TITLE:
Synthesis and in Vitro Biological Activities of 4,5-Disubstituted 1,2,4-Triazole-3-Thiols
AUTHORS:
Humaira Nadeem, Muhammad Mohsin, Hasan Afzaal, Sadaf Riaz, Ammar Zahid, Syed Aun Muhammad
KEYWORDS:
4, 5-Disubstituted 1, 2, 4-Triazole-3-Thiols; Antibacterial; Antitumor; Antioxidant; Cytotoxic
JOURNAL NAME:
Advances in Microbiology,
Vol.3 No.4,
August
6,
2013
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.