Syntheses of(4, 1-Benzoxazepine-3-ylidene)acetic Acid Derivatives and Their Inhibition of Squalene Synthase^<1)>

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The(3, 5-trans)-7-chloro-5-(2-chlorophenyl)-2-oxo-1, 2, 3, 5-tetrahydro-4, 1-benzoxazepine-3-acetic acid derivatives 1 have been previously identified as potent squalene synthase inhibitors. A series of(4, 1-benzoxazepin-3-yli-dene)acetic acid derivatives were synthesized and evaluated for their inhibition of rat and human squalene synthase, and the(E)-isomers were found to exhibit potent inhibitory activity, with the same potency as 4, 1-benzoxazepine-3-acetie acid derivatives. In contrast the(Z)-isomers did not exhibit significant inhibitory activiey, and the active conformation of the 4, 1-benzoxazepine-3-acetic acid derivatives was deduced from the folded conformation of the(E)-isomers.
社団法人日本薬学会の論文
2002-01-01