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N-monosubstituted thiosemicarbazide as novel Ure inhibitors: synthesis, biological evaluation and molecular docking.
Ni, Wei-Wei; Fang, Hai-Lian; Ye, Ya-Xi; Li, Wei-Yi; Yuan, Chu-Ping; Li, Dong-Dong; Mao, Shi-Jia; Li, Su-E; Zhu, Qi-Hui; Ouyang, Hui; Xiao, Zhu-Ping; Zhu, Hai-Liang.
Afiliación
  • Ni WW; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Fang HL; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Ye YX; State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, 210093, PR China.
  • Li WY; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Yuan CP; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Li DD; College of Chemical Engineering, Nanjing Forestry University, 159 Long Pan Road, Nanjing, 210037, China.
  • Mao SJ; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Li SE; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Zhu QH; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Ouyang H; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Xiao ZP; National Demonstration Center for Experimental Chemistry Education, Hunan Engineering Laboratory for Analyse & Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou, 416000, PR China.
  • Zhu HL; State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, 210093, PR China.
Future Med Chem ; 12(18): 1633-1645, 2020 09.
Article en En | MEDLINE | ID: mdl-32892642
Background: Identification of novel Ure inhibitors with high potency has received considerable attention. Methodology & results: Ure inhibition was determined using the indophenol method, the affinities to Ure were estimated via surface plasmon resonance. Seventeen new plus ten known N-monosubstituted thiosemicarbazides were synthesized and identified as novel Ure inhibitors. Out of these compounds, compound b5 shows excellent activity against both crude Ure from Helicobacter pylori (IC50 = 0.04 µM) and Ure in living cell (IC50 = 0.27 µM), with the potency being over 600-fold higher than clinical used drug acetohyroxamic acid, respectively. Surface plasmon resonance demonstrated the high affinity (Kd.#x00A0;= 6.32 nM) of b5 to Ure. Conclusion: This work provides a class of novel and promising Ure inhibitors.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Semicarbacidas / Helicobacter pylori / Factores de Virulencia / Antibacterianos Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Future Med Chem Año: 2020 Tipo del documento: Article Pais de publicación: Reino Unido
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Semicarbacidas / Helicobacter pylori / Factores de Virulencia / Antibacterianos Tipo de estudio: Prognostic_studies Límite: Humans Idioma: En Revista: Future Med Chem Año: 2020 Tipo del documento: Article Pais de publicación: Reino Unido