59211-76-6Relevant articles and documents
A minimalistic approach to develop new anti-apicomplexa polyamines analogs
Panozzo-Zénere, Esteban A.,Porta, Exequiel O.J.,Arrizabalaga, Gustavo,Fargnoli, Lucía,Khan, Shabana I.,Tekwani, Babu L.,Labadie, Guillermo R.
, p. 866 - 880 (2017/12/13)
The development of new chemical entities against the major diseases caused by parasites is highly desired. A library of thirty diamines analogs following a minimalist approach and supported by chemoinformatics tools have been prepared and evaluated agains
Synthesis, cytotoxicity, antibacterial and antileishmanial activities of imidazolidine and hexahydropyrimidine derivatives
De Carvalho, Gustavo S. G.,Dias, Rafael M. P.,Pavan, Fernando R.,Leite, Clarice Q. F.,Silva, Vania L.,Diniz, Cláudio G.,De Paula, Daniela T. S.,Coimbra, Elaine S.,Retailleau, Pascal,Da Silva, Adilson D.
, p. 351 - 359 (2013/07/28)
This paper describes the synthesis and in vitro biological activities of imidazolidine and hexahydropyrimidine derivatives against bacteria (Escherichia coli, Staphylococcus aureus and Mycobacterium tuberculosis) and Leishmania protozoa. Out of sixteen heterocyclic derivatives tested, none were cytotoxic against mammalian cells. The compounds showed significant bacterial effects and leishmanicidal activity. Compounds 4a and 4c were active against S. aureus and E. coli, respectively. Compounds 3a-3f, 4h and 4i presented promising results against M. tuberculosis, with MIC values ranging from 12.5 to 25.0 μg/mL, comparable to the "first and second line" drugs used to treat tuberculosis. Compounds 4a, 4c and 4e were active against L major. Three of them were structurally characterized by single-crystal X-ray diffraction.
Reversible aminal formation: Controlling the evaporation of bioactive volatiles by dynamic combinatorial/covalent chemistry
Buchsnee Levrand, Barbara,Godin, Guillaume,Trachsel, Alain,De Saint Laumer, Jean-Yves,Lehn, Jean-Marie,Herrmann, Andreas
supporting information; experimental part, p. 681 - 695 (2011/03/22)
Dynamic mixtures generated by reversible aminal formation efficiently prolong the duration of evaporation of bioactive volatile aldehydes. Secondary diamines used for the generation of dynamic mixtures are obtained by treatment of primary diamines with carbonyl compounds and reduction of the diimines with NaBH4. The reversibilities of the reactions were demonstrated by NMR measurements in buffered aqueous solutions. Kinetic rate constants and equilibrium constants for the formation and hydrolysis of aminals were determined. The performance of dynamic mixtures as delivery systems for perfumery ingredients was tested after deposition onto cotton, and the long-lastingness of fragrance evaporation was investigated by dynamic headspace analysis against a reference sample. The simplicity of the concept together with its excellent performance makes this delivery system highly interesting for applied perfumery. Reversible aminal formation might also be successfully applicable to dynamic combinatorial/covalent chemistry for screening of pharmaceutically or catalytically active ligands and receptors. The evaporation of bioactive volatiles that are emitted from flowers to attract insects and that are used as fragrances in our everyday life is limited in time. Dynamic mixtures obtained by reversible aminal formation of suitably designed diamines with volatile aldehydes prolong the perception of these compounds in functional perfumery.