The Anti-MRSA Activity of Phenylthiazoles: A Comprehensive Review
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作者:
Shahin, Inas G. G.
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October Univ Modern Sci & Arts, Fac Pharm, Dept Organ Chem, Giza 11787, EgyptOctober Univ Modern Sci & Arts, Fac Pharm, Dept Organ Chem, Giza 11787, Egypt
Shahin, Inas G. G.
[1
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Mohamed, Khaled O. O.
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Cairo Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Cairo 11562, EgyptOctober Univ Modern Sci & Arts, Fac Pharm, Dept Organ Chem, Giza 11787, Egypt
Mohamed, Khaled O. O.
[2
]
Taher, Azza T. T.
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Cairo Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Cairo 11562, Egypt
October 6 Univ, Coll Pharm, Dept Pharmaceut Organ Chem, 6 October, Giza, EgyptOctober Univ Modern Sci & Arts, Fac Pharm, Dept Organ Chem, Giza 11787, Egypt
Taher, Azza T. T.
[2
,3
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Mayhoub, Abdelrahman S. S.
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Al Azhar Univ, Coll Pharm, Dept Pharmaceut Organ Chem, Cairo 11884, Egypt
Univ Sci & Technol, Nanosci Program, Zewail City Sci & Technol, October Gardens,6th October, Giza 12578, EgyptOctober Univ Modern Sci & Arts, Fac Pharm, Dept Organ Chem, Giza 11787, Egypt
Mayhoub, Abdelrahman S. S.
[4
,5
]
Kassab, Asmaa E. E.
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Cairo Univ, Fac Pharm, Dept Pharmaceut Organ Chem, Cairo 11562, EgyptOctober Univ Modern Sci & Arts, Fac Pharm, Dept Organ Chem, Giza 11787, Egypt
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
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.
机构:
Chinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China
Univ Chinese Acad Sci, Coll Life Sci, Beijing, Peoples R ChinaChinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China
Li, Chao
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Bao, Wuyundalai
Zhang, Haoyue
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Hebei Univ, Coll Life Sci, Inst Life Sci & Green Dev, Key Lab Microbial Div Res & Applicat Hebei Prov, Baoding, Peoples R ChinaChinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China
Zhang, Haoyue
Lyu, Zhitang
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Hebei Univ, Coll Life Sci, Inst Life Sci & Green Dev, Key Lab Microbial Div Res & Applicat Hebei Prov, Baoding, Peoples R ChinaChinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China
Lyu, Zhitang
Chen, Yihua
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Chinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China
Univ Chinese Acad Sci, Coll Life Sci, Beijing, Peoples R ChinaChinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China
Chen, Yihua
Guo, Zhengyan
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Chinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China
Univ Chinese Acad Sci, Coll Life Sci, Beijing, Peoples R ChinaChinese Acad Sci, CAS Key Lab Microbial Physiol & Metab Engn, Inst Microbiol, State Key Lab Microbial Resources, Beijing, Peoples R China