Uridine phosphorylase inhibitors: chemical modification of benzyloxybenzyl-barbituric acid and its effects on urdpase inhibition.

5-(o-Benzyloxy)benzylbarbituric acid (6) and 5-(p-benzyloxy)benzylbarbituric acid (7) were prepared and their inhibitory activities compared to 5-(m-benzyloxy)-benzylbarbituric acid (BBB) a known, potent inhibitor of uridine phosphorylase (UrdPase). Compounds 6 and 7 were 18-fold and 51-fold less active, respectively, than BBB in inhibiting UrdPase. These data provide solid evidence that the 5-benzylbarbituric acids possessing meta substituents are the most active inhibitors. In addition, 2-thioBBB (11) was synthesized and it was shown to be as active an inhibitor as BBB.

[Undesirable dermatologic results of drugs. Result of a drug monitoring survey]. / Conséquences dermatologiques indésirables des médicaments. Résultat d'une enquête de pharmacovigilance.

A prospective survey of drug-induced diseases has been performed along a one year period in a department of dermatology. Among the 550 patients hospitalized during this period for a cutaneomucous event, a drug-induced disease is pointed out in 30 of them (5.6 p. cent). The use of algorithm allows the establishment of the cause-effect relationship; the relative value of literature data and the role of three main predisposing factors (age, allergic antecedents, polymedication) are insisted upon. Three categories of drugs are primarily implicated: cardiovascular, antiinflammatory and antiinfectious drugs. The most commonly observed events are erythrodermia and allergic phenomena. If favorable evolution is usual, one fatal adverse drug reaction is firmly established in our series. Such a survey would lead to preventive attitudes.

[Acquired angioneurotic edema caused by acquired deficiency of C1 esterase inhibitor disclosing lymphoproliferative syndrome. Apropos of a case, review of the literature]. / Oedème angio-neurotique (acquis) par déficit acquis en inhibiteur de Ci-estérase révélateur d'un syndrome lympho-prolifératif. A propos d'un cas, revue de la littérature.

One case of acquired angio-neurotic oedema is described and discussed with the other cases recorded in literature since Caldwell's one in 1972. This entity is characterized by: --the late onset of angio-oedema but its presence only in about half cases, --a complement deficiency resulting from the lack of C1-esterase inhibitor, --the absence of familial identical cases, --the great frequency of associated illnesses overall lympho-proliferative diseases, --the therapeutic response to either etiologic treatment of the associated disease or to the symptomatic effect of drugs used in hereditary angio-neurotic oedema.