Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-Chagas agents

A new series of 4-aminopyridyl-based lead inhibitors targeting Trypanosoma cruzi CYP51 (TcCYP51) has been developed using structure-based drug design as well as structure-property relationship (SPR) analyses. The screening hit starting point, LP10 (K(D) ≤ 42 nM; EC50 of 0.65 µM), has been optimized...

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Hlavní autoři: Choi, Jun Yong, Calvet, Claudia M., Gunatilleke, Shamila S., Ruiz, Claudia, Cameron, Michael D., McKerrow, James H., Podust, Larissa M., Roush, William R.
Médium: Artigo
Jazyk:Inglês
Vydáno: 2013
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On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC3864028/
https://ncbi.nlm.nih.gov/pubmed/24079662
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm401067s
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