• Media type: E-Book
  • Title: Synthesis of analogues of the pentamidine bearing heterocyclic platforms (rhodanine, benzimidazole, pyrazole and imidazole) and their biological evaluations ; Synthèse d'analogues de la pentamidine porteurs de plateformes hétérocycliques (rhodanine, benzimidazole, pyrazole et imidazole) et leurs évaluations biologiques
  • Contributor: Ambeu, N'Ta Christelle [VerfasserIn]
  • imprint: [Erscheinungsort nicht ermittelbar]: HAL CCSD, 2015
  • Language: French
  • Origination:
  • University thesis: Dissertation, HAL CCSD, 2015
  • Footnote:
  • Description: This thesis manuscript is focused on the development of multi-steps synthesis strategy of new compounds bearing several heterocyclic platforms (rhodanine, benzimidazole, pyrazole and imidazole) for multiple therapeutic use to fight malaria, leishmaniasis, cancer et neurodegenarative diseases. The pharmacomodulations of these compounds were developped from the design of pentamidine 35 which containins 2 fragments benzamidine (parts ''West'' and ''East''). Indeed, the substitution of its part ''West'' by a platform rhodanine or benzimidazole and its part ''East'' by an azole" aromatic ring system (pyrazole, imidazole) lead respectively to 5-arylidene rhodanines (50, 58), to derivatives ''aza'' (99,100) and to derivatives ''aza azoles'' 174 which are pentamidine analogs. The chemical yields of these compounds are ranging respectively from 26 to 98%, 10 to 93% and 10 to 97%. All the compounds synthesized in the chapters II, III and IV of this research work were evaluated for their antiproliferative activity on tumoral cell lines and for their inhibitory activity on protein kinases.
  • Access State: Open Access