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Antileishmanial and Antibacterial Activity of a New Pyrazole Derivative Designated 4‐[2‐(1‐(Ethylamino)‐2‐methyl‐ propyl)phenyl]‐3‐(4‐methyphenyl)‐1‐phenylpyrazole
Author(s) -
Dardari Zainaba,
Lemrani Meryem,
Sebban Abdelfatah,
Bahloul Abdelmejid,
Hassar Mohammed,
Kitane Said,
Berrada Mohammed,
Boudouma Mohammed
Publication year - 2006
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200500266
Subject(s) - leishmania infantum , antibacterial activity , pyrazole , amphotericin b , minimum inhibitory concentration , chemistry , leishmania tropica , leishmania , stereochemistry , in vitro , amastigote , staphylococcus aureus , leishmaniasis , antifungal , microbiology and biotechnology , bacteria , cutaneous leishmaniasis , biology , visceral leishmaniasis , biochemistry , immunology , parasite hosting , genetics , world wide web , computer science
Here, we report for the first time the synthesis and the antileishmanial activity of a new pyrazole derivative, namely 4‐[2‐(1‐(ethylamino)‐2‐methylpropyl)phenyl]‐3‐(4‐methyphenyl)‐1‐phenylpyrazole). Micromolar concentrations of this compound were found to inhibit the in vitro multiplication of Leishmania tropica , Leishmania major , and Leishmania infantum , three species causing different forms of leishmaniasis. Furthermore, the 50% inhibitory concentration (IC 50 ) values for the compound are only slightly higher than those of amphotericin B, one of the most active antileishmanial agents used as a satisfactory substitute in cases not responding to pentostam. The IC 50 values after 48 h for L. tropica, L. major , and L. infantum promastigote growth were 0.48 μg/mL, 0.63 μg/mL and 0.40 μg/mL, respectively for the compound, while they were 0.23 μg/mL, 0.29 μg/mL and 0.24 μg/mL, respectively for amphotericin B. We also tested this compound for its antibacterial activity against several bacteria. The strongest antibacterial activity was observed against Entrococcus feacalis and Staphylococcus aureus with a minimal inhibitory concentration (MIC) of 60 μg/mL.