Biomedical subjects

T Draper

Publications and source records attributed to T Draper.

14 recordsLinked to original sources

PubMed1996

Growth rate of infrarenal aortic aneurysms.

OBJECTIVE: To delineate the natural history of infrarenal aortic aneurysms with respect to growth rate. METHODS: A referral based series of 233 patients with abdominal aortic aneurysm was serially assessed by abdominal ultrasound. RESULTS: The mean age was 71 years and the median follow up 26 months (range 6-146). The mean growth rate of the series was 3.2mm/year. Division of the initial size into those less than 41 mm (128 patients), between 41-60 mm (92 patients) and those above 60 mm (13 patients) in AP diameter showed mean growth rates per year were 2.6 mm/year, 4.1 mm/year and 6.5 mm/year. Examination of the relationship between aneurysm size and subsequent growth rate over the whole study period revealed a rank correlation of 0.19 (p = 0.002). Aneurysms were also observed to expand at an erratic rate both in terms of time and size. CONCLUSIONS: When the initial decision is to observe the patient, serial ultrasound examinations facilitate later judgements on the balance of risks in relation to surgical treatment.

Adult↗

PubMed1995

Structures of four methyltetrazole-containing antiviral compounds in human rhinovirus serotype 14.

Four novel antiviral WIN compounds, that contain a methyl tetrazole ring as well as isoxazole, pyridazine or acetylfuran rings, have had their structures determined in human rhinovirus serotype 14 at 2.9 A resolution. These compounds bind in the VP1 hydrophobic pocket, but are shifted significantly towards the pocket pore when compared to previously examined WIN compounds. A putative water network at the pocket pore is positioned to hydrogen bond with these four WIN compounds, and this network can account for potency differences seen in structurally similar WIN compounds.

Journal Article↗

PubMed1995

Picornavirus inhibitors: trifluoromethyl substitution provides a global protective effect against hepatic metabolism.

Several modifications of the oxazoline ring of WIN 54954, a broad spectrum antipicornavirus compound, have been prepared in order to address the acid lability and metabolic instability of this compound. We have previously shown that the oxadiazole analogue 3 displayed comparable activity against a variety of rhinoviruses and appeared to be stable to acid. A monkey liver microsomal assay was developed to examine the metabolic stability in vitro of both compounds, and it was determined that WIN 54954 displayed 18 metabolic products while 3 was converted to 8 products. Two major products of 3 were determined by LC-MS/MS to be monohydroxylated at each of the terminal methyl groups. Replacement of the methyl on the isoxazole ring with a trifluoromethyl group, while preventing hydroxylation at this position, did not reduce the sensitivity of the molecule to microsomal metabolism at other sites. However, the (trifluoromethyl)oxadiazole 9 not only prevented hydroxylation at this position but also provided protection at the isoxazole end of the molecule, resulting in only two minor products to the extent of 4%. The major product was identified as the monohydroxylated compound 23. The global metabolic protective effect of trifluoromethyl group on the oxadiazole ring was further demonstrated by examining a variety of analogues including heterocyclic replacements of the isoxazole ring. In each case, the trifluoromethyl analogue displayed a protective effect when compared to the corresponding methyl analogue.

Animals↗

PubMed1995