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Article Title

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Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.

Goethe-University Frankfurt

Synthesis and biological evaluation of C(5)-substituted derivatives of leukotriene biosynthesis inhibitor BRP-7.

Gazi University

4,5-Diarylisoxazol-3-carboxylic acids: A new class of leukotriene biosynthesis inhibitors potentially targeting 5-lipoxygenase-activating protein (FLAP).

Gazi University

Recent advances for FLAP inhibitors.

Astrazeneca

Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).

Boehringer Ingelheim Pharmaceuticals

Novel benzoxazole inhibitors of mPGES-1.

Pfizer

Identification of novel benzimidazole derivatives as inhibitors of leukotriene biosynthesis by virtual screening targeting 5-lipoxygenase-activating protein (FLAP).

Gazi University

Evaluation of endo- and exo-aryl-substitutions and central scaffold modifications on diphenyl substituted alkanes as 5-lipoxygenase activating protein inhibitors.

Merck Research Laboratories

Substituted 2,2-bisaryl-bicycloheptanes as novel and potent inhibitors of 5-lipoxygenase activating protein.

Merck Frosst Centre For Therapeutic Research

Modulators of leukotriene biosynthesis and receptor activation.

Abbott Laboratories

5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.

Amira Pharmaceuticals

Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: discovery of MK-5286.

Merck Frosst Centre For Therapeutic Research

5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.

Amira Pharmaceuticals

Selective inducible microsomal prostaglandin E(2) synthase-1 (mPGES-1) inhibitors derived from an oxicam template.

Pfizer

5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.

Amira Pharmaceuticals

5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).

Amira Pharmaceuticals

Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX).

Eberhard Karls University Tuebingen

 

Development of L-689,065 - the prototype of a new class of potent 5-lipoxygenase inhibitors

TBA

 

A new class of leukotriene biosynthesis inhibitors: The discovery of MK0591

TBA

Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.

Merck Frosst Centre For Therapeutic Research

Inhibitors of the inducible microsomal prostaglandin E2 synthase (mPGES-1) derived from MK-886.

Merck Frosst Centre For Therapeutic Research

Design and Development of Microsomal Prostaglandin E2 Synthase-1 Inhibitors: Challenges and Future Directions.

University Jena

Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors.

Merck Frosst Center For Therapeutic Research

Discovery and Early Clinical Development of an Inhibitor of 5-Lipoxygenase Activating Protein (AZD5718) for Treatment of Coronary Artery Disease.

TBA

Novel Chemical Series of 5-Lipoxygenase-Activating Protein Inhibitors for Treatment of Coronary Artery Disease.

TBA

Substituted thiopyrano[2,3,4-c,d]indoles as potent, selective, and orally active inhibitors of 5-lipoxygenase. Synthesis and biological evaluation of L-691,816.

Merck Frosst Centre For Therapeutic Research

Thiopyranol[2,3,4-c,d]indoles as inhibitors of 5-lipoxygenase, 5-lipoxygenase-activating protein, and leukotriene C4 synthase.

Merck Frosst Centre For Therapeutic Research

Identification of multi-target inhibitors of leukotriene and prostaglandin E

Gazi University

Discovery and optimization of oxadiazole-based FLAP inhibitors.

Boehringer Ingelheim Pharmaceuticals

Synthesis and HIV-1 RT inhibitory action of novel (4/6-substituted benzo[d]thiazol -2-yl)thiazolidin-4-ones. Divergence from the non-competitive inhibition mechanism.

Aristotle University of Thessaloniki

Carbonic anhydrase inhibitors: in vitro inhibition of a isoforms (hCA I, hCA II, bCA III, hCA IV) by flavonoids.

Ondokuz Mayis University

Chalcones: a valid scaffold for monoamine oxidases inhibitors.

Sapienza University of Rome

Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.

Yale University

Paracyclophanes: a novel class of water-soluble inhibitors of HIV proteinase.

Sandoz Research Institute

Role of inhibitor aliphatic chain in the thermodynamics of inhibitor binding to Escherichia coli enoyl-ACP reductase and the Phe203Leu mutant: a proposed mechanism for drug resistance.

University of Alabama At Birmingham