1362020-64-1

Upstream product

• 536-90-3 m-Anisidine 
• 3866-16-8 3-methoxyphenyl azide 
• 141-97-9 ethyl acetoacetate 
• 4341-76-8 Ethyl 2-butynoate 

Relevant academic research and scientific papers

Primary discovery of 1-aryl-5-substituted-1H-1,2,3-triazole-4-carboxamides as promising antimicrobial agents

Three series of novel 1H-1,2,3-triazole-4-carboxamides: 1-aryl-5-alkyl/aryl-1H-1,2,3-triazole-4-carboxamides, 1-aryl-5-amino-1H-1,2,3-triazole-4-carboxamides and 1,2,3-triazolo[1,5-a]quinazoline-3-carboxamides were synthesized via base-mediated click azide reactions. Compounds were evaluated for their antimicrobial activities against primary pathogens: Gram-positive and Gram-negative bacterial strains Escherichia coli, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus, as well as fungal strain Cryptococcus neoformans var. grubii and Candida albicans. Compounds exhibiting moderate to good activities were selected for SAR analysis. Several 5-methyl-1H-1,2,3-triazole-4-carboxamides 4d, 4l, 4r, showed potent antibacterial effect against S. aureus. On the contrary, 5-amino-1H-1,2,3-triazole-4-carboxamide 8b and [1,2,3]triazolo[1,5-a]quinazoline-3-carboxamide 9a were active against pathogenic yeast C. albicans. Thus, compound 4l under 1 μM demonstrated 50% growth inhibition against S. aureus. At the same concentration, the compound 9a killed approx. 40% of C. albicans cells. In general, these compounds demonstrated selective action and no significant impact on the viability of human keratinocytes of HaCaT line.

An integrated high-throughput strategy enables the discovery of multifunctional ionic liquids for sustainable chemical processes

Development of new chemical processes with simplified reaction systems and work-up procedures is a challenging task. Although ionic liquids are a class of potential multifunctional compounds to simplify traditional chemical processes, their rational design is difficult due to complex interactions. In this work, a proof-of-concept strategy has been proposed to achieve an integration of high-throughput preparation of ionic liquids and in situ screening of their reaction-promoting performance in 96-well plates. The integrated approach then enables a facile identification of optimal ionic liquids from a 400-ionic liquid candidate pool to act as the solvent, the catalyst and the separating assistant, simultaneously, for carbonyl-azide cycloaddition reactions. Merits of the ionic liquids-based processes have been demonstrated not only in the convenient and efficient synthesis of 1,2,3-triazolyl compounds but also in the discovery of a new reaction for the chemical post-modification of free peptides.

Design, synthesis, and in vitro biological evaluation of 1 H -1,2,3-triazole-4-carboxamide derivatives as new anti-influenza A agents targeting virus nucleoprotein

The influenza virus nucleoprotein (NP) is an emerging target for anti-influenza drug development. Nucleozin (1) and its closely related derivatives had been identified as NP inhibitors displaying anti-influenza activity. Utilizing 1 as a lead molecule, we successfully designed and synthesized a series of 1H-1,2,3-triazole-4-carboxamide derivatives as new anti-influenza A agents. One of the most potent compounds, 3b, inhibited the replication of various H3N2 and H1N1 influenza A virus strains with IC 50 values ranging from 0.5 to 4.6 μM. Compound 3b also strongly inhibited the replication of H5N1 (RG14), amantidine-resistant A/WSN/33 (H1N1), and oseltamivir-resistant A/WSN/1933 (H1N1, 274Y) virus strains with IC 50 values in sub-μM ranges. Further computational studies and mechanism investigation suggested that 3b might directly target influenza virus A nucleoprotein to inhibit its nuclear accumulation.