Literature DB >> 16619283

Antileishmanial and antibacterial activity of a new pyrazole derivative designated 4-[2-(1-(ethylamino)-2-methyl- propyl)phenyl]-3-(4-methyphenyl)-1-phenylpyrazole.

Zainaba Dardari1, Meryem Lemrani, Abdelfatah Sebban, Abdelmejid Bahloul, Mohammed Hassar, Said Kitane, Mohammed Berrada, Mohammed Boudouma.   

Abstract

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 (IC50) 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 IC50 values after 48 h for L. tropica, L. major, and L. infantum promastigote growth were 0.48 microg/mL, 0.63 microg/mL and 0.40 microg/mL, respectively for the compound, while they were 0.23 microg/mL, 0.29 microg/mL and 0.24 microg/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 microg/mL.

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Year:  2006        PMID: 16619283     DOI: 10.1002/ardp.200500266

Source DB:  PubMed          Journal:  Arch Pharm (Weinheim)        ISSN: 0365-6233            Impact factor:   3.751


  4 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Ethyl 5-amino-1-(4-chloro-2-nitro-phen-yl)-1H-pyrazole-4-carboxyl-ate.

Authors:  Muhammad Zia-Ur-Rehman; Mark R J Elsegood; Jamil Anwar Choudary; Muhammad Fasih Ullah; Hamid Latif Siddiqui
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-01-10

3.  5-Amino-1-phenyl-1H-pyrazole-4-carboxylic acid.

Authors:  Muhammad Zia-Ur-Rehman; Mark R J Elsegood; Nosheen Akbar; Rahman Shah Zaib Saleem
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-06-21

4.  Successful Dendrimer and Liposome-Based Strategies to Solubilize an Antiproliferative Pyrazole Otherwise Not Clinically Applicable.

Authors:  Silvana Alfei; Andrea Spallarossa; Matteo Lusardi; Guendalina Zuccari
Journal:  Nanomaterials (Basel)       Date:  2022-01-11       Impact factor: 5.076

  4 in total

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