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Non-carboxylic analogues of arylpropionic acids: synthesis, anti-inflammatory activity and ulcerogenic potential.

European journal of medicinal chemistry (2006-10-21)
Kamel A Metwally, Shada H Yaseen, El-Sayed M Lashine, Hassan M El-Fayomi, Mohamed E El-Sadek
ABSTRACT

Two series of 1,2,4-triazoles and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles derived from three selected arylpropionic acids namely, ibuprofen, flurbiprofen and naproxen, were synthesized and evaluated for anti-inflammatory activity and ulcerogenic potential. All the tested compounds exhibited anti-inflammatory activity comparable to that of hydrocortisone. Compared to ibuprofen, however, all the tested compounds displayed more potent anti-inflammatory activity. Compounds tested for ulcerogenicity showed no or minimal ulcerogenic effect compared to indomethacin.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Hydrocortisone, BioReagent, suitable for cell culture
Sigma-Aldrich
Ibuprofen, ≥98% (GC)
Sigma-Aldrich
Hydrocortisone solution, 50 μM, sterile-filtered, BioXtra, suitable for cell culture
Sigma-Aldrich
Indomethacin, 98.5-100.5% (in accordance with EP)
Sigma-Aldrich
Hydrocortisone, ≥98% (HPLC)
Sigma-Aldrich
Hydrocortisone, γ-irradiated, powder, BioXtra, suitable for cell culture
Sigma-Aldrich
Hydrocortisone-Water Soluble, BioReagent, suitable for cell culture
Supelco
Ibuprofen
Sigma-Aldrich
Indomethacin, meets USP testing specifications
Sigma-Aldrich
Ibuprofen, meets USP testing specifications
Sigma-Aldrich
Hydrocortisone, meets USP testing specifications
Supelco
Hydrocortisone, VETRANAL®, analytical standard