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Identification and Characterization of a Novel Δ6/Δ5 Fatty Acid Desaturase Inhibitor As a Potential Anti-Inflammatory Agent
TLDR
Results suggest that Δ5 and/or Δ6 desaturase inhibitors have the potential to manifest an anti-inflammatory response by decreasing the level of AA and the ensuing production of eicosanoids. Expand
Identification and characterization of a novel delta6/delta5 fatty acid desaturase inhibitor as a potential anti-inflammatory agent.
TLDR
Results suggest that delta5 and/or delta6 desaturase inhibitors have the potential to manifest an anti-inflammatory response by decreasing the level of AA and the ensuing production of eicosanoids. Expand
Peptidomimetic antagonists of alphavbeta3 inhibit bone resorption by inhibiting osteoclast bone resorptive activity, not osteoclast adhesion to bone.
TLDR
Interestingly, however, osteoclasts treated with SC-65811, SC-56631 or the disintegrin echistatin, at concentrations that inhibit bone resorption did not inhibit osteoclast adhesion to bone, suggesting that alphavbeta3 antagonists inhibited bone resorbent activity or efficiency but not by inhibiting osteopontin- and vitronectin-coated surfaces per se. Expand
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor
TLDR
Four ester prodrug/acid active metabolite pairs from the ABAS series were evaluated in canine studies for their ability to block collagen-induced aggregation in platelet-rich plasma, the elimination profile, repeated oral dosing studies, and oral systemic availability, and a pharmacophore model based on inhibitors from several different benzamidine classes including 2a (ABAS class) was developed. Expand
A novel series of orally active antiplatelet agents.
TLDR
A novel series of orally active fibrinogen receptor antagonists has been discovered through structural modification of the lead intravenous antiplatelet agent, 5-(4-amidinophenyl)pentanoyl-Asp-Phe 1 (SC-52012), found to be a potent inhibitor of canine platelet aggregation in vitro. Expand
Orally bioavailable dual MMP-1/MMP-14 sparing, MMP-13 selective alpha-sulfone hydroxamates.
A series of phenyl piperidine alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that areExpand
Adenovirus inhibition by peptidomimetic integrin antagonists.
TLDR
The results suggest that integrins interact with adenoviral RGD in a manner similar to that of other protein ligands such as vitronectin, and suggest peptidomimetic compounds may be useful antimicrobial agents in the treatment of a variety of diseases. Expand
Design of orally active, non-peptide fibrinogen receptor antagonists. An evolutionary process from the RGD sequence to novel anti-platelet aggregation agents.
TLDR
The evolutionary process from the Arg-Gly-Asp-Phe (RGDF) tetrapeptide to potent orally active anti-platelet agents is presented and the structure-activity relationships described underline the importance of the beta-amino acid substitution for potency. Expand
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