RP-64966(RP-64966) - 药物靶点：水解酶_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

水解酶

作用机制

水解酶抑制剂

治疗领域

免疫系统疾病遗传病与畸形内分泌与代谢疾病+ [2]

在研适应症-

非在研适应症

痛风银屑病类风湿关节炎

原研机构

Rhone-Poulenc SA

在研机构-

非在研机构

Rhone-Poulenc SA

最高研发阶段终止药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C19H24O3S

InChIKeyGJCFOZVWBUJKNH-UHFFFAOYSA-N

CAS号142259-95-8

关联

100 项与 RP-64966 相关的临床结果

登录后查看更多信息

100 项与 RP-64966 相关的转化医学

登录后查看更多信息

100 项与 RP-64966 相关的专利（医药）

登录后查看更多信息

1

项与 RP-64966 相关的文献（医药）

1992-08-01·Journal of Medicinal Chemistry1区 · 医学

.omega.-[(.omega.-Arylalkyl)aryl]alkanoic acids: a new class of specific LTA4 hydrolase inhibitors

1区 · 医学

Article

作者: Dereu, Norbert ; Kuhl, Peter ; Lautenschlaeger, Hans Heiner ; Labaudiniere, Richard ; Hilboll, Gerd ; Parnham, Michael ; Leon-Lomeli, Alicia

The synthesis and structure-activity profile of a new class of potent and specific LTA4 hydrolase inhibitors are described. Many compounds of this series of omega-[5-(omega-arylalkyl)-2-thienyl]- and omega-[4-(omega-arylalkyl)phenyl]alkanoic acids were found to be potent in vitro inhibitors of the LTB4 production by porcine leukocytes with IC50 ranging from 1 to 10 microM. The side-chain lengths were critical for an optimal activity. Substitutions on the terminal aromatic ring, in the benzene series, by lipophilic and electron-donating substituents substantially enhanced the LTA4 hydrolase inhibition potency. On the other hand, in the thiophene series, the effect of of such substitutions on the LTA4 hydrolase inhibition was rather small. Functionalization within the carboxylic acid side chain by a carbonyl or by a hydroxyl group led to less potent compounds. A metabolically stable LTA4 hydrolase inhibitor, RP64966, was obtained by insertion of an oxygen atom in the beta-position on the carboxylic acid side chain. After oral administration of RP64966 to rats, a plasma extract was found to display potent inhibition of the LTB4 biosynthesis (40% inhibition at 5 mg/kg, po).

100 项与 RP-64966 相关的药物交易

登录后查看更多信息