60295-21-8Relevant articles and documents
Tetraoxane-pyrimidine nitrile hybrids as dual stage antimalarials
Oliveira, Rudi,Guedes, Rita C.,Meireles, Patrícia,Albuquerque, Inês S.,Gon?alves, Lídia M.,Pires, Elisabete,Bronze, Maria Rosário,Gut, Jiri,Rosenthal, Philip J.,Prudêncio, Miguel,Moreira, Rui,O'Neill, Paul M.,Lopes, Francisca
, p. 4916 - 4923 (2014)
The use of artemisinin or other endoperoxides in combination with other drugs is a strategy to prevent development of resistant strains of Plasmodium parasites. Our previous work demonstrated that hybrid compounds, comprising endoperoxides and vinyl sulfones, were capable of high activity profiles comparable to artemisinin and chloroquine while acting through two distinct mechanisms of action: oxidative stress and falcipain inhibition. In this study, we adapted this approach to a novel class of falcipain inhibitors: peptidomimetic pyrimidine nitriles. Pyrimidine tetraoxane hybrids displayed potent nanomolar activity against three strains of Plasmodium falciparum and falcipain-2, combined with low cytotoxicity. In vivo, a decrease in parasitemia and an increase in survival of mice infected with Plasmodium berghei was observed when compared to control. All tested compounds combined good blood stage activity with significant effects on liver stage parasitemia, a most welcome feature for any new class of antimalarial drug.
Synthesis of Hydrazines via Radical Generation and Addition of Azocarboxylic tert -Butyl Esters
Ru, Chen-Hao,Guo, Shi-Huan,Pan, Gao-Fei,Zhu, Xue-Qing,Gao, Ya-Ru,Wang, Yong-Qiang
supporting information, p. 1910 - 1913 (2018/04/16)
A new chemistry of azo compounds that is a radical generation and addition in situ of azocarboxylic tert-butyl esters to synthesize hydrazines has been described. The protocol provides a novel strategy for the synthesis of various hydrazines. The advantag
INHIBITORS OF BRUTON'S TYROSINE KINASE
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, (2014/06/23)
The invention provides novel poly-substituted 5-membered heterocyclic compounds represented by Formula (IV), or a pharmaceutically acceptable salt, solvate, metabolites, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as selective irreversible bruton's tyrosine kinase (Btk) inhibitors and is further useful to treat inflammatory, auto immune diseases associated with aberrant B-cell proliferation such as RA (rheumatoid arthritis) and cancers. This invention also provided the preparation of a medicament using of Formula (IV), and methods of preventing or treating diseases associated with excessive Btk activity in mammals, especially humans. Formula (IV)
