Synthesis of Thymol Derivatives as Potential Non-Irritant Antimicrobial and Insecticidal Agents

Author(s): Mostafa M.M. El-Miligy*, Aly A. Hazzaa, Saad R. El-Zemity, Ahmed K. Al-Kubeisi.

Journal Name: Current Bioactive Compounds

Volume 15 , Issue 1 , 2019

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Abstract:

Background: Thymol has been reported to have a variety of antimicrobial and insecticidal activities but it has irritation side effect due to its phenolic nature.

Methods: A new series of potential non-irritant non-phenolic thymol derivatives were designed to hybridize the well-known biologically active thymol scaffold with various five membered heterocyclic antimicrobial and insecticidal pharmacophores like 1,3,4-oxadiazole, 1,3,4-thiadiazole, 1,2,4-triazole, thiazole and 4-thiazolidinone through different spacers. The target compounds were biologically evaluated for their in vitro antibacterial, antifungal and insecticidal activities.

Results: Compounds 4b and 9c showed weak antibacterial activity against S. aureus and B.subtilis with the inhibition zone diameters ranging from 2 to 7 mm and 4 mm respectively compared with ciprofloxacin with the inhibition zone diameter of 21 mm. Compounds 9a, 7d and 13b showed weak antibacterial compounds against B. subtilis with inhibition zone diameters 4, 4 and 6 mm respectively. Compounds 12b, 9c and 7a showed 20% insecticidal activity at a concentration of 0.157 mg/cm2 for each compound against Tribolium castaneum (Herbst) and Sitophilus oryzae (L.). Compound 6 showed moderate larvicidal activity against Culex pipiens with 40% mortality at a concentration of 1000 ppm.

Conclusion: Compound 9c showed weak dual antimicrobial and insecticidal activities.

Keywords: Thymol, insecticide, antimicrobial, azoles, azolidinones, morphology.

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Article Details

VOLUME: 15
ISSUE: 1
Year: 2019
Page: [125 - 137]
Pages: 13
DOI: 10.2174/1573407213666171115161626
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