A5024375675- Carbohydrate Chemistry and Synthesis
- Synthesis and Biological Evaluation
- Synthesis and Reactions of Organic Compounds
- Bioactive Compounds and Antitumor Agents
- Cancer therapeutics and mechanisms
- Synthesis and biological activity
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis of Organic Compounds
- Fluorine in Organic Chemistry
- Microbial Natural Products and Biosynthesis
- Chemical Synthesis and Analysis
- Synthesis of Indole Derivatives
- Antimicrobial Resistance in Staphylococcus
- Biochemical and Molecular Research
- Phenothiazines and Benzothiazines Synthesis and Activities
- DNA and Nucleic Acid Chemistry
- Click Chemistry and Applications
- Quinazolinone synthesis and applications
- Glycosylation and Glycoproteins Research
- Cancer Treatment and Pharmacology
- Organophosphorus compounds synthesis
- Asymmetric Synthesis and Catalysis
- HIV/AIDS drug development and treatment
- Analytical Chemistry and Chromatography
- Genomics, phytochemicals, and oxidative stress
Gause Institute of New Antibiotics Russian Academy of Medical Sciences
2009-2018
Russian Academy of Sciences
2004-2016
Academy of Medical Sciences
1988-2014
Institute of Biomedical Chemistry
2010
SINTEF
2008
Vavilov Institute of General Genetics
2008
Norwegian University of Science and Technology
2008
United States Army Medical Research Institute of Infectious Diseases
2007
National Defense Medical Center
2006
KU Leuven
2003-2005
A comprehensive comparative analysis of the structure-antifungal activity relationships for series biosynthetically engineered nystatin analogues and their novel semisynthetic derivatives, as well amphotericin B (AMB) its was performed. The data obtained revealed significant influence structure C-7 to C-10 polyol region on antifungal these polyene antibiotics. Comparison positions hydroxyl groups in antibiotics vitro showed that most active are compounds which C-8 C-9 or C-10. Antibiotics...
Solid-state NMR has been used to examine isolated cell walls and intact whole cells of Staphylococcus aureus complexed five different vancomycin, eremomycin, chloroeremomycin derivatives. The were specifically labeled with d-[1-13C]alanine, or a combination [1-13C]glycine [ε-15N]lysine. Each the bound glycopeptides had 19F-labeled substituent at either its C-terminus disaccharide position. 13C{19F} rotational-echo double-resonance (REDOR) dephasing for cell-wall 13C-labeled bridging...
There is an urgent need for potent inhibitors of dengue virus (DENV) replication the treatment and/or prophylaxis infections with this virus. We here report on aglycon analogue antibiotic teicoplanin (code name LCTA-949) that inhibits DENV-induced cytopathic effect (CPE) in a dose-dependent manner. Virus infection was completely inhibited at concentrations had no adverse host cells. These findings were corroborated by quantification viral RNA levels culture supernatant. Antiviral activity...
The review is devoted to the latest achievements in design of dual action antibiotics ? heterodimeric (chimeric) structures based on antibacterial agents different classes (fluoroquinolones, anthracyclines, oxazolidines, macrolides and so on). Covalent binding can make pharmacokinetic characteristics these molecules more predictable improve penetration each component into cell. Consequently, not only does drug efficacy increase owing inhibition two targets but also resistance one or both be...
Background: The ability of boron-containing compounds to undergo a number novel binding interactions with drug target functional groups has recently been described. In an extension this work, we have incorporated scaffold, the benzoxaborole, into several glycopeptides antibiotics. aim work is exploit inherent reactivity boron gain additional bacterial cell wall components improve affinity and thereby overcome resistance. Results: Three antibacterial (vancomycin, eremomycin teicoplanin...
A series of new 4,11-diaminoanthra[2,3-b]furan-5,10-dione derivatives with different side chains were synthesized. Selected 2-unsubstituted 11-14 showed high antiproliferative potency on a panel mammalian tumor cell lines including multidrug resistance variants. Compounds utilized multiple mechanisms cytotoxicity inhibition Top1/Top2-mediated DNA relaxation, reduced NAD(+)/NADH ratio through tNOX inhibition, suppression NAD(+)-dependent sirtuin 1 (SIRT1) deacetylase activity, and activation...
A variety of semisynthetic derivatives natural antibacterial glycopeptide antibiotics such as vancomycin, eremomycin, ristocetin A, teicoplanin A2-2, DA-40926, their aglycons, and also the products partial degradation with a destroyed or modified peptide core show marked anti-retroviral activity in cell culture. In particular, aglycon antibiotic containing various substituents preferably hydrophobic nature displayed against human immunodeficiency virus type 1 (HIV-1), HIV-2, Moloney murine...
CONTENTS I. Introduction 753 II. Methods of preparation indolines 754 III. substituents into the benzene ring indoline molecule 758 IV. pyrrole 763 V. Conversion derivatives indoles 764
Aminomethylation of 9b,10-dihydro-1H-indolo[1,7:4,5,6]pyrrolo[3,4:2,3][1,4]diazepino-[1,7-a]indole-1,3(2H)-diones or 1H-indolo[1,7:4,5,6]pyrrolo[3,4:2,3][1,4]diazepino[1,7-a]indole-1,3(2H)-diones resulted in dialkylaminomethyl derivatives. Alkylation the nitrogen atom maleimide moiety polyannelated diazepines with 1,3-dibromopropane and subsequent reaction thiourea its N-alkyl derivatives gave isothiourea-carrying compounds. The compounds containing isothiourea were active against individual...
Twenty-three new derivatives of the heptaene nystatin analogue 28,29-didehydronystatin A1 (1) (S44HP) were obtained by chemical modification C16 carboxyl and amino groups mycosamine. These comprised 15 carboxamides, 4 N-alkyl derivatives, 3 N-derivatives containing additional N-linked monosaccharide or disaccharide moiety (products Amadori rearrangement), 1 N-aminoacyl derivative. The have been tested in vitro against yeasts Candida albicans, Cryptococcus humicolus, filamentous fungi (molds)...
The review summarizes advances in the methods for synthesis of polyene antibiotics (amphotericin B, partricin A, etc.) and investigations structure–activity relationship made last 15 years. State-of-the-art approaches based on combination chemical genetic engineering are considered. Emphasis is given to design semisynthetic antifungal agents against chemotherapy-resistant pathogens having highest therapeutic indices. Recent results research mechanisms action polyenes outlined.
Ten protein kinase C (PKC) isozymes play divergent roles in signal transduction. Because of sequence similarities, it is particularly difficult to generate isozyme-selective small molecule inhibitors. In order identify such a selective binder, we derived pharmacophore model from the peptide EAVSLKPT, fragment PKCε that inhibits interaction and receptor for activated C-kinase 2 (RACK2). A database 330 000 molecules was screened silico, leading discovery series thienoquinolines disrupt with...
Staphylococcus aureus grown in the presence of an alanine-racemase inhibitor was labeled with d-[1-(13)C]alanine and l-[(15)N]alanine to characterize some details peptidoglycan tertiary structure. Rotational-echo double-resonance NMR intact whole cells used measure internuclear distances between (13)C (15)N amino acids incorporated peptidoglycan, from those labels (19)F a glycopeptide drug specifically bound peptidoglycan. The observed (13)C-(15)N average distance 4.1-4.4 Å d- l-alanines...