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초록
A series of heterocycle-linked constrained phenylbenzyl amides were found to be TRPV1 antagonists with promising in vivo profiles. In particular, one of the analogues containing a furan linker exhibited excellent TRPV1 antagonistic activity and in vivo analgesic efficacy. In addition, the binding modes of dibenzyl thiourea, benzylphenethyl amide, and furan-linked phenylbenzyl amide were examined by using the flexible docking study within the rTRPV1 homology model.
키워드
antagonists; ligand design; medicinal chemistry; molecular modeling; TRVP1; VANILLOID RECEPTOR-1 ANTAGONISTS; CAPSAICIN RECEPTOR; BIOLOGICAL EVALUATION; IMPROVED SOLUBILITY; CLINICAL CANDIDATE; DISCOVERY; POTENT; PAIN; ANALOGS; DESIGN
- 제목
- Heterocycle-linked Phenylbenzyl Amides as Novel TRPV1 Antagonists and Their TRPV1 Binding Modes: Constraint-Induced Enhancement of In Vitro and In Vivo Activities
- 저자
- Kim, Nam-Jung; Li, Fu-Nan; Lee, Jin Hee; Park, Seul-gi; Kim, Kyeojin; Lim, Changjin; Han, Young Taek; Yun, Hwayoung; Jung, Jong-Wha; Park, Hyeung-geun; Kim, Hee-Doo; Woo, Byoung Young; Shin, Song Seok; Kim, Sun-Young; Choi, Jin Kyu; Jeong, Yeon-Su; Park, Yanghui; Park, Young-Ho; Kim, Dae-Duk; Choi, Sun; Suh, Young-Ger
- 발행일
- 2013-02
- 유형
- Article
- 권
- 8
- 호
- 2
- 페이지
- 400 ~ 409
- 언어
- ENG
- 출판사
- WILEY-V C H VERLAG GMBH
- 발행국가
- 독일
- 분량
- 10 페이지
- ISSN
- E 1861-471X
P 1861-4728