A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity. Triazole derivatives
3a–
e and
4a–
e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds
1a–
e
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A series of novel thiourea and urea derivatives containing 1,2,4-triazole moieties were synthesized and evaluated for their antifungal and larvicidal activity. Triazole derivatives
3a–
e and
4a–
e were synthesized by reacting thiocarbohydrazide with thiourea and urea compounds
1a–
e and
2a–
e, respectively, in a 130–140 °C oil bath. The proposed structures of all the synthesized compounds were confirmed using elemental analysis, UV,
IR,
1H-NMR and mass spectroscopy. All compounds were evaluated for antifungal activity against plant pathogens, larvicidal and biting deterrent activity against the mosquito
Aedes aegypti L. and
in vitro cytotoxicity and anti-inflammatory activity against some human cell lines.
Phomopis species were the most sensitive fungi to these compounds. Compounds
1b,
1c,
3a and
4e demonstrated selectively good activity against
Phomopis obscurans and only
1b and
4e showed a similar level of activity against
P. viticola. Compound
3d, with a LD
50 value of 67.9 ppm, followed by
1c (LD
50 = 118.8 ppm) and
3e (LD
50 = 165.6 ppm), showed the highest toxicity against
Aedes aegypti larvae. Four of these compounds showed biting deterrent activity greater than solvent control, with the highest activity being seen for
1c, with a proportion not biting (PNB) value of 0.75, followed by
1e,
2b and
1a. No cytotoxicity was observed against the tested human cancer cell lines. No anti-inflammatory activity was observed against NF-kB dependent transcription induced by phorbol myristate acetate (PMA) in human chondrosarcoma cells.
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