Torisu Kazuhiko, Kobayashi Kaoru, Iwahashi Maki, Egashira Hiromu, Nakai Yoshihiko, Okada Yutaka, Nanbu Fumio, Ohuchida Shuichi, Nakai Hisao, Toda Masaaki
Minase Research Institute, Ono Pharmaceutical Co., Ltd, Shimamoto, Mishima, Osaka 618-8585, Japan.
Bioorg Med Chem Lett. 2004 Sep 6;14(17):4557-62. doi: 10.1016/j.bmcl.2004.06.006.
A series of Indomethacin analogs were synthesized and biologically evaluated. Among the compounds tested, N-(p-butoxy)benzoyl-2-methylindole-4-acetic acid 2 was discovered as a new chemical lead for a prostaglandin D2 (PGD2) receptor antagonist. Structure-activity relationship data are also presented.
合成了一系列吲哚美辛类似物并进行了生物学评估。在测试的化合物中,发现N-(对丁氧基)苯甲酰基-2-甲基吲哚-4-乙酸2是一种新型前列腺素D2(PGD2)受体拮抗剂的化学先导物。还给出了构效关系数据。