In 2010,Yu, Ming; Lizarzaburu, Mike; Beckmann, Holger; Connors, Richard; Dai, Kang; Haller, Katrin; Li, Cong; Liang, Lingming; Lindstrom, Michelle; Ma, Ji; Motani, Alykhan; Wanska, Malgorzata; Zhang, Alex; Li, Leping; Medina, Julio C. published 《Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity》.Bioorganic & Medicinal Chemistry Letters published the findings.Application of 29682-15-3 The information in the text is summarized as follows:
Piperazine-bisamide analogs I (X = 1,4-phenylene, 2-fluoro-1,4-phenylene, pyridine-2,5-diyl, thiazole-2,4-diyl, etc.; R1 = Ph, 6-indolyl, 8-quinolinyl, etc.; R2, R3 = H, Me; R4 = Ph, 3-MeOC6H4, 2-ClC6H4, 4-pyridyl, etc.) were synthesized and studied for their binding to human growth hormone secretagogue receptor (GHSR). Compounds I [X = 1,4-phenylene; R4 = (un)substituted phenyl] were shown to be partial agonists of GHSR in a high throughput screening. The partial agonists were optimized for potency and converted into antagonists through structure-activity relationship (SAR) studies. The efforts led to the identification of potent antagonist I [X = 3-fluoro-1,4-phenylene; R1 = 6-indolyl; R2 = (S)-Me; R3 = H; R4 = 4-pyridyl] with favorable PK profile suitable as a tool compound for in vivo studies.Methyl 5-bromopicolinate(cas: 29682-15-3Application of 29682-15-3) was used in this study.
Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. Pyridine derivatives lend themselves to many roles in the spirited field of supramolecular chemistry – whether as the ligand backbone of metal-organic polymers or presiding over the key electronic stations of nanodevices. In biochemistry, pyridine-containing cofactors are necessary nutrients on which our lives depend. Application of 29682-15-3