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제목 |
The Chemotherafeutic Effects of the Newly Synthesized Thiocarbanilides on the Drug Resistant Strains of Mycobacterium Tuberculosis in Vitro |
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저자 |
Jae Key Oh., Hyung Ho Yang, and Joon Lew |
소속 |
Department of College of Pharmacy, Chungang University and Microbiology, Yonsei University, College of Medicine, Seoul, Korea |
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년도 |
1967 |
권 |
4 |
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호 |
1 |
번호 |
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시작페이지 |
73 |
끝페이지 |
90 |
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첨부 |
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요약 |
Mycobacterium tuberculosis was discovered by R. Kock in 1882, 10 years later, G. H.
A. Hansen discovered the Mycobacterium leprae which was the first microorganism
known to be pathogenic to the human host.
Brilliant progress has been achieved in the field of tuberculosis, I.e. In it's artificial
culture, animal transmission and chemotherapy, but the progress made in the field of
Mycobacterium leprae is far behind through its discovery proceeded the tubercle bacilli
by 10 years.
Modern chemotherapy in the treatment of tuberculosis was developed in the late
1930's. Meanwhile, Domagk recognized the chemotherapeutic effect of
2',4'-diaminoazobenzene 4-sulfonamide hydrochloride (Prontosil) on mice experimentally
infected with streptococci.
Later, Prontosil failed in the chemotherapy of tuberculosis, the introduction of
Prontosil, however, encouraged workers to produce many sulfonamides and sulfones in
the field of modern chemotherapy.
Thereafter, almost at the same time streptomycin(SM) by Waksman, para
aminosalicylic acid (PAS) by Rosdahl et. Al. And isonicotinic acid hydrazide (INH) were
introduced by the workers at the laboratories of Farbenfabriken Bayer, Hoffman-Roche
and E. R. Squibb and Sons Company.
At the present time SM, PAS and INH used in the treatment of tuberculosis are
considered the most elective drugs and they have become the standard chemotherapeutic
agents for tuberculosis. However, they are not the final drug in the treatment of
tuberculosis ant their affectiveness remains for from satisfactory. Because they requires
a long period of treatment as in the case of almost all antituberculosis drugs their
ultimate value is limited by the development of primary drug-resistant strains in the
treated subjects. And also they have strong toxicity with many side reactions. The
shortage problems and much disatisfaction of the antituberculosis drugs have led
workers to develop new and more effective compounds for the chemotherapeutics of
tuberculosis.
Mayer, Eisman and Konopka developed a series of the derivaties of thiocarbanilides
(diphenyl thiourea) at the laboratories of Ciba Company, and among 295 compounds of
this derivatives 27 compounds demonstrated significant antituberculosis activities in vitro
and in-vivo.
Independently Buu.Hoi and Xuong at the Pasteur Institute reported a series of the
symmetric compounds of thiocarbanilides as effective therapeutic agents for leprosy and
tuberculosis. Among these compounds 4,4'-diethoxy thiocarbanilides (D.E.T.C.) and
4,4'-diisoamyloxythiocarbanilide (D.A.T.C.) have been widely known as therapeutic drugs
for tuberculosis.
Choi et al. reported new compounds of asymmetric thiocarbanilide derivatives in the
experimental studies on tuberculosis and leprosy. Among them
N-(p-ethoxyphenyl)-N'-(thiocyanophenyl) thiocarbamide (LK-59) and N-
(p-ethoxyphenil)-N'-(p-aminodiphynyl) thiocarbamide (LK-65) showed remarkable
antituberculosis effects in-vitro and in-vivo. Kim et al. also reported antifungal activities
of these drugs and Chang et al. reported antimicrobial activities on gram positive and
negative microorganisms.
Attention was paid to the thiocarbanilide derivatives and the author has continued to
study the chemotherapeutic effects of the newly synthesized LK-59 and LK-65 on
Mycobacterium tuberculosis and drug-resistant strains of Mycobacterium tuberculosis.
The results of this study are included in this paper. |
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