Synthesis and aldose reductase inhibitory activities of novel dibenzocycloheptenone derivatives

Jun Inoue; Ying She Cui; Libaniel Rodriguez; Zhou Chen; Peter F. Kador

doi:10.1016/S0223-5234(99)80089-0

Synthesis and aldose reductase inhibitory activities of novel dibenzocycloheptenone derivatives

Jun Inoue, Ying She Cui, Libaniel Rodriguez, Zhou Chen, Peter F. Kador

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

A number of dibenzocycloheptenone derivatives, a novel series of aldose reductase inhibitors, were synthesized and evaluated in vitro for their ability to inhibit rat lens aldose reductase enzyme. The design of these ARIs was based on previously published pharmacophore requirements. The most active compound in this series was a spirosuccinimide derivative, spiro{2,8- dihydroxy-5H-dibenzo[a, d]cycloheptene5,3'-pyrrolidine}-2',5'-dione 11, having an IC₅₀ of 3.0 μM.

Original language	English (US)
Pages (from-to)	399-404
Number of pages	6
Journal	European Journal of Medicinal Chemistry
Volume	34
Issue number	5
DOIs	https://doi.org/10.1016/S0223-5234(99)80089-0
State	Published - May 1999
Externally published	Yes

Keywords

Aldose reductase inhibitor
Diabetic complications
Dibenzocycloheptenone

ASJC Scopus subject areas

Pharmacology
Drug Discovery
Organic Chemistry

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10.1016/S0223-5234(99)80089-0

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title = "Synthesis and aldose reductase inhibitory activities of novel dibenzocycloheptenone derivatives",

abstract = "A number of dibenzocycloheptenone derivatives, a novel series of aldose reductase inhibitors, were synthesized and evaluated in vitro for their ability to inhibit rat lens aldose reductase enzyme. The design of these ARIs was based on previously published pharmacophore requirements. The most active compound in this series was a spirosuccinimide derivative, spiro{2,8- dihydroxy-5H-dibenzo[a, d]cycloheptene5,3'-pyrrolidine}-2',5'-dione 11, having an IC50 of 3.0 μM.",

keywords = "Aldose reductase inhibitor, Diabetic complications, Dibenzocycloheptenone",

author = "Jun Inoue and Cui, {Ying She} and Libaniel Rodriguez and Zhou Chen and Kador, {Peter F.}",

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T1 - Synthesis and aldose reductase inhibitory activities of novel dibenzocycloheptenone derivatives

AU - Inoue, Jun

AU - Cui, Ying She

AU - Rodriguez, Libaniel

AU - Chen, Zhou

AU - Kador, Peter F.

PY - 1999/5

Y1 - 1999/5

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AB - A number of dibenzocycloheptenone derivatives, a novel series of aldose reductase inhibitors, were synthesized and evaluated in vitro for their ability to inhibit rat lens aldose reductase enzyme. The design of these ARIs was based on previously published pharmacophore requirements. The most active compound in this series was a spirosuccinimide derivative, spiro{2,8- dihydroxy-5H-dibenzo[a, d]cycloheptene5,3'-pyrrolidine}-2',5'-dione 11, having an IC50 of 3.0 μM.

KW - Aldose reductase inhibitor

KW - Diabetic complications

KW - Dibenzocycloheptenone

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Synthesis and aldose reductase inhibitory activities of novel dibenzocycloheptenone derivatives

Abstract

Keywords

ASJC Scopus subject areas

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