M. Anthony McKervey

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A series of novel synthetic dipeptides, containing a C-terminal glyoxal grouping (-COCHO), have been tested as inhibitors against typical members of the serine- and cysteine-proteinase families. For example, the sequences benzyloxycarbonyl (Cbz)-Pro-Phe-CHO (I) and Cbz-Phe-Ala-CHO (II), which fulfil the known primary and secondary specificity requirements(More)
A new lupane type triterpenic acid, pulsatillic acid, and two new lupane type triterpenoid glycosides, pulsatilloside A and B, along with the known 23-hydroxybetulinic acid were isolated from the roots of Pulsatilla chinensis. Their structures were characterized as 3-oxo-23-hydroxy-lup-20(29)-en-28-oic acid, 3 beta, 23-dihydroxy-lup-20(29)-en-28-oic acid(More)
A series of peptidyl alpha-keto aldehydes (glyoxals) have been synthesised as putative inhibitors of the chymotryptic-like activity of proteasome. The most potent peptides, Cbz-Leu-Leu-Tyr-COCHO and Bz-Leu-Leu-Leu-COCHO, function as slow-binding reversible inhibitors, exhibiting final Ki values of approximately 3.0 nM. These are among the lowest values so(More)
Four lipophilic sulphur and/or nitrogen containing calixarene derivatives have been tested as ionophores in Ag(I)-selective poly (vinyl chloride) membrane electrodes. All gave acceptable linear responses with one giving a response of 50 mV/dec in the Ag(I) ion activity range 10(-4)-10(-1)M and high selectivity towards other transition metals and sodium and(More)
The complexing ability of a range of 19 symmetrical, unsymmetrical and bridged calix[4]arene derivatives having ester, ketone, amide, amine and thioether functionalities were determined by the picrate extraction method. On incorporating these calix[4]arene derivatives as neutral carrier ionophores in sodium-selective poly (vinyl chloride) membrane(More)
The use of a leucine-derived alpha-keto-beta-aldehyde (glyoxal) as a substrate in the Horner-Emmons (Wadsworth) Wittig reaction has enabled the synthesis of (Z)-7-methyl-5(S)-amino-4-oxo-methyl-oct-2-eneoate. This novel compound is a potent inhibitor (Ki = 76 nM) of leucine aminopeptidase and provides an interesting new template for the development of(More)
The functionalisation of macrocyclic p-tertbutylcalix[4]arenes at the lower rim with hydroxamic acid and proline hydroxamic acid groups gives the calixarenes chelating properties similar to siderophores. The (1)H NMR spectrum of p-tertbutylcalix[4]arene tetrahydroxamic acid shows a broad band at 10.8 ppm in DMSO-d(6) attributed to NHOH protons. Diffuse(More)
Calixarenes are synthetic macrocyclic compounds, described as "molecular baskets" as they possess high ionophoric selectivity and form inclusion complexes with many important ionic guests. In our initial work, hexameric and tetrameric tert-butylcalixarenes, unfunctionalized at the lower rim, are shown to be separable on a diol column using supercritical(More)
A series of synthetic peptides in which the C-terminal carboxyl grouping (-CO(2)H) of each has been chemically converted into a variety of ene dione derivatives (-CO-CH=CH-CO-X; X = -H, -Me, -OBut, -OEt, -OMe, -CO-OMe), have been prepared and tested as inactivators against typical members of the serine and cysteine protease families. For example, the(More)