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Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist

التفاصيل البيبلوغرافية
العنوان: Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist
المؤلفون: William J. Martin, D. Euan MacIntyre, Ravi P. Nargund, Rubana N. Kalyani, Rui Tang, George A. Doss, Min K. Park, Alison M. Strack, Erin McGowan, Joseph M. Metzger, Charles Rosenblum, Randall R. Miller, Palucki Brenda, Qianping Peng, Arthur A. Patchett, Ralph A. Stearns, Patrick G. Pollard, Lex H.T. Van der Ploeg, Iyassu K. Sebhat, Constantin Tamvakopoulos, Cherrie Shepherd, Aurawan Vongs, Tanya MacNeil, David H. Weinberg, Zhixiong Ye
المصدر: Bioorganic & Medicinal Chemistry Letters. 15:171-175
بيانات النشر: Elsevier BV, 2005.
سنة النشر: 2005
مصطلحات موضوعية: Male, Agonist, medicine.drug_class, Stereochemistry, Clinical Biochemistry, Pharmaceutical Science, Carboxamide, Biochemistry, Chemical synthesis, Piperazines, Mice, Dogs, Erectile Dysfunction, Piperidines, In vivo, Drug Discovery, medicine, Animals, Obesity, Receptor, Molecular Biology, Chemistry, Organic Chemistry, Haplorhini, In vitro, Rats, Receptor, Melanocortin, Type 4, Molecular Medicine, Melanocortin
الوصف: We report the discovery and optimization of substituted 2-piperazinecarboxamides as potent and selective agonists of the melanocortin subtype-4 receptor. Further in vivo development of lead agonist, MB243, is disclosed.
تدمد: 0960-894X
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38e9173e9b0b0823886380b760b7694a
https://doi.org/10.1016/j.bmcl.2004.10.020
حقوق: CLOSED
رقم الأكسشن: edsair.doi.dedup.....38e9173e9b0b0823886380b760b7694a
قاعدة البيانات: OpenAIRE
الوصف
تدمد:0960894X