- Antibacterial barbituric acid analogues inspired from natural 3-acyltetramic acids; Synthesis, tautomerism and structure and physicochemical property-antibacterial activity relationships
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The synthesis, tautomerism and antibacterial activity of novel barbiturates is reported. In particular, 3-acyl and 3-carboxamidobarbiturates exhibited antibacterial activity, against susceptible and some resistant Gram-positive strains of particular inter
- Jeong, Yong-Chul,Moloney, Mark G.
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- Identification of a pyrimidinetrione derivative as the potent DprE1 inhibitor by structure-based virtual ligand screening
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Despite the increasing need of new antituberculosis drugs, the number of agents approved for the market has fallen to an all-time low. In response to the emerging drug resistance followed, structurally unique chemical entities will be highlighted. decaprenylphosphoryl-β-D-ribose oxidase (DprE1) participating in the biosynthesis of mycobacterium cell wall is a highly vulnerable and validated antituberculosis target. On the basis of it, a systematic strategy was applied to identify a high-quality lead compound (compound 50) that inhibits the essential enzyme DprE1, thus blocking the synthesis of the mycobacterial cell wall to kill M. tuberculosis in vitro and in vivo. Correspondingly, the rational design and synthetic strategy for compound 50 was reported. Notably, the compound 50 has been confirmed to be no toxicity. Altogether, our data suggest the compound 50 targeting DprE1 is a promising candidate for the tuberculosis (TB) therapy.
- Gao, Ya,Xie, Jinshan,Tang, Ruotian,Yang, Kaiyin,Zhang, Yahan,Chen, Lixia,Li, Hua
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- SUBSTITUTED HYDRAZIDE COMPOUNDS AND USE THEREOF
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The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R have the same meanings as given in the Description. The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.
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Page/Page column 14
(2012/06/16)
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- SUBSTITUTED HYDRAZIDE COMPOUNDS AND APPLICATION THEREOF
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The invention relates to substituted hydrazide compounds as shown by general formula I, including geometrical isomers, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof, and use of the same, wherein the substitutents Ar and R having the same meanings as given in the Description. T The invention further relates to the use of compounds of general formula I in the preparation of medicament for the treatment and/or prevention of cancer and other proliferative diseases.
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Page/Page column 16
(2012/07/03)
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- Identification of 1-arylmethyl-3-(2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists
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Based on SAR from bicyclic GnRH antagonists such as 6-aminomethyl-7-arylpyrrolo[1,2-a]pyrimid-4-ones (1) and 2-aryl-3-aminomethylimidazolo[1,2-a]pyrimid-5-ones (2a,b), a series of novel uracil compounds (4) were derived as the GnRH antagonists. Their synt
- Zhu, Yun-Fei,Gross, Timothy D.,Guo, Zhiqiang,Connors Jr., Patrick J.,Gao, Yinghong,Tucci, Fabio C.,Struthers, R. Scott,Reinhart, Greg J.,Saunders, John,Chen, Ta Kung,Killam Bonneville, Anne L.,Chen, Chen
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p. 2023 - 2026
(2007/10/03)
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