A total of 62 leprosy patients, 47 lepromatous type, 9 tuberculoid, 5 borderline group and 1 indeterminate group, have been treated with a synthesized thiocarbanilide L-4, and the effectiveness of L-4 administration in the treatment of leprosy is evaluated on the basis of clinical and bacteriological improvements. The results are summarized and conc1uded as follows; 1. L-4, contained in gelatin capsule, can be safely administered orally to the patients through slow induction, from initial dosages of 50 mg to 100 mg dai1y to the therapeutic maintenance levels of 200 mg to 300 mg daily, for a period of time. 2. L-4 administration has brought apparent and remarkable improvement in clinical symptoms of the patients after a relatively short period of medication compared with that of DDS administration. 3. Changes of SFG values caused by L-4 administration were much speedier than, (or, at least, equivalent to) the effect caused by DDS. The changes of SFG values, in general, synchronized fairly well with clinical improvement of the patients. 4. Lepromatous cases with leprosy reaction or sulfone allergy responded well to L-4 medication with remarkable clinical improvement, and prolonged administration of L-4 did not provoke such a precipitating action to leprosy reaction as did DDS.
Adolescent ; Adult ; Anilides/chemical synthesis ; Anilides/therapeutic use* ; Anti-Infective Agents/chemical synthesis ; Anti-Infective Agents/therapeutic use* ; Child ; Female ; Human ; Leprosy/drug therapy* ; Male ; Middle Age ; Sulfur*

AIMTo synthesize novel derivatives of hydroxylbenzenedisulfonanilide with high insecticidal activity against the Fasciola hepatica.

METHODSo-(m-, p-) Chlorphenol were used to synthesize the title compounds by sulphonation and nucleiphilic-substitution reaction. The uncoupling activity (insecticidal activity) of these compounds were tested by determining the influence on mitochondrial respiration control ratio (RCR) and the variation of inorganic phosphate in oxidative phosphorylation (delta Pi).

RESULTSCompounds 1-14 are new compounds. The structures of the compounds were determined by IR, HNMR and elemental analysis. Most new compounds have relatively high uncoupling activities, especially compounds 3, 5, 6 and 9.

CONCLUSIONCompounds 3, 5, 6 and 9 will become novel fasciolicides and are worth further studying.

Anilides ; chemical synthesis ; chemistry ; pharmacology ; Animals ; Anthelmintics ; chemical synthesis ; chemistry ; pharmacology ; Fasciola hepatica ; drug effects ; Mitochondria, Liver ; physiology ; Molecular Structure ; Oxygen Consumption ; drug effects ; Sulfonamides ; chemical synthesis ; chemistry ; pharmacology