Delving into the Latest Updates on DuP-983 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

POR

Action

inhibitors

Mechanism

POR inhibitors(Cytochrome P450 reductase inhibitors)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Psoriasis

Originator Organization

Bristol Myers Squibb Co.

Active Organization-

Inactive Organization

Bristol Myers Squibb Co.

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC22H18FN3O

InChIKeyDZGMNXWTQWGZTK-UHFFFAOYSA-N

CAS Registry137103-53-8

The synthesis, biological evaluation, and structure-activity relationships of a series of 1-(pyridylphenyl)-1-phenyl-2-imidazolylethanols are described. These compounds show potent dose-dependent topical antiinflammatory activity in murine models of skin inflammation. This effect is likely due to inhibition of cytochrome P450 and consequent reduction in levels of 12R-HETE in the skin. These compounds were examined for their ability to inhibit the oxidative metabolism of arachidonic acid; they specifically inhibit the formation of prostacyclins in mouse macrophages. To study the effects of structure on the in vivo activity, three general features of the molecules were varied: the position of attachment of the pyridine nucleus (A), the second aromatic residue (B), and the nitrogen base on the ethanol chain (C). 1-[4-(4-Pyridyl)phenyl]-1-(4-fluorophenyl)-2- imidazolylethanol (2a, DuP 983) shows a very attractive profile of antiinflammatory activity and has been selected for clinical evaluation as a topical antiinflammatory agent.

Organic Reactions (Hoboken, NJ, United States)

The Stille reaction

Author: Farina, Vittorio ; Krishnamurthy, Venkat ; Scott, William J.

A review of the article The Stille reaction.

100 Deals associated with DuP-983

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