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Antirhino/enteroviral vinylacetylene benzimidazoles: a study of their activity and oral plasma levels in mice.
TLDR
The present study concentrated on fluoro substitution of this class of molecules and found that fluorine substitution directly on the left-hand aromatic ring does give good oral blood levels and fluorine incorporation at other positions in the molecule was not as effective at maintaining either the activity or the oral plasma levels. Expand
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.
TLDR
It was found that the indole-3-glyoxamides with a 4-oxyacetic acid substituent had optimal inhibitory activity and LY315920 (6m) was selected for evaluation clinically as an hnps-PLA2 inhibitor. Expand
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 2. Indole-3-acetamides with additional functionality.
TLDR
The further implementation of this structure-based design strategy and continued SAR development to produce indole-3-acetamides with additional functionalities which provide increased interaction with important residues within the enzyme active site are described. Expand
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 3. Indole-3-glyoxamides.
Phospholipases (PLAs) produce rate-limiting precursors in the biosynthesis of various types of biologically active lipids involved in inflammatory processes. Increased levels of human nonpancreaticExpand
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 1. Indole-3-acetamides.
TLDR
This work describes the syntheses, structure--activity relationships, and pharmacological activities of a series of indole-3-acetamides and related compounds derived from this lead and identifies chemical structures which could inhibit hnps-PLA2. Expand
Small peptidic aldehyde inhibitors of human rhinovirus 3C protease
Abstract Small peptide aldehydes were designed to mimic the preferred substrate requirements for the human rhinovirus 3C protease. Di- and tripeptide aldehydes containing a methionine sulfone as a PExpand
Discovery of antirhinoviral leads by screening a combinatorial library of ureas prepared using covalent scavengers
Abstract Solution phase parallel synthesis of equimolar mixtures of ureas was accomplished using a solid-supported “covalent scavenger” (aminomethylpolystyrene) to remove isocyanate impurities.Expand
Antirhinoviral vinyl acetylene benzimidazoles
TLDR
This work has concentrated on a new series of compounds containing a vinyl acetylene moiety, which possess both good activity and promising bioavailability in animals and are likely to treat the common cold. Expand
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