Synthesis, Antimicrobial, and Antioxidant Screening of Aryl Acetic Acid Incorporated 1,2,4‐Triazolo‐1,3,4‐Thiadiazole Derivatives

Abstract

in Wiley Online Library (wileyonlinelibrary.com).Some novel [1,2,4]triazolo [3,4-b] [1,3,4]thiadiazole derivatives were synthesized from aryl acetic acids. All the synthesized derivatives were selected for the screening of antibacterial potential against Grampositive bacteria [Staphylococcus aureus (MTCC 3160) and Micrococcus luteus (MTCC 1538)] and Gram-negative bacteria [Escherichia coli (MTCC 1652) and Pseudomonas aeruginosa (MTCC 424)] and antifungal potential against Aspergillus niger (MTCC 8652) and Candida albicans (MTCC 227), and free radical scavenging activity through 2,2-diphenyl-2-picrylhydrazyl hydrate method. The compounds TH-4, TH-13, and TH-19 were found to be more potent antimicrobial agents compared to standard drugs. The compounds TH-3, TH-9, and TH-18 also showed significant antimicrobial activity. The compound TH-13 showed antioxidant activity with IC 50 value better than the standard compound. The structures of all the synthesized compounds were confirmed by Fourier transform infrared, 1 H-NMR, liquid chromatography-mass spectrometry, and CHN analyzer.

Synthesis, Antibacterial Activity, and Mechanisms of Novel 6-Sulfonyl-1,2,4-triazolo[3,4-b][1,3,4]thiadiazole Derivatives

“…They often exhibit higher biological activity, especially antimicrobial activity, due to their thickening with a triazole . 1,2,4-Triazolo­[3,4- b ]­[1,3,4]­thiadiazole compounds are widely used to develop medical antibacterial agents − and antifungal agents, − but they have been less studied in the control of plant pathogenic bacteria.…”

Benzoik Asit Temelli Yeni 1,3,4-Tiyadiazollerin Sentezi, Karakterizasyonu, ve Antioksidan Aktiviteleri

“…Thiadiazole is a heterocyclic compound covering both two nitrogen atoms and sulfur atom as part of the five-membered aromatic ring [1]. 1,3,4-Thiadiazole compounds have shown numerous medicinal properties and biological activities such as antituberculosis [1], anticancer [2], urease inhibitory [3], anti-inflammatory [4], antibacterial [5], antimicrobial [6], anti-leishmanial [7], and antioxidant activity [3,[8][9][10]. Furthermore, they are largely used in agricultural applications, such as herbicides, fungicides, pesticides, insecticides, and bactericides [11].…”

Yeni 1,3,4-Tiyadiazol-Piperazin Türevlerinin Sentezi, İn Vitro Antikolinesteraz ve Antimikrobiyal Değerlendirilmesi

“…1,3,4-Thiadiazole moiety is connected to a broad spectrum of biological activities possibly due to the presence of pharmacophoric (N-C=S) moiety [4]. Thiadiazole by acting as "two-electron donor system" and "hydrogen binding domain" also made itself as a constrained pharmacophore.…”

“…The core motif thiadiazole and its derivatives have been reported in the literature for wide varieties of pharmacological activities such as antitumoral, antimicrobial, antiviral, antifungal, anti-inflammatory, antiplatelet, anti-tubercular, and antidepressant activities [6]. Acetazolamide, methazolamide, and megazol are thiadiazole containing drugs available in the market [4].…”