Synthesis and Biological Evaluation of New Piplartine Analogues As Potent Aldose Reductase Inhibitors (ARIs)

Overview

Journal Eur J Med Chem

Specialty Chemistry

Date 2012 Nov 6

PMID 23124161

Citations 15

Authors

Vidadala Ramasubba Rao

Puppala Muthenna

Gundeti Shankaraiah

Chandrasekhar Akileshwari

Kothapalli Hari Babu

Ganji Suresh

Katragadda Suresh Babu

Rotte Sateesh Chandra Kumar

Kothakonda Rajendra Prasad

Potharaju Ashok Yadav

J Mark Petrash

Geereddy Bhanuprakash Reddy

Janaswamy Madhusudana Rao

Affiliations

Soon will be listed here.

Abstract

As a continuation of our efforts directed towards the development of anti-diabetic agents from natural sources, piplartine was isolated from Piper chaba, and was found to inhibit recombinant human ALR2 with an IC(50) of 160 μM. To improve the efficacy, a series of analogues have been synthesized by modification of the styryl/aromatic and heterocyclic ring functionalities of this natural product lead. All the derivatives were tested for their ALR2 inhibitory activity, and results indicated that adducts 3c, 3e and 2j prepared by the Michael addition of piplartine with indole derivatives displayed potent ARI activity, while the other compounds displayed varying degrees of inhibition. The active compounds were also capable of preventing sorbitol accumulation in human red blood cells.

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