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Dibasic inhibitors of human mast cell tryptase. Part 1: synthesis and optimization of a novel class of inhibitors.
The synthesis and optimization of a novel class of reversible and active-site directed dibasic inhibitors of human mast cell tryptase are described. The compounds were shown to be both remarkablyExpand
Large-Scale Syntheses of FMOC-Protected Non-Proteogenic Amino Acids: Useful Building Blocks for Combinatorial Libraries
Convenient and reliable large-scale procedures for the protection of various amino acids with N-(9-fluorenylmethoxycarbonyl)oxysuccinimide (FMOC-OSu) are described. Commercially availableExpand
An effective chirospecific synthesis of (+)-pilocarpine from L-aspartic acid
A short and efficient synthesis of (+)-pilocarpine (1) has been accomplished in 10 steps and 51% overall yield from L-aspartic acid. The synthesis features a diastereoselective alkylation of aExpand
Dibasic inhibitors of human mast cell tryptase. Part 2: structure-activity relationships and requirements for potent activity.
Detailed structure activity relationships (SARs) for a series of dibasic human tryptase inhibitors are presented. The structural requirements for potent inhibitory activity are remarkably broad withExpand
Novel 1,2-dithiins: synthesis, molecular modeling studies, and antifungal activity.
The first structure-activity study involving the 1,2-dithiin class of compounds (1,2-dithiacyclohexadienes) is herein reported. A series of 3,6-disubstituted 1,2-dithiins was synthesized fromExpand
Dibasic inhibitors of human mast cell tryptase. Part 3: identification of a series of potent and selective inhibitors containing the benzamidine functionality.
A survey of charged groups and linkers for a series of symmetrical and unsymmetrical dibasic inhibitors is described, leading to several classes of potent and selective inhibitors. In particular, theExpand
Solid-phase library synthesis of alkoxyprolines.
The library synthesis of alkoxyprolines was achieved using an acid-stable, nucleophile-cleavable solid support. A hydroxythiophenol linker derived from Merrifield resin was esterified with theExpand
Synthetic analogues of irlbacholine: a novel antifungal plant metabolite isolated from Irlbachia alata.
Irlbacholine and a series of related analogues were synthesized and their antifungal activities against Candida albicans, Cryptococcus neoformans, and Aspergillus fumigatus were assessed. The naturalExpand
Solid-phase synthesis of 2,4-diaminoquinazoline libraries.
A series of libraries containing the 2,4-diaminoquinazoline ring system were prepared, starting from polymer-bound amines. The key steps included reaction of the support-bound amine withExpand