Design synthesis and biological

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Design, synthesis, and biological evaluation studies of novel thiophene substituted thiazolidinones scaffold as promising antimicrobial agents

The outcomes are to be compared with typical drugs given that compounds are examined against gram-positive and gram-negative strains of bacteria and fungus. Against bacterial strains, products with nitro, methyl, and bromo substituents in the p-position of the benzene ring, as well as products with the nitro group at the m-position, showed very excellent activities against bacterial strains, while compounds with chloro substituent at p-position and m-position demonstrated good activity against the fungal strains Aspergillus niger and Fusarium javanicum.

8p dianmotminh02 03-05-2024 7 2 Download

Design, in silico studies, synthesis, and in vitro anticancer assessment of new naphthylidene isoxazolidinedione derivatives

. In vitro biological evaluation revealed the most active compound 4d with an inhibitory concentration of 42.87 μM against K562 and 47.42 μM on A549 cells. The anticancer activity of this naphthylidene isoxazolidinedione derivative was evident by cell cycle and apoptosis assays, which showed arrest of the G2/M phase (65.6%) of the K562 cells and induction of apoptosis with 21.47% apoptotic cells as compared to 0.2% of untreated cells, respectively.

10p dianmotminh02 03-05-2024 7 3 Download

Design, synthesis and biological evaluation of 1,3,4-oxadiazoles/thiadiazoles bearing pyrazole scaffold as antimicrobial and antioxidant candidates

A series of semicarbazones, thiosemicarbazones, 1,3,4-oxadiazoles/thiadiazoles bearing pyrazole scaffold were designed and synthesized. All the synthesized new compounds were characterized by 1H NMR, 13C NMR, MS and elemental analysis.

14p tocectocec 26-05-2020 28 2 Download
Báo cáo Y học: Synthesis, conformational analysis and biological activity of cyclic analogs of the octadecaneuropeptide ODN Design of a potent endozepine antagonist

The octadecaneuropeptide (ODN; QATVGDVNTDRPG LLDLK) and its C-terminal octapeptide (OP; RPGLLDLK), which exert anxiogenic activity, have been previously shown to increase intracellular calcium concentration ([Ca21]i) in cultured rat astrocytes through activation of a metabotropic receptor positively coupled to phospholipase C. It has also been found that the [D -Leu5]OP analog possesses a weak antagonistic activity. The aim of the present study was to synthesize and characterize cyclic analogs of OP and [D -Leu5]OP.

13p system191 01-06-2013 32 4 Download
Specific and sensitive quantitative RT-PCR of miRNAs with DNA primers

important regulators of biological processes in animals and plants. MiRNAs regulate gene expression at the posttranscriptional level by binding to mRNAs and either inhibit translation or modify the stability of the mRNA. Due to the important biological role of miRNAs it is of great interest to study their expression level in the cells. Furthermore, miRNAs have been associated with cancer and other diseases [1] and miRNA expression can help in the diagnosis and prognostic of human disease [2,3].

11p zingzing09 24-04-2013 51 3 Download
Báo cáo khoa học: Synthesis and characterization of a new and radiolabeled high-afﬁnity substrate for H+/peptide cotransporters

In this study we described the design, rational synthesis and functional characterization of a novel radiolabeled hydrolysis-resistant high-affinity substrate for H + ⁄peptide cotransporters. l-4,4¢-Biphenylalanyl–l-Proline (Bip-Pro) was synthesized according to standard procedures in peptide chemistry.

10p media19 05-03-2013 37 4 Download