Discovery of a novel series of indoline carbamate and indolinylpyrimidine derivatives as potent GPR119 agonists

…, H Sugimoto, K Rikimaru, H Imoto, M Kamaura…

文献索引：Sato, Kenjiro; Sugimoto, Hiromichi; Rikimaru, Kentaro; Imoto, Hiroshi; Kamaura, Masahiro; Negoro, Nobuyuki; Tsujihata, Yoshiyuki; Miyashita, Hirohisa; Odani, Tomoyuki; Murata, Toshiki Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 5 p. 1649 - 1666

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被引用次数: 6

摘要

Abstract GPR119 has emerged as an attractive target for anti-diabetic agents. We identified a structurally novel GPR119 agonist 22c that carries a 5-(methylsulfonyl) indoline motif as an early lead compound. To generate more potent compounds of this series, structural modifications were performed mainly to the central alkylene spacer. Installation of a carbonyl group and a methyl group on this spacer significantly enhanced agonistic activity, ...