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Chemotherapy of Leprosy with Newly Synthesized Thiocarbanilides

Yonsei Medical Journal 1966년 7권 1호 p.52 ~ 57
 ( Lew Joon ) - 연세대학교 의과대학 미생물학교실

 ( Chang Chai-Hoon ) - 연세대학교 의과대학 미생물학교실
 ( Choi Tae-Kyung ) - 연세대학교 의과대학 미생물학교실

Abstract


Attention has been paid to the thiocarbanilide derivative and the authors synthesized some new compounds of thiocarbanilides for experimental studies on tuberculosis and leprosy.

The series of newly synthesized chemical compounds of thiocarbanilides were studied for comparision with the already known antimycobacterial agents; INH, PAS, Streptomycin and D. D. S. The strains of Mycobacterium tubercubsis (H37 Rv, Ravenel, and B. C. G.) and Mycobacterium phlei were used for the in vitro experiments. In the in vivo experiments, the strain of Mycobacterium tuberculosis var. bovis (Ravenel) was employed.

The strain of Mycobacterium leprae murium (Hawaiian strain) was used for the murine leprosy experiments.

The experimental animals for the in vivo tests were white mice (CFW strain) and these were extensively employed in tuberculosis and leprosy as well. Sixteen cases of Various types of human leprosy, were treated with one of the newly synthesized thiocarbanilides (L-4).

Among the newly synthesized chemical compounds of thiocarbanilides studied for their antituberculous and antimurine leprosy activity in vitro and in vivo experiments, two compounds were shown to be suppressive agents for those infections without significant toxicity. These two compounds were named tentatively as L-1 and L-4.


1) LD50 of L-1 was 1,054 mg/kg and that of L-4 was 1,028 mg/kg, while the LD50 of INH was 650 mg/kg and PAS was 4,000mg/kg orally in the experimental animals.

2) L-1 and L-4 showed remarkable suppressive activity in vitro using solid media with 100r/ml. concentration. These data were parallel to 1r/ml. of INH and 50r/ml. of PAS. The inferiority of L-1 and L-4 to INH and PAS in vitro studies might have been due to the water insolubility of these compounds while INH and PAS were readily soluble in water.

3) In vivo experiments with L-1 showed a much-more superior antituberculous effect than was found with INH and PAS.

4) A method of grading the bacterial count in a homogenized tissue suspension of visceral organs (lungs, liver, spleen and kidneys) using the simple technique of the Gaffky scale was accurate and time saving technique in screening the results of the chemotherapeutic agents in tuberculosis.

5) Among the newly synthesized compounds L-4 showed the most remarkable suppressive effect on murine leprosy. The suppressive results were similar to those of INH.

6) The method of measuring the size and the weight of leproma at the inoculated site was simple and is an adequate screening test for chemotherapeutic effect in murine leprosy.

7) In the trials with human leprosy 16 cases of various types, using L-4, the effectiveness in clinical as well as in bacteriological improvement was remarkable.

a) After L-4 treatment decrease in bactriologica1 indices and remarkable clinical improvement after a relative1y short period of treatment were observed.

b) L-4, up to the maximum daily dose of 500 mg, can be safely administered orally to the patients without any significant side reactions.

c) L-4 could be used with remarkable clinical improvement for the patients in lepra reactions.

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