36823-82-2Relevant articles and documents
Design and synthesis of N-(3-sulfamoylphenyl)amides as Trypanosoma brucei leucyl-tRNA synthetase inhibitors
Li, Zezhong,Xin, Weixiang,Wang, Qing,Zhu, Mingyan,Zhou, Huchen
, (2021/03/16)
The protozoan parasite Trypanosoma brucei (T. brucei) causes human African trypanosomiasis (HAT), which is a fatal and neglected disease in the tropic areas, and new treatments are urgently needed. Leucyl-tRNA synthetase (LeuRS) is an attractive target for the development of antimicrobial agents. In this work, starting from the hit compound thiourea ZCL539, we designed and synthesized a series of amides as effective T. brucei LeuRS (TbLeuRS) synthetic site inhibitors. The most potent compounds 74 and 91 showed IC50 of 0.24 and 0.25 μM, which were about 700-fold more potent than the starting hit compound. The structure-activity relationship was also discussed. These compounds provided a new scaffold and lead compounds for further development of antitrypanosomal agents.
Novel domino synthesis of 2-(2,3.4-substituted phenyl) quinazolin-4-amine
Ali, Ibrahim A. I.,El Rayes, Samir M.,Fathalla, Walid,Khalifa, Mohamed E.,Pazdera, Pavel
, (2022/01/13)
Convenient domino protocol was developed for the synthesis of 2-arylquinazolin-4-amines by the reaction of N-(2-cyanophenyl) substituted benzimidoyl isothiocyanates with isopropyl amine. The major advantages of this protocol are short reaction times, mild conditions, simple work up, high yields, and pure products. The efficacy of this protocol owes to the competence of synthesis, pure isolation of imidoyl isothiocyanates, and the unique structure conformation of the corresponding intermediate thiourea derivatives.
Small-Molecule Choline Kinase Inhibitors as Anti-Cancer Therapeutics
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Page/Page column 18; 27-28, (2011/10/31)
Small molecule choline kinase inhibitors having the following formula: are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting choline kinase enzymatic activity, and methods of treating tumors by administering an effective amount of a Formula I compound.