Antileishmanial and Antibacterial Activity of a New Pyrazole Derivative Designated 4‐[2‐(1‐(Ethylamino)‐2‐methyl‐ propyl)phenyl]‐3‐(4‐methyphenyl)‐1‐phenylpyrazole

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.

Synthesis, antiviral, cytotoxicity and antitumor evaluations of A4 type of porphyrin derivatives

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Synthesis and antimicrobial activity of substituted [(pyrazol‐4‐yl)methylene]hydrazono‐2,3‐dihydrothiazoles and their sugar derivatives

“…Table 1 In vitro antimicrobial activity by agar diffusion method of tested compounds. (8). To a solution of the substituted thiazole 4 (4.97 g, 10 mmol) and potassium hydroxide (0.56 g, 10 mmol) in absolute ethanol (20 mL) was added 2-(2-chlorethoxy)ethanol (1.24 g, 10 mmol).…”

Synthesis and anti-bacterial activity of novel 1,3-pheylene-bis-N-acetyl- and N-phenylpyrazole derivatives

“…[1][2][3][4][5][6][7][8] Addition, pyrazole derivatives play an important role in the development of pesticides and medicines. Several of pyrazole products are available and widely used as fungicides, antiviral agents, analgesic agents, insecticides and herbicides.…”