3-Arylpropenoyl-adamantane amides: Synthesis, structural determin | 60881
Journal of Proteomics & Bioinformatics

Journal of Proteomics & Bioinformatics
Open Access

ISSN: 0974-276X

3-Arylpropenoyl-adamantane amides: Synthesis, structural determination and biological activity

18th World Congress on Structural Biology

September 28, 2022 | Webinar

Assoc Prof Dr. Maya Chochkova

South-West University ā??ā??Neofit Rilskiā??ā?? Blagoevgrad, Bulgaria

Scientific Tracks Abstracts: J Proteomics Bioinform

Abstract :

The emergence and spread of drug-resistant pathogens, including bacteria, viruses, fungi and parasites continues to threaten not only humans, but also animals, and plants [1]. Antimicrobial resistance (AMR) is responsible for more than 1 million death. Particularly, antiviral drug resistance is an increasing concern, especially in immunocompromised patients, due to their permanent treating with antiviral therapies [2]. WHO prognosticates that AMR could lead to 10 million deaths per year by 2050? However, it is known that two-thirds to three-fourths of cases of acute respiratory illness are virusinduced [3]. Therefore, finding of new alternative therapies, and the development of new antivirals is a hot topic. Adamantane nucleus is a key pharmacophore, used in creation of a diverse library of compounds with antimicrobial, neuroprotective, antimalarial, anti-inflammatory, and etc. [4]. The purpose of our study is to evaluate antiviral effects of 3-Arylpropenoylamides (described in Fig.1) against three Influenza strains A/FortMonmouth/1/1947; A/Jinnan/15/2009; A/Wuhan/359/1995. The amides were prepared in sufficiently yields by TBTU couplings [5]. Ther structures were entirely characterized by melting points and spectroscopic data (UV, IR, 1H NMR, 13C NMR, HRMS). The geometry of –CH=CH- side chain of desired compounds was assigned as an (E)-ļ°-diastereomeric form on the basis of J values (>15.0 Hz) in the 1H NMR spectra. Methodology & Theoretical Orientation: The virus-induced CE was recorded when the CPE of virus control group reached 4, and IC50 of drugs were determined using Reed and Muench method. Findings: In general, in comparison with clinically used antiviral drugs (oseltamivir and ribavirin), the group of hybrids shows weaker antiviral activity against the influenza strains tested. Conclusion & Significance: Amongst the tested adamantane hybrids, emerges N-sinapoylmemantine and thienyl-adamantane, which suppressed the viral replication of both strain A/FortMonmouth/1/1947 and A/Wuhan/359/1995, whereas they are resistant against strain A/Jinnan/15/2009

Biography :

Maya Chochkova has her expertise in the field of discovery of novel biologically active compounds by chemical modification of natural compounds (cinnamic acids, peptides, amino acids, alkaloids) or drugs (anti-influenza, anti-Alzheimer) using conventional and green methodologies. Furthermore, her scientific interest is devoted to in vitro evaluation of anti-tyrosinase, anti-glucosidase and radical scavenging activities of the novel compounds. Currently, she is Assoc. Professor in Organic Chemistry at the South-West University “Neofit Rilski”, Blagoevgrad, Bulgaria.