The Anti-MRSA Activity of Phenylthiazoles: A Comprehensive Review

被引:0
作者
Shahin, Inas G. G. [1 ]
Mohamed, Khaled O. O. [2 ]
Taher, Azza T. T. [2 ,3 ]
Mayhoub, Abdelrahman S. S. [4 ,5 ]
Kassab, Asmaa E. E. [2 ]
机构
[1] October Univ Modern Sci & Arts, Fac Pharm, Dept Organ Chem, Giza 11787, Egypt
[2] Cairo Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Cairo 11562, Egypt
[3] October 6 Univ, Coll Pharm, Dept Pharmaceut Organ Chem, 6 October, Giza, Egypt
[4] Al Azhar Univ, Coll Pharm, Dept Pharmaceut Organ Chem, Cairo 11884, Egypt
[5] Univ Sci & Technol, Nanosci Program, Zewail City Sci & Technol, October Gardens,6th October, Giza 12578, Egypt
关键词
Anti-MRSA; phenylthiazoles; antibiotic resistance; pharmacokinetics; vancomycin; oxadiazoles; pyrimidines; RESISTANT STAPHYLOCOCCUS-AUREUS; METHICILLIN-RESISTANT; ANTIBACTERIAL ACTIVITY; OXADIAZOLE LINKER; ANTIBIOTICS; DERIVATIVES; THIAZOLES; DISCOVERY; DESIGN; POTENT;
D O I
10.2174/1381612829666221124112006
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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. 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. 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. 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.
引用
收藏
页码:3469 / 3477
页数:9
相关论文
共 81 条
  • [1] [Anonymous], 2017, World Health Organization Report
  • [2] [Anonymous], 2017, GLOB ANT RES SURV SY
  • [3] Synthesis of some novel N4-(naphtha[1,2-d]thiazol-2-yl)semicarbazides as potential anticonvulsants
    Azam, Faizul
    Alkskas, Ismail A.
    Khokra, Sukhbir Lal
    Prakash, Om
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (01) : 203 - 211
  • [4] New antibiotics for bad bugs: where are we?
    Bassetti, Matteo
    Merelli, Maria
    Temperoni, Chiara
    Astilean, Augusta
    [J]. ANNALS OF CLINICAL MICROBIOLOGY AND ANTIMICROBIALS, 2013, 12
  • [5] Bad Bugs, No Drugs: No ESKAPE! An Update from the Infectious Diseases Society of America
    Boucher, Helen W.
    Talbot, George H.
    Bradley, John S.
    Edwards, John E., Jr.
    Gilbert, David
    Rice, Louis B.
    Scheld, Michael
    Spellberg, Brad
    Bartlett, John
    [J]. CLINICAL INFECTIOUS DISEASES, 2009, 48 (01) : 1 - 12
  • [6] Structure-Activity Relationship for the 4(3H)-Quinazolinone Antibacterials
    Bouley, Renee
    Ding, Derong
    Peng, Zhihong
    Bastian, Maria
    Lastochkin, Elena
    Song, Wei
    Suckow, Mark A.
    Schroeder, Valerie A.
    Wolter, William R.
    Mobashery, Shahriar
    Chang, Mayland
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2016, 59 (10) : 5011 - 5021
  • [7] Antibacterial activity of indolyl-quinolinium derivatives and study their mode of action
    Cai, Senyuan
    Yuan, Wenchang
    Li, Ying
    Huang, Xuanhe
    Guo, Qi
    Tang, Ziwei
    Fang, Zhiyuan
    Lin, Hai
    Wong, Wing-Leung
    Wong, Kwok-Yin
    Lu, Yu-Jing
    Sun, Ning
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2019, 27 (07) : 1274 - 1282
  • [8] Synthesis and activity of sulfonamide-substituted 4,5-diaryl thiazoles as selective cyclooxygenase-2 inhibitors
    Carter, JS
    Kramer, S
    Talley, JJ
    Penning, T
    Collins, P
    Graneto, MJ
    Seibert, K
    Koboldt, CM
    Masferrer, J
    Zweifel, B
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 1999, 9 (08) : 1171 - 1174
  • [9] Centers for Disease Control and Prevention (CDC), 2019, Antibiotic Resistance Threats in the United States, 2019
  • [10] Community-associated MRSA - Resistance and virulence converge
    Chambers, HF
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 2005, 352 (14) : 1485 - 1487