BENZYLIDENETHIAZOLIDINE-2,4-DIONES SHOWING ANTIMICROBIAL ACTIVITY Russian patent published in 1996 - IPC

Abstract SU 1417436 A1

FIELD: organic chemistry. SUBSTANCE: product: substituted derivatives of thiazolidine, in part, 3-alkoxycarbonyl-5-substituted benzylidenethiazolidine-2,4- dones of the general formula where: R₁-CH₃, R₂-Cl, R₃-H(1); R₁-CH₃, R₂ and R₃-Cl(2); R₁-CH₃, R₃-F; R₃-H,R₁-C₂H₅, R₂-Cl, R₃-H(4),. Synthesis is carried out from the corresponding substituted thiazolidine-2,4-dione and chlorocarbonic acid methyl ester in the presence of triethylamine, in chloroform medium, at 80 C. The yield, %; m.p., C; empirical formula; antifungal activity in vitro, for example, genus Microsporum, antibacterial activity, for example, S. aureus (by maximally tolerated concentration, mcg/ml); therapeutic efficacy (against trichophytosis in guinea pig), % toxicity, mg/kg: 68; 150-151; C₁₂H₈ClNO₄S; 7.8; 31.2; 16.5; 921 (1); 59; 132-134; C₁₂H₇Cl₂NO₄S; 15.6; 7.8; 21.8; 783 (2); 67; 143-144; C₁₂H₈FNO₄S; 15.6; 125; 10; 854 (3); 61; 134-135; C₁₃H₁₀ClNO₄S; 7.8; 125; 51.4; 593 (4). Synthesized compounds show antimicrobial activity and can be used in medicine. EFFECT: increased activity, decreased toxicity. 6 tbl

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SU 1 417 436 A1

Authors

Levshin I.B.

Glushkov R.G.

Silin V.A.

Padejskaja E.N.

Dates

1996-04-27—Published

1986-12-10—Filed