Biomedical subjects
Publications and source records attributed to W R Williamson.
The synthesis and biological properties of 85 benzophenones and related compounds are described. The majority of the compounds inhibit the release of leukotrienes (LT) C4 and D4 in vitro from sensitized guinea pig chopped lung. In addition, some of the compounds inhibited the release of LTs from passively sensitized human chopped lung and protected guinea pigs from the effects of anaphylaxis in a modified Herxheimer test.
A large series of N-arylanthranilic acids has been prepared. Many of these compounds show high anti-inflammatory activity as measured by the anti-UV-erythema test. From this series have come the clinically useful non-steroidal anti-inflammatory agents, flufenamic acid (Arlef), mefenamic acid (Ponstel), and the latest and most potent agent, N-(2,6-dichloro-m-tolyl)anthranilic acid (meclofenamic acid, Meclomen = the sodium salt). The structure-activity relationships of this series is discussed and a graphical representation is presented which allows the prediction of activity of new agents.
The syntheses of a number of amines and their derivatives, based on the phenylpiperidine nucleus, are described. Their activities on the rat paw carrageenan test are also reported. Activities comparable to that of phenylbutazone were obtained for some of the amines, notably 4-piperidino-beta-methylphenethylamine.
Compounds having acenaphthene and indan as their parent nuclei were synthesized for antiinflammatory testing. Compounds which showed activity were 1-phenyl-5-acenaphthenylacetic acid and its alpha-methyl derivative (carrageenan rat paw edema) and the same alpha-methylacenaphthenylacetic acid and 2-(4-chlorobenzylidene)-3-oxo-5-indanacetic acid and its alpha-methyl derivative (rat adjuvant arthritis). None of the compounds was more active than the control compounds phenylbutazone and indomethacin.
A number of 1,2-benzisoxazoles, substituted in the 3 position with 4-substituted phenyl groups and in the 5--7 positions with acetic and propionic acid residues, have been synthesized and tested in the rat carrageenan foot edema assay. Activity has been found in the 6- and 7-substituted acids.
4- and 7-benzoxazoleacetic and alpha-methylacetic acids substituted in the 2 position with phenyl and substituted phenyl groups have been synthesized and tested on the carrageenan-induced rat paw edema assay. The only compound found to have significant activity, albeit of a low order, was 2-phenyl-alpha-methyl-7-benzoxazoleacetic acid.
Trabeculectomy with cautery was performed on 31 eyes of of 25 glaucoma patients uncontrolled on maximal medical therapy. The procedure was designed to combine the effectiveness of Scheie's thermal sclerostomy with the low incidence of complications associated with trabeculectomy. There was an 81 percent success rate overall and an 83 percent success rate in blacks. Average follow-up was 25 months. The average preoperative pressure was 29 mm Hg and the average postoperative pressure was 11 mm Hg. Immediate postoperative complications were minimal. The most serious long-term problem was the acceleration of lenticular changes. The procedure is technically simple with a majority of cases being performed by house staff at a relatively early stage of training. It is believed that trabeculectomy with cautery is indicated in blacks, in far-advanced glaucoma cases, and in patients in whom a conventional trabeculectomy has failed.
The synthesis of alpha-methyl-5-benzimidazoleacetic acid (17), its 2-amino, 2-phenyl, 2-(4-chlorophenyl), and 2-(4-chlorophenyl)-1-methyl derivatives (18,4,3, and 5, respectively), and alpha-methyl-2-oxo-2,3-dihydro-5-benzimidazoleacetic acid (19) is described. None of the compounds were effective in reducing carrageenan-induced edema in rat paws.
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