1932043-29-2Relevant academic research and scientific papers
Synthesis and biological evaluation of pyrimidine derivatives with diverse azabicyclic ether/amine as novel GPR119 agonist
Yang, Zunhua,Fang, Yuanying,Park, Haeil
, p. 2515 - 2519 (2017/05/10)
A class of novel pyrimidine derivatives bearing diverse conformationally restricted azabicyclic ether/amine were designed, synthesized and evaluated for their GPR119 agonist activities against type 2 diabetes. Most compounds exhibited superior hEC50
Bridged bicyclic amine derivatives useful as CCR-3 receptor antagonists
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Page/Page column 8; 9; 10, (2010/02/08)
Compounds having the formula (I), Ar—(F)(E)-(CR3R4)—(CHR5)m-(T)-(Q)-Ar1, are useful as CCR-3 receptor antagonists, wherein T is a bridged heterocyclyl group having one N atom and a bridge of one to two bridgehead carbon atoms; Ar and Ar1 are aryl or heteroaryl; F is alkylene, alkenylene, or a bond; E is —C(═O)N(R10)—, —SO2N(R10)—, —N(R11)C(═O)N(R10O)—, —N(R11)SO2N(R10)—, —N(R11)C(═S)N(R10)—, —N(R11)C(═O)—, —N(R11)SO2—, —N(R12)C(═O)CH(R13)—, or CH(R13)C(═O)N(R12)—; Q is —C(═O)— or C1-2alkylene; and R3, R4, R5, R9, R10, R11, R12, and R13 are defined as set forth in the specification.
Design and synthesis of novel CCR3 antagonists
Gong, Leyi,Hogg, J. Heather,Collier, James,Wilhelm, Robert S.,Soderberg, Carol
, p. 3597 - 3600 (2007/10/03)
As part of our investigation into the development of potent CCR3 antagonists, a series of piperidine analogues was designed and prepared. Exploration of the piperidine core examined both the basicity and the location of a nitrogen, as well as conformational variants. The bicyclo-piperidine 24c was found to be the most potent inhibitor of CCR3 with an IC50 of 0.0082 μM in the binding assay and 0.0024 μM in the chemotaxis assay.
