208396-72-9Relevant academic research and scientific papers
Novel 1-acyl-4-substituted semicarbazide derivatives of primaquine-synthesis, cytostatic, antiviral and antioxidative studies
Perkovic, Ivana,Trsinar, Sara,Zanetic, Jelena,Kralj, Marijeta,Martin-Kleiner, Irena,Balzarini, Jan,Hadjipavlou-Litina, Dimitra,Katsori, Anna Maria,Zorc, Branka
, p. 601 - 610 (2013/05/22)
A series of novel 1,4-substituted semicarbazides 5a-g with a primaquine moiety bridged by a carbonyl group at position 1 and a cycloalkyl, aryl, benzyloxy or hydroxy substituent at position 4 were prepared and biologically evaluated. The synthetic pathway
Semicarbazone-based inhibitors of cathepsin K, are they prodrugs for aldehyde inhibitors?
Adkison, Kim K.,Barrett, David G.,Deaton, David N.,Gampe, Robert T.,Hassell, Anne M.,Long, Stacey T.,McFadyen, Robert B.,Miller, Aaron B.,Miller, Larry R.,Payne, J. Alan,Shewchuk, Lisa M.,Wells-Knecht, Kevin J.,Willard Jr., Derril H.,Wright, Lois L.
, p. 978 - 983 (2007/10/03)
Starting from potent aldehyde inhibitors with poor drug properties, derivatization to semicarbazones led to the identification of a series of semicarbazone-based cathepsin K inhibitors with greater solubility and better pharmacokinetic profiles than their parent aldehydes. Furthermore, a representative semicarbazone inhibitor attenuated bone resorption in an ex vivo rat calvarial bone resorption model. However, based on enzyme inhibition comparisons at neutral pH, semicarbazone hydrolysis rates, and 13C NMR experiments, these semicarbazones probably function as prodrugs of aldehydes.
Synthesis and anti-trypanosomal activity of novel 5-nitro-2-furaldehyde and 5-nitrothiophene-2-carboxaldehyde semicarbazone derivatives
Cerecetto, Hugo,Di Maio, Rossanna,Ibarruri, Gerardo,Seoane, Gustavo,Denicola, Ana,Peluffo, Gonzalo,Quijano, Celia,Paulino, Margot
, p. 89 - 94 (2007/10/03)
Several novel semicarbazones derivatives were prepared from 5-nitro-2-furaldehyde or 5-nitrothiophene-2-carboxaldehyde, and tested in vitro as potential anti-trypanosomal agents. The compounds were prepared in good to excellent yields in 2-3 steps from readily available starting materials. Some derivatives were found to be active against Trypanosoma cruzi with an activity similar to that of Nifurtimox.
