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. 2018 Apr;27(4):1269-1275.
doi: 10.1007/s00044-018-2146-4. Epub 2018 Feb 27.

Evaluation of Triazole and Isoxazole Derivatives as Potential Anti-infective Agents

Amer H Tarawneh  1   2 , Lo Ay A Al-Momani  2 , Francisco León  1 , Surenda K Jain  1   3 , Anastassiya V Gadetskaya  3   4 , Sultan T Abu-Orabi  5 , Babu L Tekwani  2 , Stephen J Cutler  1   6
Affiliations

Evaluation of Triazole and Isoxazole Derivatives as Potential Anti-infective Agents

Amer H Tarawneh et al. Med Chem Res. 2018 Apr.

Abstract

A series of isoxazole and triazole derivatives, with interesting bioactive scaffolds, were examined for their in vitro antibacterial, antifungal, and antiprotozoal activities. These compounds exhibited antitrypanosomal activity comparable to difluoromethylornithine (DMFO), a drug used in the treatment of human African trypanosomiasis. Isoxazole analogues 1, 3 and 4, and triazole derivatives 16, 17, 28, 37, 40 and 42 showed the highest antitrypanosomal activity with IC50 values of 17.89, 1.82, 10.38, 10.26, 11.77, 9.29, 3.93, 2.11, and 0.93 μM, respectively. Compounds 40 and 42 showed the most potent activity against Leishmania donovani amastigotes with IC50 values of 18.28 and 10.54 μM, respectively. Compound 42 showed the most potent activity against Leishmania donovani macrophage internalized amastigotes with an IC50 value of 8.32 μM. Conjugate triazoles 40-43 displayed potential antimalarial activity against chloroquine-resistant W2 and chloroquine sensitive D6 Plasmodium falciparum strains (IC50 value range from 0.58 to 8.36 μM). Compound 37 showed antibacterial activity against Staphylococcus aureus, MRSA and Mycobacterium intracellulare with IC50 values of 15.53, 14.22 and 47.45 μM, respectively. None of the compounds exhibited antifungal activity.

Keywords: antibacterial and antiprotozoal activity; triazole and isoxazole derivatives.

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Conflict of interest statement

Conflict of Interest: The authors declare that they have no conflict of interest.

Figures

Figure 1
Figure 1
Isoxazole and dihydroisoxazole derivatives (1–12)
Figure 2
Figure 2
Triazole derivatives (13–36)
Figure 3
Figure 3
Triazole conjugated derivatives (37–43)
Figure 4
Figure 4
Survival chart for mice in antimalarial study (43)
See this image and copyright information in PMC

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