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KMID : 0386319680050010025
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Korean Leprosy Bulletin
1968 Volume.5 No. 1 p.25 ~ p.44
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Studies on the Treatment of Leprosy With a Synthesized Thiocarbanilide Derivative L-4
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柳駿/Lew, Joon
張在薰/崔大卿/Chang, Chai Hoon/Choi, Tae Kyung
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Abstract
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Introduction
Though Chaulmoogra oil (Mouat 1854) had been used empirically in the treatment of leprosy from the ancient time, the very beginning of modern chemotherapy of leprosy
was initiated by the work of Faget et al. (1943) who originated the Promin treatment of leprosy. Promin was a less toxic derivative of the parent sulphone, ie., DDS (Diaminodiphenyl sulphone) which was synthesized by Fromm and Whittmann (1908). However, Promin itself was too toxic to be given orally or subcutaneously, and therefore, it had only to be given intravenously. By the introduction of other derivatives. of DDS such as Sulfoxone sodium, U.S.P. (Diasone sodium), Solapsone, B.P. (Sulphetrone), Acetosulphone (Promacetin) and Thiazolsulphone that could be given orally in similar doses with safety, Promin was eventually replaced by those drugs.
Meanwhile, the pioneering works done by Cochrane et al. (1949), Lowe and Smith (1949) and Lowe (1950) firmly established that DDS, the parent sulphone of those derivatives, did possess activity against Mycobacteria, and DDS has become the choice of drug in the treatment of leprosy since then on.
Today, it- is well recognized that DDS is the drug having the virtues of low cost,. general efficacy, suitability of outpatient treatment, rarity of drug resistance, and its prophylactic effectiveness. However, as Davey (1964) pointed out, DDS has still many limitations such as 1) its rather strong toxicity,. 2) the existence of idiosyncrasy, 3) the precipitation of hypersensitive state, 4) the development of leprosy reactions, 5) the prolonged time of medication, 6) occasional occurrence of non-responding patients and etc. Those limitations of DDS indicate that it could not be a sole and the most ideal antileprosy chemotherapeutic.
Efforts (Buu-Hoi 1954, 1955a, 1955b, Buu-Hoi et al. 1955a, Buu-Hoi et al. 1955b, Buu-Hoi et al. 1955c, Mayer 1941, 1954, Mayer et al. 1953, Mayer et al. 1959) have been made to produce alternative, ideal drugs that would exert lesser toxicity, speedier action and smoother progress during the treatment in addition to the virtues of DDS. Following representatives of several classes of various organic compounds have been discovered and have been shown. to possess activities against. Mycobacterium leprae at more than one institute throughout the world; Diami￢nodiphenylsulfoxide (Buu-Hoi et al. 1955a) Sulfamethoxypyrazine (Lederkyn; Schneider
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