Synthesis and in Vitro Biological Activities of 4,5-Disubstituted 1,2,4-Triazole-3-Thiols

Humaira Nadeem, Muhammad Mohsin, Hasan Afzaal, Sadaf Riaz, Ammar Zahid, Syed Aun Muhammad

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Department of Pharmaceutics, Riphah Institute of Pharmaceutical Sciences, Riphah International University Islamabad, Islamabad, Pakistan.

DOI: 10.4236/aim.2013.34050                

Abstract

Purpose: The triazole nucleus is an important part of the therapeutically interesting drug candidate as antimicrobial, analgesic, anticancer, anticonvulsant and anti-inflammatory agents. Methods: Therefore, in this study, twelve 4,5-disubstituted-1,2,4-triazole-3-thiols were synthesized by the reaction of substituted isothiocyanates and hydrazides using the common method of base catalysed intramolecular dehydrative cyclization of substituted thiosemicarbazides 3(a-f) and 4(a-f). The structures of these compounds were characterized by means of FT-IR, ¹H-NMR, and elemental analysis data. All these compounds were screened for antibacterial, antioxidant, antitumor and cytotoxic activities. Results: Among these compounds: 5c, 5f and 6f were found active against gram positive cocci, the compounds 5a, 5b, 5d, 6a and 6f showed 85% free radical scavenging effect at 3 ppm when tested for antioxidant activity, 75% tumors inhibition was recorded using 5c, 5d and 6a and brine shrimps lethality assay declared 5a, 5b and 6d was 129.62 μg/ml, 161.577 μg/ml and 81.56 μg/ml respectively. Conclusion: Compounds carrying significant bioactivity can be further studied using animal models to establish their safety profile prior to initiating clinical trials.

Keywords

4, 5-Disubstituted 1, 2, 4-Triazole-3-Thiols; Antibacterial; Antitumor; Antioxidant; Cytotoxic

Conflicts of Interest

The authors declare no conflicts of interest.

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