Synthesis and biological evaluation of fluoroquinolones containing a pyridoxine derivatives moiety.

We report herein the design, synthesis and biological evaluation of series of 7-substituted fluoroquinolones with pyridoxine derivatives. In vitro screening of antibacterial activity and toxicity of 39 synthesized fluoroquinolones defined compounds 7 and 28 as lead compounds for further investigations. On various clinical isolates lead compounds 7 and 28 exhibited antibacterial activity comparable with reference fluoroqinolones.

Antimicrobial Activity of the Serum before and after Vaccination with EpiVacCorona.

We evaluated the effect of vaccination with anti-COVID-19 vaccine EpiVacCorona on serum antimicrobial activity, formation of specific IgG antibodies, and expression of some antimicrobial peptides. Antimicrobial activity of the serum from 55 volunteers towards S. aureus cells was measured spectrophotometrically; IgG-antibodies against SARS-CoV-2 antigen were assayed by ELISA; expression of genes encoding antimicrobial peptides LL37, HBD1, and HBD2 was evaluated by PCR with reverse transcription.

Method of salivary histatins determination.

Histatins are the most significant antimicrobial peptides (AMP) of saliva and there are 12 types of such AMP. Histatin molecules contain relatively high percent of histidine and tyrosine residues. This property allows to use well known from organic chemistry Pauly reaction for detection of protein bounded histidine and tyrosine residues (BHT), which are in fact characterize the summary content of all histatins in saliva.

Synthesis, antitumor activity and structure-activity studies of novel pyridoxine-based bioisosteric analogs of estradiol.

A new efficient approach to the synthesis of 6-alkenyl substituted pyridoxine derivatives has been developed. A series of 31 novel alkenyl pyridoxine derivatives, stilbene-based bioisosteric analogs of estradiol, were synthesized. In vitro cytotoxicity of the obtained compounds against MCF-7 (ER+) breast cancer tumor cells was studied using the MTT assay.

Thiacalixarene based quaternary ammonium salts as promising antibacterial agents.

The search for new antibacterial and antiseptic drugs is an urgent problem due to the resistance of microorganisms to existing drugs. In this work, for the first time, the design of antibacterial and bactericidal agents based on quaternary ammonium compounds on thiacalixarene macrocyclic platform was proposed and implemented. A series of tetrasubstituted quaternary ammonium salts with different nature and length of the substituent (-N(CH)R, R = CHPh, CH, n = 1, 4, 8, 10) based on p-tert-butylthiacalix[4]arene in cone and 1,3-alternate conformations was obtained with excellent yields.