Advertisement

Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-(2-oxocyclopentyl)methylphenyl}propanoic acid: Non-steroidal Anti-inflammatory Drugs with Low Gastric Ulcerogenic Activity.

20:49 EDT 19th May 2013 | BioPortfolio

Summary of "Synthesis and biological evaluation of derivatives of 2-{2-fluoro-4-(2-oxocyclopentyl)methylphenyl}propanoic acid: Non-steroidal Anti-inflammatory Drugs with Low Gastric Ulcerogenic Activity."

We previously reported that 2-fluoroloxoprofen has lower gastric ulcerogenic activity than loxoprofen, a non-steroidal anti-inflammatory drug (NSAID) without selectivity for COX-2. We synthesized derivatives of 2-fluoroloxoprofen and studied their properties. Compared to 2-fluoroloxoprofen, one derivative, 11a, exhibited higher anti-inflammatory activity and an equivalent ulcerogenic effect. These results suggest that 11a could be therapeutically beneficial for use as an NSAID.

Affiliation

Journal Details

This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804
Pages:

Links

Medical and Biotech [MESH] Definitions

Ethylenes

Derivatives of ethylene, a simple organic gas of biological origin with many industrial and biological use.

Synthetic Biology

A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.

Dexamethasone

An anti-inflammatory 9-fluoro-glucocorticoid.

Evaluation Studies As Topic

Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.

Drug Evaluation, Preclinical

Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.

PubMed Articles [ 17975 Associated PubMed Articles listed on BioPortfolio]

Properties and Synthesis of 2-{2-Fluoro (or Bromo)-4-(2-oxocyclopentyl)methylphenyl}propanoic Acid: Nonsteroidal Anti-inflammatory Drugs with Low Membrane Permeabilizing and Gastric Lesion-Producing Activities.

We previously proposed that membrane permeabilization activity of NSAIDs is involved in NSAID-induced gastric lesions. We here synthesized derivatives of loxoprofen that have lower membrane permeabili...

A practical synthesis of Rho-Kinase inhibitor Y-27632 and fluoro derivatives and their evaluation in human pluripotent stem cells.

A practical synthesis of the Rho-Kinase inhibitor Y-27632 and two new fluoro derivatives was achieved in seven steps and with a good overall yield of 45% starting from commercially available (R)-1-phe...

Synthesis, hypolipidemic and hypoglycemic activity of some novel 2-(4-(2-substituted aminothiazole-4-yl) phenoxy)-2-methyl propanoic acid derivatives.

An improved synthetic protocol for a novel series of 2-(4-(2-substituted aminothiazole-4-yl) phenoxy)-2-methyl propanoic acid derivatives has been developed using different methods of synthesis. The s...

4-deoxy-4-fluoro-xyloside derivatives as inhibitors of glycosaminoglycan biosynthesis.

Various 4-deoxy-4-fluoro-xylosides were prepared using click chemistry for evaluating their potential utility as inhibitors of glycosaminoglycan biosynthesis. 2,3-Di-O-benzoyl-4-deoxy-4-fluoro-β-D-xy...

Synthesis and Biological Activities of 2-Amino-thiazole-5-carboxylic Acid Phenylamide Derivatives.

In an attempt to develop potent and selective anti-tumor drugs, a series of novel 2-amino-thiazole-5-carboxylic acid phenylamide derivatives were designed based on the structure of dasatinib. All comp...

Clinical Trials [ 1437 Associated Clinical Trials listed on BioPortfolio]

5-Fluoro-2'-Deoxycytidine and Tetrahydrouridine in Treating Patients With Advanced Solid Tumors

RATIONALE: Drugs used in chemotherapy, such as 5-fluoro-2'-deoxycytidine and tetrahydrouridine, work in different ways to stop the growth of tumor cells, either by killing the cells or by...

A Study Evaluating the Effects of Lipid Lowering Treatment on Steroid Synthesis

Cholesterol is the precursor of glucocorticoids, mineralocorticoids and sex steroids. Both adrenal and non-adrenal (ovarian + testicular) all steroid hormones are primarily synthesized usi...

5-Fluoro-2-Deoxycytidine and Tetrahydrouridine in Treating Patients With Acute Myeloid Leukemia or Myelodysplastic Syndromes

RATIONALE: 5-Fluoro-2'-deoxycytidine (FdCyd) may inhibit cancer cell growth by increasing the production in cells of compounds that suppress growth or by otherwise killing cells. Although...

Effect of Nutrition on Muscle Protein Synthesis

The present proposal is designed to examine the effect of carbohydrate and protein co-ingestion on muscle protein synthesis during endurance type exercise activities. We hypothesize that m...

Coronally Advanced Flap in Combination With Acellular Dermal Matrix and Enamel Matrix Derivatives for Root Coverage

The aim of this study is to compare the clinical outcomes of root coverage procedures, using coronally advanced flap in combination with acellular dermal matrix with or without enamel ma...

Search BioPortfolio: