Six candidate irreversible inhibitors of uridine--deoxyuridine phosphorylase (EC 2.4.2.3) from Walker 256 rat tumor were synthesized. These compounds connect a terminal sulfonyl fluoride group to the 1-benzyl moiety of 1-benzyl-5-(3-ethoxybenzyl)uracil (9). Although none of the compounds were irreversible inhibitors, the four 3-[(fluorosulfonyl)benzamido] analogues (14-17) of 9 were good reversible inhibitors of the enzyme which were complexed from 125- to 360-fold better than the substrate, 5-fluoro-2'-deoxyuridine.

Animals↗

PubMed1980

Ambulatory hospital dental services.

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Ambulatory Care↗

PubMed1978

The patient's greatest hazard.

To reduce the patient's hazard in the dental office, the dentist must take a medical history, perform a limited medical examination, order and interpret laboratory tests when indicated, initiate medical consultation when necessary, and evaluate the data obtained in order to make appropriate treatment modifications for high risk patients. The current status of health which our population enjoys must not be confused with a status of robustness. An apparently well patient may be in great jeopardy while you are delivering the most skillful dental care unless adequate precautions are taken.

Blood Coagulation Disorders↗

PubMed1978

Mental state and other prognostic factors in femoral fractures of the elderly.

Fifty elderly patients with fractured femurs were followed up for six months. A hospital stay of less than 28 days and a good prefracture mental state were such important favourable prognostic factors that their absence made the outlook poor and carried clear implications concerning management.

Aged↗

PubMed1977

Irreversible enzyme inhibitors. 200. Active-site-directed inhibitors of deoxycytidine kinase.

Forty-three pyrimidine derivatives, mainly containing the 4-aminopyrimidine system, have been prepared and evaluated as inhibitors of deoxycytidine kinase. The most effective inhibitors were 2-alkylthio-4-aminopyrimidines and 1-alky-1-cytosines. The best inhibitors in both groups were those with large alkyl substituents, which indicate that hydrophobic bonding is occurring, possibly in the same area adjacent to the active site.

Alkylation↗

PubMed1976

Irreversible enzyme inhibitors. Inhibitors of guinea pig complement derived by quaternization of substituted pyridines with benzyl halides.

A series of 83 compounds derived from hydrocarbon-substituted pyridines by quaternization with PhCH2Br usually containing a 2-SO2F or 6-Cl-2-SO2F group was synthesized and evaluated as inhibitors of guinea pig complement and in most cases its C1 component. The most active compounds were 3-(4-phenylphenylbutyl)-N-(6-choro-2-fluorosulfonylbenzyl) pyridinium bromide (43) and 3-(4-phenylphenylbutyl)-N-(2-fluorosulfonylbenzyl) pyridinium bromide (44), each showing 50% inhibition at 7.8 muM. The most effective irreversible inhibitor of the C1 component was N-(6-chloro-2-fluorosulfonylbenzyl)-5,6-benzoquinolinium bromide (87), which showed 50% inhibition at 4 muM.

Animals↗

PubMed1974