A series of peptide derivatives based on the transition-state mimetic concept has been designed that inhibit the proteinase from the human immunodeficiency virus (HIV). The more active compounds inhibit both HIV-1 and HIV-2 proteinases in the nanomolar range with little effect at 10 micromolar against the structurally related human aspartic proteinases.… (More)
Two sighted peopled showed a remarkable ability to perceive vibrotactile patterns generated by the Optacon, a reading aid for the blind. These individuals were able to read at very high rates, 70 to 100 words per minute, through their fingertips. Additional testing showed them to be much better than other people at discriminating and recognizing… (More)
Using a combination of gas chromatography, mass spectrometry, and selected ion recording techniques, we have identified nicotine and its major metabolite, continine, in the breast fluid of nonlactating women smokers. As little as 25 picograms could be measured by using the deuterated variants, [5',5'-2H]nicotine and [3,3-2H]cotinine, both as internal… (More)
BACKGROUND The 8-amino and 9-hydroxy substituents of antimalarial cinchona alkaloids have the erythro orientation while their inactive 9-epimers are threo. From the X-ray structures a 90 degrees difference in torsion angle between the N1-H1 and C9-O12 bonds in the two series is believed to be important. In order to kill the malaria parasite, alkaloids must… (More)
Antimalarial chloroquine (CQ) prevents haematin detoxication when CQ-base concentrates in the acidic digestive vacuole through protonation of its p-aminopyridine (pAP) basic aromatic nitrogen and sidechain diethyl-N. CQ export through the variant vacuolar membrane export channel, PFCRT, causes CQ-resistance in Plasmodium falciparum but 3-methyl CQ… (More)
There are errors in the published article. Fig 1 does not show the enantiomeric bond from 4-amino to methyl. In the caption for Fig 1, the reference given is incorrect. The correct reference is . Please see the correct Fig 1 and its caption here. Fig 1. Structures of the main pAP compounds examined. Note outline (blue) of the p-aminopyridine moiety in… (More)
An acetylenic C-glucuronide of the sedative-hypnotic drug ethchlorvynol was isolated from rabbit urine as the major metabolite. The C-glucuronide represents a novel metabolic pathway for acetylenes and is a rare example of the formation of a carbon-glucuronide bond in mammalian systems.