Preparation of 3-(trimethylsilanyl)propynoic acid N-(hydroxyalkyl)amides

Медведева, А. С.; Andreev, Michael; Safronova, L. A.; Sarapulova, G. I.; Афонин, А. В.

doi:10.3998/ark.5550190.0002.917

Cited by 2 publications

(1 citation statement)

References 3 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Some reagents have used to preparation of ester analogs [35][36][37][38]; in this study, the compounds 9 or 10 were prepared by the reaction of 7 or 8 with (4-nitro-phenyl)-acetonitrile using 1,3dicyclohexylcarbodiimide (DCC) (Figure 4). It is noteworthy that when DCC is used in some esterification reactions it can produce N-acylurea byproducts.…”

Section: Preparation Of Steroid-ester Derivativesmentioning

confidence: 99%

Experimental and theoretical evaluation of two indol-steroid-cyclobuta-imidazole derivatives as antibacterial drugs

2019

Biointerface Res Appl Chem

View full text Add to dashboard Cite

There some for treatment of infectios deseasses; however, some drugs can induce several adverse effects. The aim of this study was synthesizing and to determinate the antibacterial activity of two indol-steroid-cyclobuta-imidazole complex (compound 11 and 12) against Staphylococcus aureus, Escherichia colli and Klebsiella pneumoniae in a minimum inhibitory concentration (MIC) model, using gentamicin, ciprofloxacin, cefotaxime as controls. The following stage involved the theoretical evaluation of the interaction of both compounds 11 and 12 with the β-lactamase enzyme (5f1g) using a docking software. The data found indicate that compound 12 decrease the growth bacterial of Staphylococcus aureus, Escherichia colli and Streptococcus pneumoniae in comparison with the compound 11 and this effect only was similar to cefotaxime Other theoretical data indicated that compound 12 could interact with different type of amino acids residues such as Ser61, Leu116, Gln117, Asp120, Tyr147, Asn149, Ser209, Tyr218, Thr318, Asn342 involved in the surface of 5f1g compared with 11. These data indicate that; i) the steroid derivative (12) show better affinity by the 5f1g protein in comparison with compound 11 which is translated as higher antibacterial activity; ii) this compound is particularly interesting because could constitute a novel therapy as antibacterial agent.

show abstract

Section: Preparation Of Steroid-ester Derivativesmentioning

confidence: 99%