Click Synthesis, Anticancer Activity and Molecular Docking Studies on Pyridazinone Scaffolds

Design, Synthesis, and Antimicrobial Activities of 1,2,3-Triazole Glycoside Clickamers

“…The Cu(I)-catalyzed cycloaddition of the 2-(2-(2-methoxyethoxy)ethoxy)-ethyl 3-azidobenzoate 1 [26] with the terminal alkyne groups of the acetylated D-galactose 2, D-glucose 3, and D-xylose 4 [72] afforded the corresponding 1,2,3-triazole-based glycosides 5-7 in good yields (75%-81%) as demonstrated in Scheme 1. The 1,2,3-triazole ring acts as a linker connecting the substituted-aryl and sugar units.…”

“…The FT-IR spectra were recorded on a Shimadzu IR 8400s spectrophotometer (KBr, ν max /cm −1 ) at the Micro Analytical Laboratory, Cairo University, Egypt. The aromatic azides (1 and 8) and acetylenic sugars (2, 3, and 4) were prepared according to the reported procedures in the literature [26,27,72]. The title compound was separated and purified by column chromatography (Petroleum ether/ethyl acetate 8/2) as a yellow oil (78%).…”

“…Therefore, special concern should be devoted to the development of new antimicrobial agents, possessing completely different chemical structures, and working with different modes of actions. The Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction offers a versatile synthetic access to the 1,2,3-triazole heterocycle derivatives, which are associated with a wide spectrum of pharmacological activities, including antimycobacterial [18][19][20][21], antitubercular [22][23][24][25], anticancer [26][27][28][29], antiviral [30][31][32][33][34], antidiabetic [35][36][37][38], antifungal [39][40][41][42], anti-HIV [43][44][45][46], anti-inflammatory [47][48][49][50], antimalarial [51][52][53][54], anti-oxidant [55][56][57][58], anti-proliferative [59][60][61][62] properties. The 1...…”

“…1,2,3-Triazoles linked to carbohydrates have attracted widespread attention, on account of their positive effect on enhancing solubility and biological activity [65][66][67][68][69][70][71]. In continuation of our previous work on the synthesis of bioactive molecular architectures based on the 1,2,3-triazole heterocycle [26,27,30], we report in this study the synthesis, characterization, and antimicrobial evaluation of six novel 1,2,3-triazole glycosides using the click chemistry synthetic approach.…”

Hydrophobically Modified Dextran Esters as Potential External Biocides

“…Based on the type of polymeric system, antimicrobial polymers can be classified [7]: (1) biocidal polymers, with intrinsic antimicrobial activity; (2) polymeric biocides, which have biocide molecules attached on the polymer backbone; and (3) biocidereleasing polymers, having biocide molecules included in a polymeric matrix. 1,2,3-triazoles and their derivatives, synthesized in the last decades by "click chemistry" [1,48,55], have various pharmacological activities, such as: anticancer [14,15,24], anti-HIV [25,37,64], antiviral [9,19,32], antimycobacterial [3,4,20,42], antifungal [2,13,29], antidiabetic [5,18,49], antitubercular [41,46,50], antimalarial [8,10,43], anti-inflammatory [38,45]. These N-heterocyclic derivatives linked to carbohydrates have captured broad attention, due to their increased solubility and biological activity [17,28,54].…”