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Zusammenfassung
Twenty-four title compds., RCONR1CH2R2 (I, R = Me, Ph, 3- or 4-pyridyl; R1 = H or RR1 = CH2CH2CO; R2 = OH, NMe2, S2CNMe2, NEt2, S2CNEt2, morpholino, morpholinothiocarbonylthio, 4-methyl-1-piperazinyl, and 4-methyl-1-piperazinylthiocarbonylthio), prepd. by known methods from RCONHR1 with HCHO and (or) amine and (or) CS2, showed in vivo carcinostatic and in vitro fungistatic effects, whereas they ...
Zusammenfassung
Twenty-four title compds., RCONR1CH2R2 (I, R = Me, Ph, 3- or 4-pyridyl; R1 = H or RR1 = CH2CH2CO; R2 = OH, NMe2, S2CNMe2, NEt2, S2CNEt2, morpholino, morpholinothiocarbonylthio, 4-methyl-1-piperazinyl, and 4-methyl-1-piperazinylthiocarbonylthio), prepd. by known methods from RCONHR1 with HCHO and (or) amine and (or) CS2, showed in vivo carcinostatic and in vitro fungistatic effects, whereas they were ineffective against gram-pos. and gram-neg. bacteria. Yoshida sarcoma of rats was inhibited by 25-66%. The most effective compd. was N-(hydroxymethyl)acetamide [625-51-4]. The inhibitory effects of I were transitory and ceased after ceasing I administration. The effects of I against fungi increased in the order N-hemiacetal < aminal < ester. Compared with the isosteric beta -amino ketones and dithiourethanes, the fungistatic activity was low.
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