Synthesis, characterization, and antifungal activity of biaryl-based bis(1,2,3-triazoles) using click chemistry

Synthesis and Antifungal Activity of Benzamidine Derivatives Carrying 1,2,3-Triazole Moieties

“…1,2,3-Triazoles are very important heterocycles showing excellent bioactivities in pharmaceutical and agrochemical applications. Compounds containing 1,2,3-triazoles have been reported for their antifungal [21,22,23], antibacterial [24,25,26,27], anti-HIV [28], insecticidal [29], herbicidal [30], antiviral [31], antitumor [32], tuberculosis inhibitory [33], antiprotozoal [34], antimalarial [35], anticancer [36], and larvicidal [37] activities. The fungicidal activity of the commercial fungicide fluconazole can be improved by introducing a 1,2,3-triazole moiety into the molecule [38,39].…”

Synthesis and antimicrobial evaluation of 1,4-disubstituted 1,2,3-triazoles containing benzofused N-heteroaromatic moieties

“…All the synthesized compounds exhibited moderate-togood antifungal activity against tested fungal strains as depicted by MIC values expressed in lmol/cm 3 The results clearly indicated that the presence of electron withdrawing groups on phenyl ring improved the antifungal activity of synthesized compounds against A. niger; whereas, presence of electron donating groups on phenyl ring increased the fungicidal activity of synthesized triazoles against C. albicans. Moreover, replacement of benzyl group by phthalimide-NCH 2 group at N 1 position of triazole ring of compound (9f) having carbazolyl moiety increased the antifungal efficiency against A. niger.…”

“…Among these heterocycles, much importance has been given to the triazole nucleus which possess a wide range of pharmacological activities like antimicrobial [2,3], antitrypanosomal [4], antimalarial [5,6], anti-HIV [7], anticancer [8][9][10], antitubercular [11,12], anticonvulsant [13], antiallergic [14], etc. The regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles through copper(I) catalyzed 1,3-dipolar cycloaddition was independently reported by Sharpless [15] and Meldal [16] in 2002, led to great success over Huisgen's classical thermal method [17] which yields 1,4-and 1,5-disubstituted isomers.…”

Synthesis of 1,4-disubstituted 1,2,3-triazole Derivatives Using Click Chemistry and their Src Kinase Activities

“…There has been a great interest in the development of five-membered nitrogen heterocycles in medicinal chemistry. Among them, 1,2,3-triazole heterocycles containing molecules are reported to possess a large biological spectrum as antimicrobial [20][21][22], antimalarial [23], antihistaminic [24], antifungal [25,26], anti-Hiv [27,28], antitubercular [29] Rf = 0.1 (Cyclohexane/EtOAc, 1:1, v/v); Yellow solid; mp: 147-149°C; IR: 3429 (NH), 3357 (NH), 3108 (CHar) 1745 (C=O ester); Yield =70%; 1 2-(4-(thiophen-3-yl)-1H-1,2,3-triazol-1-yl)…”