A Novel Dual Antagonist of Thromboxane A2 and Leukotriene D4 Receptors: Synthesis and Structure-Activity Relationships of Chloroquinolylviny Derivatives
-
- Okamoto Yoshinori
- Chemistry Research Laboratories, Astellas Pharmaceutical Inc.
-
- Yokota Masaki
- Chemistry Research Laboratories, Astellas Pharmaceutical Inc.
-
- Kawazoe Soichiro
- Process Chemistry Laboratories, Astellas Pharmaceutical Inc.
-
- Kubota Hirokazu
- Chemistry Research Laboratories, Astellas Pharmaceutical Inc.
-
- Nagaoka Hitoshi
- Chemistry Research Laboratories, Astellas Pharmaceutical Inc.
-
- Arakida Yasuhito
- Planning & Administration Dept., Astellas Pharmaceutical Inc.
-
- Takeuchi Makoto
- Chemistry Research Laboratories, Astellas Pharmaceutical Inc.
書誌事項
- タイトル別名
-
- A Novel Dual Antagonist of Thromboxane A2 and Leukotriene D4 Receptors: Synthesis and Structure-Activity Relationships of Chloroquinolylvinyl Derivatives
- Novel Dual Antagonist of Thromboxane A2 and Leukotriene D4 Receptors Synthesis and Structure Activity Relationships of Chloroquinolylviny Derivatives
この論文をさがす
抄録
To discover an orally active thromboxane A2 (TXA2) and leukotriene D4 (LTD4) dual antagonist, we designed and synthesized chloroquinolylvinyl derivatives based on the structures of the TXA2 antagonist daltroban and the LTD4 antagonist montelukast. Among these derivatives, 4-{[(2-(4-chlorophenylsulfonylamino)-1-{3-[(E)-2-(7-chloro-2-quinolyl)vinyl]phenyl}ethyl)thio]methyl}benzoic acid (18d) showed potent inhibitory activity against U46619-induced aggregation of guinea pig platelets and LTD4-induced contraction in the guinea pig ileum, with IC50 values of 340 nm and 0.40 nm, respectively. Oral administration of 18 d also inhibited both the LTD4-induced acceleration of plasma leakage to skin in guinea pig and the U46619-induced increase in airway resistance in guinea pig with ED50 values of 0.47 mg/kg and 3.3 mg/kg, respectively.
収録刊行物
-
- CHEMICAL & PHARMACEUTICAL BULLETIN
-
CHEMICAL & PHARMACEUTICAL BULLETIN 54 (5), 603-610, 2006
公益社団法人 日本薬学会
- Tweet
キーワード
詳細情報 詳細情報について
-
- CRID
- 1390282679144996864
-
- NII論文ID
- 110004836339
-
- NII書誌ID
- AA00602100
-
- COI
- 1:CAS:528:DC%2BD28Xmt1ehsrg%3D
-
- ISSN
- 13475223
- 00092363
-
- NDL書誌ID
- 7892760
-
- PubMed
- 16651753
-
- 本文言語コード
- en
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可