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Syntheses of Fused Heterocyclic Compounds and Their Inhibitory Activities for Squalene Synthase by Takashi Miki; Masakuni Kori; Akira Fujishima; Hiroshi Mabuchi; Ryu-ichi Tozawa; Masahira Nakamura; Yasuo Sugiyama; Hidefumi Yukimasa is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Syntheses of Fused Heterocyclic Compounds and Their Inhibitory Activities for Squalene Synthase about?
A variety of fused heterocyclic compounds (2-11) were synthesized as a modification of the lead compound 1a and evaluated for their inhibition of squalene synthase. 4,1-Benzothiazepine derivative 2, 1,4-benzodiazepine derivative 6, 1,3-benzodiazepine derivative 7, 1-benzazepine derivative 9, and 4,1-benzoxazocine derivative 10 potently inhibited squalene synthase activity, whereas the 4,1-benzoxazepine derivatives 1 was the most potent inhibitor. 4,1-Benzothiazepine S-oxide derivative 4, 1,4benzodiazepine derivative 5, 1,3,4-benzotriazepine derivative 8, and 1,2,3,4-tetrahydroquinoline derivative 11 were found to be weakly active. Comparison of the X-ray structures of these compounds (1a, 2, 4, 5, 7 and 10) suggests that orientation of the 5-(or 6)-phenyl group is important for activity.
Who reads Syntheses of Fused Heterocyclic Compounds and Their Inhibitory Activities for Squalene Synthase?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Takashi Miki; Masakuni Kori; Akira Fujishima; Hiroshi Mabuchi; Ryu-ichi Tozawa; Masahira Nakamura; Yasuo Sugiyama; Hidefumi Yukimasa
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2002
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)