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Synthesis and biological evaluation of triazepane derivatives as DPP-IV inhibitors
- Park, Woul Seong;
- Jun, Mi Ae;
- Shin, Mi Sik;
- Kwon, Sung Wook;
- Kang, Seung Kyu;
- ... Lee, Duck Hyung;
- 외 7명
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15초록
A series of triazepane derivatives such as (R)-3-amino-1-(1,2,5-triazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-ones (7, 13a-p) and (R)-3-amino-1-(1,2,5-triazepan-5-yl)-4-(2,4,5-trifluorophenyl)butan-1-ones (17a-e) was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DPP-IV) enzyme. Compounds with the acid moiety were found to be potent inhibitors of DPP-IV without inhibiting CYP 3A4. Among them, compound 13p ((R)-4-[1-acetyl-2-{3-amino-4-(2,4,5-trifluorophenyl)butanoyl-1,2,5-triazepan-5-carbonyl}benzoic acid]) showed a good in vitro activity without inhibiting CYP. (C) 2009 Elsevier B.V. All rights reserved.
키워드
Dipeptidyl peptidase IV; Incretin; Diabetes; Triazepane; DIPEPTIDYL-PEPTIDASE-IV; GLUCAGON-LIKE PEPTIDE-1; GLUCOSE-TOLERANCE; DISCOVERY; POTENT; PHARMACOKINETICS; METABOLISM
- 제목
- Synthesis and biological evaluation of triazepane derivatives as DPP-IV inhibitors
- 저자
- Park, Woul Seong; Jun, Mi Ae; Shin, Mi Sik; Kwon, Sung Wook; Kang, Seung Kyu; Kim, Ki Young; Rhee, Sang Dal; Bae, Myung Ae; Narsaiah, Banda; Lee, Duck Hyung; Cheon, Hyae Gyeong; Ahn, Jin Hee; Kim, Sung Soo
- 발행일
- 2009-11
- 유형
- Article
- 권
- 130
- 호
- 11
- 페이지
- 1001 ~ 1010
- 언어
- ENG
- 출판사
- Elsevier BV
- 발행국가
- 스위스
- 분량
- 10 페이지
- ISSN
- E 1873-3328
P 0022-1139