity for the human GAL3 receptor (Ki = 17 nM) and to be highly selective for GAL3 over a broad panel of targets, including GAL1 and GAL2. Compound 9 was also shown to be an antagonist in a human GAL3 receptor functional assay (Kb = 29 nM).

Published
2006

5. Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.

Author

Devasthale PV, Chen S, Jeon Y, Qu F, Shao C, Wang W, Zhang H, Cap M, Farrelly D, Golla R, Grover G, Harrity T, Ma Z, Moore L, Ren J, Seethala R, Cheng L, Sleph P, Sun W, Tieman A, Wetterau JR, Doweyko A, Chandrasena G, Chang SY, Humphreys WG, Sasseville VG, Biller SA, Ryono DE, Selan F, Hariharan N, and Cheng PT

Subjects
Adipocytes cytology, Animals, Blood Glucose drug effects, Cell Line, Diabetes Mellitus, Type 2 drug therapy, Fatty Acids blood, Glycine chemistry, Glycine pharmacology, Humans, Hyperlipidemias drug therapy, Hypoglycemic Agents pharmacokinetics, Hypoglycemic Agents pharmacology, Hypolipidemic Agents pharmacokinetics, Hypolipidemic Agents pharmacology, Insulin blood, Male, Mice, Mice, Obese, Oxazoles chemistry, Oxazoles pharmacology, Transcriptional Activation, Triglycerides blood, Glycine analogs & derivatives, Glycine chemical synthesis, Hypoglycemic Agents chemical synthesis, Hypolipidemic Agents chemical synthesis, Oxazoles chemical synthesis, PPAR alpha agonists, PPAR gamma agonists
Abstract

Muraglitazar/BMS-298585 (2) has been identified as a non-thiazolidinedione PPAR alpha/gamma dual agonist that shows potent activity in vitro at human PPARalpha (EC(50) = 320 nM) and PPARgamma(EC(50) = 110 nM). Compound 2 shows excellent efficacy for lowering glucose, insulin, triglycerides, and free fatty acids in genetically obese, severely diabetic db/db mice and has a favorable ADME profile. Compound 2 is currently in clinical development for the treatment of type 2 diabetes and dyslipidemia.

Published
2005
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