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Endothelin receptor antagonist triterpenoid, myriceric acid A, isolated from Myrica cerifera, and structure activity relationships of its derivatives.
As the first non-peptide endothelin receptor antagonist from a higher plant, a new triterpenoid, myriceric acid A (50-235) (1) was isolated from the bayberry, Myrica cerifera. Myriceric acid A (1)Expand
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Total synthesis of human chymase inhibitor methyllinderone and structure--activity relationships of its derivatives.
Total synthesis of human chymase inhibitor methyllinderone has been achieved in only four steps with an overall yield of 21% from dimethyl squarate. We developed an efficient synthetic method forExpand
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Pharmaceutical process chemistry
PART 1: INTRODUCTORY REMARKS From Milligrams to Tons: The Importance of Synthesis & Process Research in the Development of New Drugs PART 2: FUTURE APPLICATIONS Design of Dynamic Salt Catalysts BasedExpand
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Design, synthesis and pharmacological evaluation of 3-benzylazetidine-2-one-based human chymase inhibitors.
3-Benzylazetidine-2-one derivatives were designed and evaluated as a novel series of chymase inhibitors. Structure-activity relationship studies of 3-benzylazetidine-2-ones led to compounds 23, whichExpand
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1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
1-Oxacephem derivatives were evaluated as a novel series of chymase inhibitors. The structure-activity relationship studies of 1-oxacephems led to compounds 15, which exhibited 27 nM inhibition ofExpand
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Synthesis and pharmacological properties of ureidomethylcarbamoylphenylketone derivatives. A new potent and subtype-selective nonpeptide CCK-B/gastrin receptor antagonist, S-0509.
A novel series of CCK-B/gastrin receptor antagonists-ureidomethylcarbamoylphenylketone derivatives-were designed, synthesized, and evaluated for activity. Structure-activity relationship studiesExpand
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