5843-45-8Relevant academic research and scientific papers
Convenient One-Pot Two-Step Synthesis of Symmetrical and Unsymmetrical Diacyl Ureas, Acyl Urea/Carbamate/Thiocarbamate Derivatives, and Related Compounds
Hernandez, Anolan Garcia,Grooms, Gregory M.,El-Alfy, Abir T.,Stec, Jozef
, p. 2163 - 2176 (2017/05/05)
A wide range of chemicals such as amides, hydrazides, amines, alcohols, carbazate, and sulfonate were reacted with acyl isocyanates generated by the reaction of primary amides with oxalyl chloride to give symmetrical and unsymmetrical diacyl urea derivatives, acyl ureas/carbamates/thiocarbamates, and related compounds. This method provides means for convenient one-pot, two-step synthesis of compounds bearing urea, carbamate, and other functional groups from cheap and commercially available starting reagents. It is expected that the results presented in this report will expand the medicinal chemist’s toolbox.
Synthesis and antitumor activity of novel N-benzoyl-N'-substituted pyrimidinyl (thio)semicarbazide derivatives
Song, Gaopeng,Li, Jianzuo,Tian, Hao,Li, Yasheng,Hu, Dekun,Li, Ying,Cui, Zining
, p. 329 - 334 (2016/04/04)
A series of substituted pyrimidinyl (thio)semicarbazide derivatives were designed and synthesized. The antitumor results showed that the activity of thiosemicarbazide compounds (series II) was generally higher than that of the corresponding semicarbazide derivatives (series I). Among them, IIk displayed higher cytotoxicity against HL-60, BGC-823 and Bel-7402 than that of adriamycin and exhibited broad in vitro cytotoxicity against 13 human tumor cell lines. Meanwhile, the cytotoxic selectivity and anti-multidrug resistance were evaluated, and IIk exhibited selective cytotoxicity against cancer cells in comparison to human normal cells and had significant anti-multidrug resistance capability. The bioassay results showed that IIk showed great promise as a potent lead compound for further antitumor discovery.
Design, synthesis and fungicidal activity of N-substituted benzoyl-1,2,3,4-tetrahydroquinolyl-1-carboxamide
Lei, Peng,Xu, Yan,Du, Juan,Yang, Xin-Ling,Yuan, Hui-Zhu,Xu, Gao-Fei,Ling, Yun
supporting information, p. 2544 - 2546 (2016/07/07)
To find a new lead compound with high biological activity, a series of N-substituted benzoyl-1,2,3,4-tetrahydroquinolyl-1-carboxamide were designed using linking active substructures method. The target compounds were synthesized from substituted benzoic acid by four steps and their structures were confirmed by 1H NMR, IR spectrum and elemental analysis. The in vitro bioassay results indicated that some target compounds exhibited excellent fungicidal activities, and the position of the substituents played an important role in fungicidal activities. Especially, compound 5n, exhibited better fungicidal activities than the commercial fungicide flutolanil against two tested fungi Valsa Mali and Sclerotinia sclerotiorum, with EC50 values of 3.44 and 2.63 mg/L, respectively. And it also displayed good in vivo fungicidal activity against S. sclerotiorum with the EC50 value of 29.52 mg/L.
Synthesis, structure and biological activity of some new aroylurea derivatives containing 1,3,4-thiadiazole
Song, Xin-Jian,Tan, Xiao-Hong
experimental part, p. 1755 - 1765 (2009/08/15)
In an extensive search for biologically active aroylurea compounds as plant growth regulators, a series of new N-aroyl-N′-[5-(E)-styryl-1,3,4- thiadiazol-2-yl]ureas have been designed and synthesized. Their structures were characterized by IR, 1H NMR, MS, elemental analysis, and single-crystal X-ray diffraction techniques. The preliminary bioassay showed that some of the title compounds exhibited good plant-growth regulating activity. Copyright Taylor & Francis Group, LLC.
Novel antagonists of the 5-HT3 receptor. Synthesis and structure-activity relationships of (2-alkoxybenzoyl)ureas
Bradley,Ward,White,Coleman,Taylor,Rhodes
, p. 1515 - 1520 (2007/10/02)
A series of benzoylureas derived from bicycle amines were prepared and evaluated for 5-HT3 antagonist activity on the rat isolated vagus nerve. From among these compounds, those analogues which were ortho substituted by an alkoxy group on the b
Heterocyclic compounds useful as 5-HT3 antagonists
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, (2008/06/13)
Aroyl ureas and carbamic acid derivatives of formula and pharmaceutically acceptable salts thereof wherein A is a specified aromatic radical including optionally substituted phenyl W is O or S Y is NH or S and B is a specified saturated azacyclic ring, eg tropan-3-yl or quinuclidin-3-yl, possess 5-HT3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.
