Novel Hemocompatible Imine Compounds as Alternatives for Antimicrobial Therapy in Pharmaceutical Application

Mohammad A Altamimi,Abdulmalik Alnami,Afzal Hussain,Ahmed Bari,Syed Sarim Imam,Sultan Alshehri

doi:10.3390/pr8111476

Mohammad A Altamimi, Abdulmalik Alnami + Show 4 more

Open Access

https://doi.org/10.3390/pr8111476

Copy DOI

Journal: Processes	Publication Date: Nov 17, 2020
Citations: 8	License type: CC BY 4.0

Affiliation: King Saud University, Alfaisal University

Abstract

The aim of this study was to synthesize, characterize, and evaluate neoteric imine compounds for antimicrobial activity and hemocompatibility. Four compounds were synthesized using 3-thiophene carboxaldehyde, ethanol, amine, and acetic acid. The compounds were characterized using nuclear magnetic resonance (NMR) spectroscopy, Fourier transform infrared (FTIR) spectroscopy, differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). A solubility study was conducted with various solvents and surfactants at 40 °C. An in vitro antimicrobial assay was performed against bacterial and fungal strains to determine the zone of inhibition and minimum inhibitory concentrations. Finally, an in vitro hemolysis study was conducted using rat erythrocytes. The structure of the compounds was confirmed by NMR, FTIR corroborated their functional group attributes, DSC determined their enthalpies of fusion and fusion temperatures, and PXRD confirmed their crystalline nature. These compounds were water-insoluble but soluble in chloroform, with a maximum solubility of ~80 mg/mL. The antimicrobial assay suggested that two of the products exerted potent activities against C. albicans and several bacterial strains. Finally, hemolysis analysis excluded the possibility of hemolysis at the assessed concentrations. In conclusion, two of the novel imine compounds showed promise as antimicrobial agents to control local and systemic microbial infections in a suitable dosage form.

Highlights

Bacteria and fungi are the most prevalent microbes on earth, a great variety of which coexists as versatile commensals with mammals
Considering the diverse biological activities of imines and chemistry, we describe synthesis thiophene-3-carboxaldehyde has been used to synthesize piperidine analogs for thethe treatment of of new analogs derived from the reaction of primary with thiophene-3-carboxaldehyde
The introduction of pharmacophores in formyl heterocycles has been shown to result in biologically introduction of pharmacophores in formyl heterocycles has been shown to result in biologically active analogs [36]

Summary

Introduction

Bacteria and fungi are the most prevalent microbes on earth, a great variety of which coexists as versatile commensals with mammals. These interactions can be both beneficial and detrimental to human health, depending on numerous microbial- and host-related factors. The exhaustive use of antibiotics and antifungal drugs has led to the emergence of drug resistance over time, thereby negating their efficacy. The emergence of resistant strains has greatly challenged the clinical application of several drugs to Processes 2020, 8, 1476; doi:10.3390/pr8111476 www.mdpi.com/journal/processes. Processes 2020, 8, 1476 negating their efficacy. The emergence of resistant strains has greatly challenged the clinical application of several drugs to control bacterial and fungal infections. Other factors (climate, ethnicity, habitat, diet, and diversity) can(climate, alter host susceptibility to control bacterial andgenetics, fungal infections

Objectives

Methods

Results

Conclusion