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Biomedical subjects

J Attard

Publications and source records attributed to J Attard.

6 recordsLinked to original sources
PubMed1997

Pressure relief characteristics in alternating pressure air cushions.

In this study a computerised system was used which continuously measured air pressure, interface pressure and pressure-time cycle characteristics of an alternating pressure air cushion (APAC), and calculated the time the interface pressure remained below three chosen thresholds of 20, 40 and 60 mm Hg. Ten healthy volunteers were used to evaluate the pressure relieving characteristics of four APACs. Results indicated significant differences between products when the threshold periods were analysed, showing some devices were not capable of relieving interface pressures below 20 mm Hg. Though deflation pressure decreased to nearer zero, interface pressure did not follow suit.

Adult↗
PubMed1993

Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones.

The design, synthesis, and biological evaluation of a new class of inhibitors of thymidylate synthase (TS) is described. The molecular design was carried out by a repetitive crystallographic analysis of protein-ligand structures. At the onset of this project, we focused on the folate cofactor binding site of a high-resolution ternary crystal complex of Escherichia coli TS, 5'-fluorodeoxyuridylate (5-FdUMP) and a classical glutamate-containing folic acid analog. A preliminary ternary crystal structure of a novel compound was successfully solved. Upon analysis of this initial complex, further structural elaborations were made, and a series of active 5-(arylthio)quinazolinones was developed. The synthetic strategy was based on the displacement of a halogen at the 5-position of a quinazolinone by various aryl thioanions. The compounds were tested for inhibition of purified E. coli and/or human TS, and were assayed for cytotoxicity against three tumor cell lines in vitro. Significant thymidine protection effects were observed with several of the inhibitors, indicating that TS was the intracellular locus of activity.

Crystallography↗
PubMed1987

The disposition of bunolol in the rabbit eye.

Following topical administration to albino rabbits, bunolol hydrochloride, a beta 1- and beta 2-adrenoceptor antagonist, was rapidly absorbed and distributed in ocular tissues, and transformed intraocularly to a single metabolite, dihydrobunolol. The half-life of bunolol was approximately 1.26 hours in the aqueous humor and 1.63 hours in the ciliary body. There was no significant accumulation of bunolol during a four-day period of twice-daily dosing. Most of the drug was excreted in the urine following ocular or intravenous administration.

Absorption↗