Yamaguchi K, Yada M, Tsuji T, Hatanaka Y, Goda K, Kobori T
Sagami Chemical Research Center, Sagamihara, Kanagawa, Japan.
Bioorg Med Chem Lett. 1999 Apr 5;9(7):957-60. doi: 10.1016/s0960-894x(99)00122-5.
A series of 4-phenylthiazole derivatives were synthesized and tested their inhibitory effect on the interleukin-6 secretion stimulated by PTH in osteoblastic cells. SCRC2941-18, 2-amino-4-(4-chlorophenyl)-5-methylthiazole, was found to be the most potent inhibitor in the derivatives. Furthermore, SCRC2941-18 significantly suppressed the bone weight loss in the ovariectomized mice, an osteoporosis model.
合成了一系列4-苯基噻唑衍生物，并测试了它们对成骨细胞中甲状旁腺激素（PTH）刺激的白细胞介素-6分泌的抑制作用。发现SCRC2941-18（2-氨基-4-（4-氯苯基）-5-甲基噻唑）是这些衍生物中最有效的抑制剂。此外，SCRC2941-18显著抑制了去卵巢小鼠（一种骨质疏松模型）的骨量流失。
