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Syntheses of (4,1-benzoxazepine-3-ylidene)acetic Acid Derivatives and Their Inhibition of Squalene Synthase

Syntheses of (4,1-benzoxazepine-3-ylidene)acetic Acid Derivatives and Their Inhibition of Squalene Synthase

Takashi Miki, Masakuni Kori, Ryu-ichi Tozawa, Masahira Nakamura, Yasuo Sugiyama, Hidefumi Yukimasa

Chem Pharm Bull (Tokyo). 2002 Jan;50(1):53-8.

PMID: 11824585

Abstract:

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-ylidene)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-acetic acid derivatives. In contrast the (Z)-isomers did not exhibit significant inhibitory activity, and the active conformation of the 4,1-benzoxazepine-3-acetic acid derivatives was deduced from the folded conformation of the (E)-isomers.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
LS7931244	1,3,5-Trimethyl-1H-pyrazol-4-ylboronic acid			Price

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