Organic & Biomolecular Chemistry · 2004 · 28 citations · 23 references
Combinatorial ChemistryMolecular PharmacologyMedicinal ChemistryBowman-birk Inhibitor AnaloguesBioorganic ChemistryPharmaceutical ScienceBiochemistryNatural Sciences4-Carbon AnaloguesMedicinePeptide SynthesisNatural DisulfideDrug DevelopmentChemical BiologyPharmacologyPharmaceutical ChemistrySynthetic ChemistryDrug Discovery
Bowman-Birk inhibitor analogues containing 2, 3 and 4-carbon analogues of the natural disulfide were synthesised via solid phase microwave-assisted RCM and found to have K(i) values against chymotrypsin in the low to sub-micromolar range, the best replacement for the disulfide arising from the linkage by RCM of two l-homoallylglycine residues.
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