Synthesis and Biological Activity of Novel Phosphoramide with Hydantoin

Synthesis and Activity of Novel Acylthiourea with Hydantoin

“…After that, the thiophosphates 2 and phosphoramidates were found to show weak herbicidal activities against Brasica campestris and Echinochloa crus-galli , while one of them exhibited excellent insecticidal activities against Myzus Persicae [ 11 , 12 ]. Then, phosphoramides 3 were further tested and showed increasing herbicidal activities against Brasica campestris as well as insecticidal activities against Myzus Persicae [ 37 ]. These results indicated that 5-(4-aminophenyl)-hydantoin, 5-(4-aminobenzyl)-hydantoin and 5-(4-aminobenzyl)-thiohydantoin were important moiety for these active compounds.…”

“…The synthesis of the intermediates 4 , 5 and 6 were carried out according to the protocols in our previous paper and their spectral data were identical with that in the reference [ 37 ]. To a suspension of benzoic acid derivative (20 mmol) in 25 mL of CH 2 Cl 2 in a 50 mL three-necked flask, 8 mL SOCl 2 and a drop of N , N -dimethylformamide (DMF) were added.…”

Synthesis, Insecticidal Activity of New Benzoylthioureas and Benzoylureas

“…, 但是迄今未见他人将 2,4-咪唑啉二酮杂环引入 到苯环上合成酰基硫脲及酰基脲的报道．本课题组在研 究含 2,4-咪唑啉二酮杂环化合物中, 发现合成的一些磷 酰胺和磷酰胺酯类化合物表现出较好的杀虫活性 [9,10] , 因此本文作者根据活性亚结构拼接原理希望将 2,4-咪唑 啉二酮活性结构片段引入到具有优异杀虫、杀菌、除草 等活性的酰基硫脲及酰基脲结构中(Scheme 1), 以进一 步观测 2,4-咪唑啉二酮杂环对酰基硫脲及酰基脲类化合 物生物活性的影响, 在前文中我们已经报道了一类新的 含 2,4-咪唑啉二酮杂环酰基硫脲的合成及生物活性, 发 现部分化合物表现出优异的除草活性, 但是整体化合物 杀菌活性很差 [11] , 本文继续报道含 2,4-咪唑啉二酮杂环…”

Application of “Hydrogen-Bonding Interaction” in Drug Design. Part 2: Design, Synthesis, and Structure–Activity Relationships of Thiophosphoramide Derivatives as Novel Antiviral and Antifungal Agents

“…Phosphoramides and their ester derivatives possess a wide range of biological activities, such as pesticidal activity, antiviral activity, herbicidal activity, etc. − Several phosphoramides have become commercial varieties, such as acephate, cyclophosphamide, methamidophos, etc.…”