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Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

IDPH 8261, IDPH-8261

Target

COX

Mechanism

COX inhibitors(Cyclooxygenases inhibitors)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Rheumatic Diseases

Originator Organization

Indian Drugs & Pharmaceuticals Ltd.

Active Organization-

Inactive Organization

Indian Drugs & Pharmaceuticals Ltd.

Drug Highest PhasePendingPhase 3

First Approval Date-

Regulation-

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Structure

Molecular FormulaC14H14O2S

InChIKeyWINXAKJYORVNHU-UHFFFAOYSA-N

CAS Registry108912-17-0

Herein we report an efficient procedure to synthesize S-4-(3-thienyl)phenyl-alpha-methylacetic acid, an enantiomerically pure intermediate of a recently approved nonsteroidal antiinflammatory cyclooxygenase inhibitor, atliprofen [methyl RS-4-(3-thienyl)phenyl-alpha-methylacetate]. The interactions of the active S-isomer of the acid were theoretically compared with those of S-ibuprofen through molecular docking studies using COX-1 and COX-2 protein structures. The results were corroborated by in vitro and in vivo studies.

01 Jan 1995·Indian journal of experimental biology

IDPH-8261--a new nonsteroidal antiinflammatory agent.

Article

Author: Rao, B E ; Singh, P P ; Muralidhar, N ; Rao, C S ; Trivedi, B S ; Junnarkar, A Y

IDPH-8261, methyl alpha-methyl-4-(3-thienyl)benzeneacetate, exhibited marked anti-inflammatory activity in acute, subacute and chronic models of inflammation. In rats, IDPH-8261 exhibited a dose related inhibition of carrageenin-induced rat paw edema and the inhibition was greater than ibuprofen, phenylbutazone, but was three times less than indomethacin. It exhibited anti-inflammatory activity in normal and adrenalectomized rats. It also exhibited the activity against various phlogistic agents. IDPH-8261 exhibited AI activity in subacute granuloma tests. In adjuvant-induced established polyarthritis. IDPH-8261 exhibited anti-arthritic effect at a very low dose (ED50 = 4 mg/kg, p.o.). Ulcerogenic liability was the lowest (UD50 = 180 mg/kg, p.o.), when compared to reference standard drugs. Low toxicity and high efficacy may make this compound a potentially useful therapeutic agent.

100 Deals associated with Atliprofen methyl ester

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