Discovery of a novel class of small-molecule antibacterial agents against Staphylococcus aureus

被引：3

作者：

Kreutzer, David ^{[1
]}

Gehrmann, Robin ^{[1
]}

Kincses, Annamaria ^{[2
]}

Szemeredi, Nikoletta ^{[2
]}

Spengler, Gabriella ^{[2
]}

Molnar, Josef ^{[2
]}

Hilgeroth, Andreas ^{[1
]}

机构：

[1] Martin Luther Univ Halle Wittenberg, Inst Pharm, D-06120 Halle, Germany

[2] Univ Szeged, Dept Med Microbiol, H-6720 Szeged, Hungary

来源：

FUTURE MEDICINAL CHEMISTRY | 2022年 / 14卷 / 05期

关键词：

antibacterial activity; inhibitor; structure-activity; substituent; synthesis; ANTIBIOTIC-RESISTANCE; MULTIDRUG-RESISTANCE; THERAPY; TUBERCULOSIS; INFECTIONS;

D O I：

10.4155/fmc-2021-0272

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: With constantly increasing resistance against the known antibiotics, the search for novel antibacterial compounds is a challenge. The number of synthetic antibacterial agents is limited. Materials & methods: We discovered novel small-molecule antibacterial agents that are accessible via a simple two-step procedure. The evaluation against Staphylococcus aureus showed antibacterial effects depending on the substituent positioning at the residues of the molecular scaffold. Additionally, we investigated the potential of the compounds to increase the antibacterial activity of tetracycline. Results: The most effective antibacterial compounds possessed a 3-methoxy function at an aromatic residue. In combination with tetracycline, we found a strong effect for a few compounds in boosting the antibacterial activity, so the first promising lead compounds with dual activities could be identified.

引用

页码：299 / 306

页数：8

共 37 条

[1] Antimicrobial resistance mechanisms and potential synthetic treatments [J].

Ali, Junaid ;

Rafiq, Qasim A. ;

Ratcliffe, Elizabeth .

FUTURE SCIENCE OA, 2018, 4 (04)

[2] Antimicrobial resistance and a diminishing pool of reserved antibiotics [J].

Altaf, Ihsan Ullah Khan ;

Khan, Ahmad ;

Mahboob, Amjad .

SAO PAULO MEDICAL JOURNAL, 2019, 137 (04) :384-385

[3] Natural products in drug discovery: advances and opportunities [J].

Atanasov, Atanas G. ;

Zotchev, Sergey B. ;

Dirsch, Verena M. ;

Supuran, Claudiu T. .

NATURE REVIEWS DRUG DISCOVERY, 2021, 20 (03) :200-216

[4] New antibiotics and antimicrobial combination therapy for the treatment of gram-negative bacterial infections [J].

Bassetti, Matteo ;

Righi, Elda .

CURRENT OPINION IN CRITICAL CARE, 2015, 21 (05) :402-411

[5] Staphylococcus aureus soft tissue infection may increase the risk of subsequent staphylococcal soft tissue infections [J].

Bouvet, Cindy ;

Gjoni, Shpresa ;

Zenelaj, Besa ;

Lipsky, Benjamin A. ;

Hakko, Elif ;

Uckay, Ilker .

INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES, 2017, 60 :44-48

[6] Treatment of HIV-related tuberculosis in the era of effective antiretroviral therapy [J].

Burman, WJ ;

Jones, BE .

AMERICAN JOURNAL OF RESPIRATORY AND CRITICAL CARE MEDICINE, 2001, 164 (01) :7-12

[7] Recent Progress in the Development of Small-Molecule FtsZ Inhibitors as Chemical Tools for the Development of Novel Antibiotics [J].

Carro, Laura .

ANTIBIOTICS-BASEL, 2019, 8 (04)

[8] Origin and Proliferation of Multiple-Drug Resistance in Bacterial Pathogens [J].

Chang, Hsiao-Han ;

Cohen, Ted ;

Grad, Yonatan H. ;

Hanage, William P. ;

O'Brien, Thomas F. ;

Lipsitch, Marc .

MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS, 2015, 79 (01) :101-116

[9] Effect of xylitol, sodium fluoride and triclosan containing mouth rinse on Streptococcus mutans [J].

Subramaniam, Priya ;

Nandan, N. .

CONTEMPORARY CLINICAL DENTISTRY, 2011, 2 (04) :287-290

[10]

Davis M., 2017, INT FARM ANIMAL

← 1 2 3 4 →