Indoline Derivatives I: Synthesis and Factor Xa (FXa) Inhibitory Activities
|
Accession number;06A0107325
|
| Title;Indoline Derivatives I: Synthesis and Factor Xa (FXa) Inhibitory Activities |
| Author;
NOGUCHI TETSUJI
(Medicinal Chemistry Res. Laboratories, Sankyo Co., Ltd.)
TANAKA NAOKI
(Medicinal Chemistry Res. Laboratories, Sankyo Co., Ltd.)
NISHIMATA TOYOKI
(Medicinal Chemistry Res. Laboratories, Sankyo Co., Ltd.)
GOTO RIKI
(Medicinal Chemistry Res. Laboratories, Sankyo Co., Ltd.)
HAYAKAWA MIHO
(Medicinal Chemistry Res. Laboratories, Sankyo Co., Ltd.)
SUGIDACHI ATSUHIRO
(Pharmacology And Molecular Biology Res. Laboratories, Sankyo Co., Ltd.)
OGAWA TAKETOSHI
(Pharmacology And Molecular Biology Res. Laboratories, Sankyo Co., Ltd.)
ASAI FUMITOSHI
(Pharmacology And Molecular Biology Res. Laboratories, Sankyo Co., Ltd.)
MATSUI YUMI
(Core Technol. Res. Laboratories, Sankyo Co., Ltd.)
FUJIMOTO KOICHI
(Medicinal Chemistry Res. Laboratories, Sankyo Co., Ltd.)
|
Journal Title;Chem Pharm Bull
|
Journal Code:G0504A
|
ISSN:0009-2363
|
|
VOL.54;NO.2;PAGE.163-174 (J-STAGE)(2006)
|
| Figure&Table&Reference;FIG.3, TBL.7, REF.23 |
| Pub. Country;Japan |
| Language;English |
| Abstract;A series of bisamidine derivatives each having a ring structure in the center of the molecule was synthesized and their Factor Xa (FXa) inhibitory activities were evaluated. Among them, some indoline derivatives showed potent inhibitory activities in vitro. In particular, (R)-18a having an (R)-configuration at the 2-position of the indoline ring exhibited the most potent FXa inhibitory activity in vitro, more potent than DX-9065a. Furthermore, (R)-18a exhibited more potent anticoagulant activity than DX-9065a. We also succeeded in obtaining an X-ray crystal structure of FXa bound with (R)-18a. (Author abst.) |
|
|
|
Related Articles;
|
|
|
