Synthesis, anti-microbial activity and molecular docking studies on triazolylcoumarin derivatives

Abstract

A series of triazolylcoumarins was synthesized by the cycloaddition of acetylenic derivatives to azide in the presence of Cu(I) catalyst at room temperature. All the synthesized compounds were evaluated for their anti-microbial activity against Gram-positive (B. subtilis and S. aureus), Gram-negative bacteria (K. pneumonia and P. vulgaris) and human pathogenic fungi (C. tropicalis and C. krusei), with tetracycline and fluconazole as standards for anti-microbial and anti-fungal activity. Triazolylcoumarins exhibit anti-microbial activity against all the tested pathogens, which is further supported by molecular docking studies.

Synthesis and antibacterial activity of some novel piperazinophanes with an intraannular ester functionality

“…Though we have shown that imino cyclophane 21 exhibited good antibacterial activity against Escherichia coli, Klebsiella pneumoniae and Staphylococcus aureus bacteria, the synthesis and the yields are challenging. Hence, recently, we synthesized various sulphonophanes 22 and tested their antibacterial activity towards Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus bacteria and we observed that their antibacterial activity was comparable to that of the piperazinophanes reported herein. In fact the antibacterial activity expressed as MIC values of some of the sulphonophanes reported earlier by our research group lies in the range of 10 mg mL À1 to 20 mg mL À1 and in the present study, the synthesized piperazinophanes show MIC values to be in the range of 12.5 mg mL À1 to 25 mg mL À1 for the three pathogens viz against Escherichia coli, Klebsiella pneumoniae and Staphylococcus aureus.…”

Coumarin–triazole Hybrids and Their Biological Activities

“…Compared with the mono‐nuclear compounds, the multinuclear derivatives often exhibited some unique properties such as the bisquinoline piperaquine that is active against both chloroquine‐sensitive and chloroquine‐resistant strains of P. falciparum . The bis/tri(coumarin–1,2,3‐triazole) hybrids displayed potential antibacterial and antifungal potency, but the majority of them were less active than the references Tetracycline and Fluconacole .…”

Synthesis, Crystal Studies and Pharmacological Role Prediction of 3-Iodo-2- Methyl-1 Phenyl Sulfonyl-1h Indole

“…Hence, the synthesis of several substituted indoles and the study of their crystal, molecular structure, and molecular docking studies continue to be an interesting field of research [4]. Docking is frequently used to predict the binding orientation of small molecules to the protein targets to predict the affinity and activity of the small molecule [5][6][7]. With this background information, a new indole derivative was synthesized.…”