1062648-72-9Relevant academic research and scientific papers
Synthesis and biological evaluation of substituted pyrazoles as blockers of divalent metal transporter 1 (DMT1)
Cadieux, Jay A.,Zhang, Zaihui,Mattice, Maryanne,Brownlie-Cutts, Alison,Fu, Jianmin,Ratkay, Laszlo G.,Kwan, Rainbow,Thompson, Jay,Sanghara, Joseph,Zhong, Jing,Goldberg, Y. Paul
, p. 90 - 95 (2012/02/16)
Three distinct series of substituted pyrazole blockers of divalent metal transporter 1 (DMT1) were elaborated from the high-throughput screening pyrazolone hit 1. Preliminary hit-to-lead efforts revealed a preference for electron-withdrawing substituents in the 4-amido-5-hydroxypyrazole series 6a-l. In turn, this preference was more pronounced in a series of 4-aryl-5- hydroxypyrazoles 8a-j. The representative analogs 6f and 12f were found to be efficacious in a rodent model of acute iron hyperabsorption. These three series represent promising starting points for lead optimization efforts aimed at the discovery of DMT1 blockers as iron overload therapeutics.
DIHYDROINDAZOLE COMPOUNDS USEFUL IN TREATING IRON DISORDERS
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Page/Page column 27, (2008/12/08)
This invention is directed to compounds of formula (I): wherein m, R1, R2, R3 and R4 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable s
