Synthesis and antimicrobial evaluation of 3-(4-tert-amino-2-butynyl)thio and alkyl/alkenylthio-4,5-disubstituted-4H-1,2,4-triazoles

Synthesis and Biological Activities of 3-Alkyl-5-substituted 1,2,4-Triazole Derivatives

“…Azoles are the prominent type of compounds used for this purpose. 1,2,4,-Triazole and its derivatives are an important class of nitrogenous heterocyclic compounds which has been shown to possess a wide range of pharmacological properties such as antifungal 2,3 , antibacterial 4,5 , antimalarial 6 , antiinflammatory, anticonvulsant, antidepressant, antiviral and antitumor activities [7][8][9][10][11][12][13][14][15][16][17][18][19][20][21] . Therefore, 1,2,4-triazole derivatives have attracted considerable attention during the last few decades [22][23][24][25] .…”

Synthesis of new sulfinyl derivatives of 4,5-diphenyl-4H-1,2,4-triazoles

“…Sulfides II-VI were obtained in almost quantitative yield. Except for sulfide IV, the products were reported previously [6], and the results of their biological assays for antimicrobial activity were given therein.Asymmetric oxidation of sulfides II-VI was performed with the use of Sharpless system modified by Kagan: the ratio Ti(OPr-i) 4 -(-)-diethyl D-tartrate-H 2 O was 1 : 2 : 1 [8]. Cumyl hydroperoxide (CHP) as a solution in cumene was selected as oxidant, and the reactions were carried out in methylene chloride at 20°C.…”

Synthesis of 1,2,4-triazole derivatives containing benzothiazoles as pharmacologically active molecule

“…[11][12][13] It is believed that aryl-azolyl-ethane moiety, present in many azole antifungal drugs, serves as pharmacophore in compounds having Mycobacterium killing activity. 14,15 Many azole derivatives have also been shown to possess interesting antimycobacterial activity in addition to antifungal activity.…”

“…13 C NMR spectra were recorded in CDCl 3 on a Bruker Avance II 400 NMR spectrometer operating at 400 MHz (δ in ppm). The microanalyses were performed on a Heraeus Carlo Erba 1180 CHN analyzer.…”

“…Ethyl nicotinate 3 on treatment with hydrazine hydrate yields nicotinoyl hydrazide 4; the IR spectra of 4 showed stretching band around 3335 and 3278 cm −1 due to amine/amide NH, whereas strong stretching band at 1610 cm −1 was attributed to amide carbonyl. 1 H NMR spectrum showed a singlet at δ 4.51 and δ 9.81, which were accounted for NH 2 13 C NMR data of 6a that showed a peak at δ 163.48 and δ 163.35 due to C 3 and C 5 of triazole. Mass spectrum of 6 displayed a molecular ion at m/z 433 that confirmed its molecular weight.…”