New potent antagonists of leukotrienes C4 and D4. 1. Synthesis and structure-activity relationships

…, S Kosuge, S Sakuyama, M Toda, Y Arai…

Index: Nakai; Konno; Kosuge; Sakuyama; Toda; Arai; Obata; Katsube; Miyamoto; Okegawa; Kawasaki Journal of Medicinal Chemistry, 1988 , vol. 31, # 1 p. 84 - 91

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Citation Number: 94

Abstract

12a-b 15a-k. m= O 16a-e, m= l in vivo, so further modifications were carried out on 9 by ring closure at the positions depicted in Table 11. Compounds lla and llb, which contain a five- membered heterocyclic ring, showed potency equal to or less than that of 9 in the in vitro assay. On the other hand, llc and lld, which contain a six-membered heterocyclic ring, showed superior antagonist activity compared to 9. The 4-0xo-4H-l-benzopyran derivative ...