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Structure−Activity Relationships of Cinnamate Ester Analogues as Potent Antiprotozoal Agents
Author(s) -
Bernal Freddy A.,
Kaiser Marcel,
Wünsch Bernhard,
Schmidt Thomas J.
Publication year - 2020
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900544
Subject(s) - antiprotozoal , trypanosoma brucei , potency , in vivo , stereochemistry , leishmania donovani , structure–activity relationship , in vitro , chemistry , biology , pharmacology , biochemistry , leishmaniasis , microbiology and biotechnology , immunology , visceral leishmaniasis , gene
Protozoal infections are still a global health problem, threatening the lives of millions of people around the world, mainly in impoverished tropical and sub‐tropical regions. Thus, in view of the lack of efficient therapies and increasing resistances against existing drugs, this study describes the antiprotozoal potential of synthetic cinnamate ester analogues and their structure‐activity relationships. In general, Leishmania donovani and Trypanosoma brucei were quite susceptible to the compounds in a structure‐dependent manner. Detailed analysis revealed a key role of the substitution pattern on the aromatic ring and a marked effect of the side chain on the activity against these two parasites. The high antileishmanial potency and remarkable selectivity of the nitro‐aromatic derivatives suggested them as promising candidates for further studies. On the other hand, the high in vitro potency of catechol‐type compounds against T. brucei could not be extrapolated to an in vivo mouse model.