The Anti-MRSA Activity of Phenylthiazoles: A Comprehensive Review

Author:

Kassab Asmaa E.1,Shahin Inas G.2,Mohamed Khaled O.1,Taher Azza T.34,Mayhoub Abdelrahman S.56

Affiliation:

1. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt

2. Department of Organic Chemistry, Faculty of Pharmacy, October University for Modern Sciences and Arts, Giza 11787, Egypt

3. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt;

4. Department of Pharmaceutical Organic Chemistry, College of Pharmacy, October 6 University, 6-October, Giza, Egypt

5. Department of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo 11884, Egypt

6. University of Science and Technology, Nanoscience Program, Zewail City of Science and Technology, October Gardens, 6th October, Giza 12578, Egypt

Abstract

Abstract: Antimicrobial resistance is an aggravating global issue therefore it has been under extensive research in an attempt to reduce the number of antibiotics that are constantly reported as obsolete jeopardizing the lives of millions worldwide. Thiazoles possess a reputation as one of the most diverse biologically active nuclei, and phenylthiazoles are no less exceptional with an assorted array of biological activities such as anthelmintic, insecticidal, antimicrobial, antibacterial, and antifungal activity [1]. Recently phenyl thiazoles came under the spotlight as a scaffold having strong potential as an anti-MRSA lead compound. It is a prominent pharmacophore in designing and synthesizing new compounds with antibacterial activity against multidrug-resistant bacteria such as MRSA, which is categorized as a serious threat pathogen, that exhibited concomitant resistance to most of the first-line antibiotics. MRSA has been associated with soft tissue and skin infections resulting in high death rates, rapid dissemination, and loss of millions of dollars of additional health care costs [2]. In this brief review, we have focused on the advances of phenylthiazole derivatives as potential anti-MRSA from 2014 to 2021. The review encompasses the effect on biological activity due to combining this molecule with various synthetic pharmacophores. The physicochemical aspects were correlated with the pharmacokinetic properties of the reviewed compounds to reach a structure-activity relationship profile. A summary of antibacterial activity of phenylthiazole derivatives against MRSA was added in a tabular form (Table 1). Lead optimization of phenyl thiazole derivatives has additionally been outlined where the lipophilicity of the compounds was balanced with the metabolic stability and oral solubility to aid the researchers in medicinal chemistry, design, and synthesizing effective anti-MRSA phenylthiazoles in the future.

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,Pharmacology

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