Your browser doesn't support javascript.
loading
Hydrophobicity-oriented drug design (HODD) of new human 4-hydroxyphenylpyruvate dioxygenase inhibitors.
Ndikuryayo, Ferdinand; Kang, Wei-Ming; Wu, Feng-Xu; Yang, Wen-Chao; Yang, Guang-Fu.
Affiliation
  • Ndikuryayo F; Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, Chemical Biology Center, College of Chemistry, Central China Normal University, Wuhan, 430079, PR China.
  • Kang WM; Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, Chemical Biology Center, College of Chemistry, Central China Normal University, Wuhan, 430079, PR China.
  • Wu FX; Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, Chemical Biology Center, College of Chemistry, Central China Normal University, Wuhan, 430079, PR China.
  • Yang WC; Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, Chemical Biology Center, College of Chemistry, Central China Normal University, Wuhan, 430079, PR China. Electronic address: tomyang@mail.
  • Yang GF; Key Laboratory of Pesticide & Chemical Biology of Ministry of Education, International Joint Research Center for Intelligent Biosensor Technology and Health, Chemical Biology Center, College of Chemistry, Central China Normal University, Wuhan, 430079, PR China; Collaborative Innovation Center o
Eur J Med Chem ; 166: 22-31, 2019 Mar 15.
Article in En | MEDLINE | ID: mdl-30684868
ABSTRACT
Involved in the tyrosine degradation pathway, 4-hydroxyphenylpyruvate dioxygenase (HPPD) is an important target for treating type I tyrosinemia. To discover novel HPPD inhibitors, we proposed a hydrophobicity-oriented drug design (HODD) strategy based on the interactions between HPPD and the commercial drug NTBC. Most of the new compounds showed improved activity, compound d23 being the most active candidate (IC50 = 0.047 µM) with about 2-fold more potent than NTBC (IC50 = 0.085 µM). Therefore, compound d23 is a potential drug candidate to treat type I tyrosinemia.
Subject(s)
Key words
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Drug Design / Cyclohexanones / Enzyme Inhibitors / 4-Hydroxyphenylpyruvate Dioxygenase / Nitrobenzoates Limits: Humans Language: En Journal: Eur J Med Chem Year: 2019 Document type: Article
Fulltext
Add to My VHL
Print
XML
PubMed Links
Search on Google

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Drug Design / Cyclohexanones / Enzyme Inhibitors / 4-Hydroxyphenylpyruvate Dioxygenase / Nitrobenzoates Limits: Humans Language: En Journal: Eur J Med Chem Year: 2019 Document type: Article