Evaluation of triazole and isoxazole derivatives as potential anti-infective agents

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.

Phytochemical study of Piliostigma thonningii, a medicinal plant grown in Nigeria

“…Difluoromethy lornithine was used as positive drug controls. IC 50 values were computed from the dose response growth inhibition curve by XLfit version 5.2.2 (Mohamed et al 2016a; Tarawneh et al 2018). …”

“…Differentiated THP1 cells were been used in the macrophage internalized amastigote assay. The macrophage internalized amastigote method was based on parasite rescued and transformation assay described earlier; pentamidine was used as positive standards (Jain et al 2012; Tarawneh et al 2018). …”

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

“…2). 16 In 2018, various biological screenings were conducted [17][18][19][20] which led to the identification of anticancer, [21][22][23] antimicrobial, [24][25][26][27][28] anti-infective, 29,30 and antioxidant [31][32][33] properties of the studied 1,2,3-triazole-bearing hybrids. Moreover, triazole-linked derivatives were suggested to affect adenosine diphosphate ribosylation biology, 34 and were used widely in peptides to mimic a trans-amide bond, despite their hazardous effects on native peptide activity.…”

Synthesis, Antimicrobial and Antioxidant Activities of 2-Isoxazoline Derivatives

“…In this study, the free radical scavenging activity of all compounds was carried out in the presence of the DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS (2’-azino–bis(3-ethylbenzoline-6-sulfonic acid) diammonium salt) using ascorbic acid and α-Tocopherol antioxidant agents as a positive control. Although several methods are available for the determination of the antioxidant activity, the DPPH and ABTS methods are very common, rapid, and two of the most appropriate methods [ 14 , 15 ].…”