antibiotic resistance

Hygromycin B（Hygrovetine）是一种氨基糖苷类抗生素，可通过干扰易位并导致70S核糖体错误翻译来抑制原核和真核细胞的蛋白质合成，常用于筛选转染有hph或hyg抗性基因的细胞。

Leptomycin B (LMB) 是一种抗真菌抗生素，可阻断真核细胞周期，抑制蛋白出核转运。Leptomycin 通过半胱氨酸残基处的共价修饰使 CRM1 exportin 1失活。

Plazomicin is a next-generation aminoglycoside that has been designed as an antibiotic to avoid resistance through aminoglycoside-modifying enzymes. Plazomicin shows high activity against the Enterobacteriaceae.

Neomycin sulfate (Framycin sulfate) 是一种广谱的氨基糖苷类抗生素。Neomycin sulfate 可以阻断细菌蛋白质的合成以发挥抗菌活性。Neomycin sulfate 常用于筛选具有 Neo 抗性基因的原核和真核细胞。

Chloramphenicol palmitate 是一种广谱抗生素，对革兰氏阳性和革兰氏阴性细菌具有活性。 Chloramphenicol palmitate 可用于在含有氯霉素抗性基因的转化细胞中作为细菌选择剂的研究。

Cinnamoylglycine 是肉桂酸和的甘氨酸结合物，是人体尿液代谢物。它被用作的尿液标志物，能够作为在抗生素研究期之后定殖耐药性的标志物。

Fumitremorgin C (12α-Fumitremorgin C) 是ABCG2 BRCP 的选择性抑制剂。

Quorum sensing-IN-8（compound 5e）具备显著的抗生物膜效果，并可应用于探究抗生素抵抗性问题。

2,5-Di-tert-butyl-1,4-benzoquinone，作为一种强效抗菌剂，主要来源于海洋Streptomyces sp. VITVSK1，有效应对抗菌耐药性问题。此外，该化合物还能作为RNA polymerase的有效抑制剂。

Anti-MRSA agent 19（Compound 1）是一种有效抗金黄色葡萄球菌的抗生素。该化合物对40种CDC分离出的细菌株显示出活性（中位 MIC=4 μg mL），这些细菌株具有不同种类并携带多种耐药性因子，如万古霉素、氨基糖苷类 四环素及恶唑烷酮。

Inh2-B1是一种针对STK1（即Ser Thr蛋白激酶）的抑制剂，通过直接结合到STK1的ATP结合催化区域发挥作用。STK1是金黄色葡萄球菌细胞壁生物合成的重要组成部分，且是导致MRSA耐药性的关键因素。因此，Inh2-B1被视为一种“抗生素耐药性破解剂”，具有阻止生物膜形成的功能。

Laterocidine是一种大环脂肽类抗生素，以其对革兰氏阴性细菌的显著抗菌性能而闻名，尤其是对Pseudomonas aeruginosa和colistin耐药性E. coli的有效性。该化合物也因其低抗生素耐药性发展风险而受到关注。

PKZ18 是一种抗生素 (antibiotic)，通过抑制细菌生长发挥作用，对大多数革兰氏阳性菌的 MIC 值为 32-64 μg mL。它能够抑制甘氨酰-tRNA 合成酶mRNA的体内转录和翻译，选择性地靶向革兰氏阳性菌中的 stem I specifier loops，并有效减少相关基因的 T-box 转录读取。PKZ18 阻止 tRNA 结合所需的密码子-反密码子读取，并具有较低的抗药性发生率。

BAR-072 是一种针对TraE的小分子抑制剂，其KD为2.7 µM。该化合物显著抑制与抗生素耐药性相关的质粒pKM101的转移。BAR-072 有望成为用于抑制细菌耐药基因扩散的候选分子，在抗感染和耐药性控制等疾病研究领域中发挥作用。

FtsZ-IN-13 (Compound C11) 是 FtsZ 的抑制剂，对 FtsZSa 的IC50值为 47.97 μM，对 FtsZPa 为 34 μM。FtsZ-IN-13 对金黄色葡萄球菌 (最低抑菌浓度为 2 μg/mL)、包括囊性纤维化金黄色葡萄球菌临床分离株和耐甲氧西林金黄色葡萄球菌 (MRSA) 显示出很强的抗菌活性。FtsZ-IN-13 可应用于抗菌素耐药性研究。

Plazomicin (ACHN 490) sulfate 是一种有效的氨基糖苷类抗生素，能够对抗抗生素耐药性。其在体外对多种耐多药菌株，如耐卡巴培南类肠杆菌科细菌，展现出活性。Plazomicin sulfate 可用于研究耐多药复杂性尿路感染 (cUTIs) 或联合治疗严重的耐卡巴培南类肠杆菌科细菌感染。

PBP4-IN-1 (Compound 1) 是一种金黄色葡萄球菌青霉素结合蛋白 4 (PBP4) 的抑制剂。它通过抑制 PBP4 的功能增强抗生素对 PBP2a 媒介的耐甲氧西林金黄色葡萄球菌 (MRSA) 的抑制作用。PBP4-IN-1 可用于研究由葡萄球菌引起的骨髓炎，还可用于探讨逆转 PBP4 介导的 β-内酰胺类抗生素耐药性。

Cephamycin C (CepC) is a nontoxic β-lactam antibiotic. CepC stands out from other cephalosporins for its greater resistance to β-lactamases.

Razupenem ( SMP-601, PTZ601) is a broad-spectrum injectable antibiotic derived from the carbapenem subgroup of β-lactam antibiotics. It has been developed as an alternative drug against bacteria that have developed antibiotic resistance to commonly used a

Platensimycin (PTM) is an antibiotic produced by S. platensis that inhibits Gram-positve bacteria by selectively inhibiting cellular lipid biosynthesis (IC50 = 0.1 μM). It targets the β-ketoacyl-acyl-carrier-protein synthase I/II, FabF/B, an enzyme that participates in the biosynthesis of fatty acids (IC50s = 48 and 160 nM for S. aureus and E. coli enzymes, respectively). By specifically targeting fatty acid synthesis in bacteria, PTM is thought to be a promising agent for overcoming antibiotic resistance. PTM is also a selective inhibitor of the mammalian fatty acid synthase and has been shown to reduce liver triglyceride levels and to improve insulin sensitivity in a diabetic mouse model after an oral dose of 30 mg/kg.

Linearmycin A is a polyene antibiotic that has been found inStreptomyces.1It is active against the bacteriaS. aureusandE. coli(MICs = 3.1 and 1.6 μg disc, respectively), the fungiS. cerevisiaeandC. albicans(MICs = 0.1 and 1.6 μg disc, respectively), and the plant pathogenic fungusA. nigerin disc assays (MIC = 0.2 μg disc). Linearmycin A induces lysis and degradation ofB. subtilisas a component ofStreptomycesMg1 extract.2 1.Sakuda, S., Guce-Bigol, U., Itoh, M., et al.Novel linear polyene antibiotics: LinearmycinsJ. Chem. Soc., Perkin Trans. 1182315-2319(1996) 2.Stubbendieck, R.M., and Straight, P.D.Escape from lethal bacterial competition through coupled activation of antibiotic resistance and a mobilized subpopulationPLoS Genet.11(12)e1005722(2015)

Linearmycin B is a polyene antibiotic that has been found inStreptomyces.1It induces lysis and degradation ofB. subtilisas a component ofStreptomycesMg1 extract.2 1.Sakuda, S., Guce-Bigol, U., Itoh, M., et al.Novel linear polyene antibiotics: LinearmycinsJ. Chem. Soc., Perkin Trans. 1182315-2319(1996) 2.Stubbendieck, R.M., and Straight, P.D.Escape from lethal bacterial competition through coupled activation of antibiotic resistance and a mobilized subpopulationPLoS Genet.11(12)e1005722(2015)

Cefsulodin is a β-lactam antibiotic that lyses actively-growingE. coliby binding specifically to the intermembrane proteins, penicillin-binding proteins 1a and b, whose transglycosylase and transpeptidase activities are involved in cell elongation and septation.1Cefsulodin has been used in combination with other β-lactam antibiotics, such as cefazolin as a strategy to circumvent drug resistance.2

CAY10742 is an orally bioavailable oxadiazole antibiotic.1It is active against the Gram-positive bacteriaS. aureus,S. epidermidis,S. haemolyticus,B. cereus,B. licheniformis,E. faecalis, andE. faecium(MICs = 1-4 μg/ml), including laboratory strains and clinical isolates with varying degrees of resistance to methicillin, vancomycin, linezolid, and other antibiotics. CAY10742 (40 mg/kg) reduces the number of bacteria in mouse neutropenic thigh models of linezolid-sensitive or -resistant methicillin-resistantS. aureus(MRSA) infection. 1.Boudreau, M.A., Ding, D., Meisel, J.E., et al.Structure-activity relationship for the oxadiazole class of antibacterialsMed. Chem. Lett.11(3)322-326(2019)