HYDRAZIDE-N-ACYLHYDRAZONE COMPOUNDS, METHOD FOR PRODUCING HYDRAZIDE-N-ACYLHYDRAZONE COMPOUNDS, USE OF INTERMEDIATE COMPOUNDS FOR PRODUCING HYDRAZIDE-N-ACYLHYDRAZONES FOF THE TREATMENT OF LEISHMANIASIS AND CHAGAS DISEASE, AND THUS OBTAINED PHARMACEUTICAL COMPOSITIONS
Universidade Federal de Alagoas;Universidade Federal do Rio de Janeiro
发明人:
LIDIA MOREIRA LIMA,Lídia Moreira Lima,ELIEZER JESUS DE LACERDA BARREIRO,Eliézer Jesus de Lacerda Barreiro,MARINA AMARAL ALVES,Marina Amaral Alves
申请号：
BRBR2013/000276
公开号：
WO2014/019044A1
申请日:
2013.07.31
申请国别(地区):
BR
年份:
2014
代理人:
摘要：
The invention relates to hydrazide-N-acylhydrazone compounds, to a method for producing hydrazide-N-acylhydrazone compounds, to the use of intermediate compounds for producing hydrazide-N-acylhydrazones for the treatment of leishmaniasis and Chagas disease, and to the thus obtained pharmaceutical compositions. The invention describes, in particular, the production of leishmanicidal and/or trypanocidal compounds that inhibit the cysteine proteinases involved in infectious processes caused by parasites of the Trypanossoma cruzi and Leishmania species. In other words, the invention relates to the development of the series of hydrazide-N-acylhydrazone compounds aimed at providing an active principle for pharmaceutical compositions for the treatment of the various clinical forms of leishmaniasis and Chagas disease； to the development of the series of functionalised hydrazide-N-acylhydrazone derivatives (series III and IV), achieved by molecular hybridization between the LASSBio-1111 (leishmanicidal) prototype and the LASSBio-1064 (trypanocidal) prototype by hybridisation of the aryl-hydrazide subunit of LASSBio-1111 with the functionalised acylhydrazone of LASSBio-1064, producing a new molecular pattern that conjugates leishmanicidal and/or trypanocidal properties.L'invention concerne des composés hydrazide-N-acylhydrazones, un procédé d'obtention de composés hydrazide-N-acylhydrazones, l'utilisation de composés intermédiaires pour l'obtention d'hydrazide-N-acylhydrazones pour le traitement de la leishmaniose et de la maladie de Chagas, ainsi que les compositions pharmaceutiques obtenues, et notamment l'obtention de composés leishmanicides et/ou tripanomicides, inhibiteurs des cystéine protéinases impliquées dans les processus infectieux causés par les parasites Trypanossoma cruzi et Leishmania sp. En d'autres termes, l'invention concerne l'élaboration de la série de composés hydrazide-N-acylhydrazones avec pour objectif de produire un principe actif pour compositions ph
