| 摘要 |
<p>Novel 1,2,4-thiadiazole-5-yl disulphide derivs. of formula (I). In formula (I), X is Cl of Br; R' is is not >12C alkyl, is not >12C alkyl which is mono-unsatd. or substd. by COOH and NH2, is not >6C cycloalkyl, phenyl, phenyl mono- or polysubstd. by F, Cl, Br, NO2, is not >4C alkyl, NR2R3, CN, OH, OR4, SR4 and/or SO2R4, benzyl, benzyl mono-or polysubstd. by CH3, F, Cl, NO2, CF3 or CN, or CCl3; R2 and R3 are H, is not >4C alkyl, formyl or acetyl; and R4 is is not >4C alkyl, phenyl, or phenyl substd. by NO2, NH2 or Cl. (I) and their acceptable salts have bacteriostatic and fungistatic activity. For example, 3-chloro-5-(4-nitrophenyldithio)-1,2,4-thiadiazole has outstanding inhibitory activity against filamentous fungi Candida strains and gram-positive and -negative bacteria (including Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Proteus vulgaris). They can also be used as medicaments, esp. for combatting microbial infections. They may also be used as intermediates for further pharmaceuticals. Specific cpds. (I) include 3-chloro-5-(4-nitrophenyldithio)-1,2,4-thiadiazole. In an example, this cpd. is prepd. by dropwise treatment of a solution of sodium 4-nitrothiophenolate in CHCl3 with 3-chloro-1,2,4-thiadiazole-5-sulphenyl chloride, the resulting mixt. being stirred overnight at room temp.</p> |
