Sulfanilamide derivatives. VIII. Sulfanilylamidines
Sulfanilamide derivatives. VIII. Sulfanilylamidines
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DOI：
10.1021/ja01264a014
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发表时间：
1942-07-01
影响因子：
15
通讯作者：
Kertesz, DJ
中科院分区：
文献类型：
--
作者：
Northey, EH;Pierce, AE;Kertesz, DJ
大多数新近开发的化疗药物都具有磺胺基环胺的结构。作者准备了。一系列类似的酰胺类化合物。具有熔点的化合物为(S=H_2NC_6H_4SO_2-)：S-乙双胺，熔点151.4-152[度]；二S-乙酰胺，熔点191.6-191.8；S-异丙烷胺，熔点126-127.2；S-a-苯基乙酰胺，熔点177-179；S-苯并肼，210.2-210.7；二S-苯甲胺，熔点206.4-207.6(12月)；S-对甲基苯胺胺，234.9-235.4；二-S-对甲苯胺，熔点166.9-167.5；S-烟肼，熔点208.1-208.2；N-S-N‘’-甲基苯甲酰胺，熔点228.1-229.2；N-S-N‘’-二乙基苯并胺，熔点193.7-194.0；N-S-N‘’-a-吡啶基苯甲胺，熔点206.8-207.5。在初步的化疗研究中，没有一种化合物比磺胺更有活性。
Most recently developed chemotherapeutic agents have the structure of sulfanilyl cyclic amidines. The authors prepd. an analogous series of amidines. Compounds prepd., with melting points, were (S = H2NC6H4SO2-): S-acetamidine, m.p. 151.4-152[degree]; di-S-acetamidine, m.p. 191.6-191.8; S-isocaproamidine, m.p. 126-127.2; S-a-phenylacetamidine, m.p. 177-179; S-benz-amidine, 210.2-210.7; di-S-benzamidine, m.p. 206.4-207.6 (dec); S-p-toluamidine, 234.9-235.4; di-S-p-toluamidine, m.p. 166.9-167.5; S-nicotinamidine, m.p. 208.1-208.2; N-S-N''-methylbenzamidine, m.p. 228.1-229.2; N-S-N''-diethylbenz-amidine, m.p. 193.7-194.0; N-S-N''-a-pyridylbenzamidine, m.p. 206.8-207.5. None of the compounds was more active than sulfanilamide in preliminary chemotherapeutic studies.