gyrase b

SPR719 is an inhibitor of gyrase B, has bactericidal activity.

E.coli Gyrase B-IN-1 (Compound 10g) 是一种E.coli Gyrase B的抑制剂，表现出抗菌活性。其对大肠杆菌 (E. coli) 的抑制作用显著，MIC值为0.12 mM。E.coli Gyrase B-IN-1 在抗菌剂研究中具有潜在应用价值。

DNA gyrase B-IN-1 是 DNA gyrase B 的有效抑制剂，表现出良好的结合亲和力和稳定性。DNA gyrase B-IN-1 能够抑制 P. aeruginosa/i> DNA gyrase B (IC50: 2.2 μM)。

DNA gyrase B-IN-3（Compound A），作为一种细菌DNA gyrase B抑制剂（IC50: <10 nM），针对革兰氏阳性菌株表现出抗菌活性。

DNA gyrase B-IN-2 (Compound E) 是一款基于2-aminobenzothiazole的DNA gyrase B抑制剂，针对ESKAPE病原体显示出强效活性。该化合物在低纳摩尔浓度下表现出优异的DNA gyrase B抑制能力(IC50< 10 nM)，具备对多种ESKAPE病原体的广谱抗菌作用。对于大部分革兰氏阳性菌，最低抑菌浓度(MIC)低于0.03 μg/mL；针对革兰氏阴性病原体如E. coli, Acinetobacter baumannii, Pseudomonas aeruginosa和Klebsiella pneumoniae，MIC为4 - 16 μg/mL。此化合物适用于感染性疾病的研究应用。

DNA gyrase/Topo IV-IN-2 (Compound AK19) 是一种抗菌剂，对 E. coli DNA 旋转酶与拓扑异构酶 IV 的IC50分别为 0.783 μM和 7.136 μM。它对革兰氏阳性与革兰氏阴性病原体呈现广谱抗菌活性，并能抑制 B. subtilis 和 MRSA 的生物膜，其对 B. subtilis 和 MRSA 的MIC为 1.9 μM。此化合物适用于研究抗耐药菌药物。

Flumequine-13C3is intended for use as an internal standard for the quantification of flumequine by GC- or LC-MS. Flumequine is a fluoroquinolone antibiotic.1It is active againstS. aureus, S. pyogenes, B. subtilis, E. coli, P. aeruginosa, S. faecalis, andK. pneumoniae(MICs = 1-100 μg/ml). Flumequine is also active against field isolates of B. hyodysenteriae (MICs = 6.25-200 μg/ml).2It inhibits DNA gyrase, disrupting supercoiling of bacterial DNA to block transcription and replication.3In vivo, flumequine (50 mg/kg) increases survival in rat models ofP. vulgaris-induced urinary tract infection andP. mirabilis-induced prostatitis.1Formulations containing flumequine have been used in the treatment of urinary tract infections in veterinary medicine. 1.Rohlfing, S.R., Gerster, J.R., and Kvam, D.C.Bioevaluation of the antibacterial flumequine for urinary tract useAntimicrob. Agents Chemother.10(1)20-24(1976) 2.Aller-Morán, L.M., Martínez-Lobo, F.J., Rubio, P., et al.Evaluation of the in vitro activity of flumequine against field isolates of Brachyspira hyodysenteriaeRes. Vet. Sci.10351-53(2015) 3.Smith, J.T.The mode of action of 4-quinolones and possible mechanisms of resistanceJ. Antimicrob. Chemother.18 (Suppl. D)21-29(1986)

Dihydronovobiocin is a coumarin antibiotic and derivative of novobiocin .1It is active against the bacteriaS. aureus,S. haemolyticus,D. pneumoniae,S. typhosa,K. pneumoniae, andP. multocida(MICs = 0.6, 2, 0.6, 10, 10, and 3 μg/ml, respectively).2Dihydronovobiocin inhibits DNA gyrase subunit B with an IC50value of 64.5 nM.3 1.Berger, J., and Batcho, A.D.Coumarin - glycoside antibioticsJ. Chromatogr. Lib.15101-158(1978) 2.Hoeksema, H.Dihydronovobiocin and derivatives thereof3,175,9441-9(1965) 3.Gevi, M., and Domenici, E.A scintillation proximity assay amenable for screening and characterization of DNA gyrase B subunit inhibitorsAnal. Biochem.300(1)34-39(2002)

Antibacterial agent 98 (compound g37) 是口服有效的抗菌剂，可以抑制 Gyrase B 的 ATP 酶活性并削弱金黄色葡萄球菌 (S. aureus )的DNA 超螺旋。Antibacterial agent 98 不会诱导 MRSA (耐甲氧西林金黄色葡萄球菌 (S. aureus)) 的耐药性发展。

DNA Gyrase-IN-3 (Compound 28) 是细菌DNA 旋转酶 B (bacterial DNA gyrase B) 抑制剂。DNA Gyrase-IN-3抑制大肠杆菌DNA 旋转酶的 IC50为5.41-15.64 μM。DNA Gyrase-IN-3显示出抗结核和抗菌活性。

DNA Gyrase-IN-2 是细菌 DNA 促旋酶 B 抑制剂，能作用于大肠杆菌 DNA 促旋酶(IC50: 3.29-10.49 μM)和结核分枝杆菌 DNA 促旋酶(IC50: 4.41-5.61 μM)，表现出抗菌和抗结核作用。

QSL-304为一种DNA旋转酶B抑制剂，并具有抗菌作用，其对金黄色葡萄球菌sa-P2003的IC50值为31.23 mg/mL。

Zoliflodacin (ETX0914) 是一种新型螺旋嘧啶三酮，对革兰氏阳性和阴性生物有抗菌活性，对金黄色葡萄球菌的b>MIC90值为0.25 μg/mL。他也是细菌DNA 促旋酶/拓扑异构酶的抑制剂。

Chebulinic acid 是从诃子果中提取的一种天然产物，结核分枝杆菌 DNA 促旋酶的有效抑制剂。它也能抑制 SMAD-3 phosphorylation 和 H+ K+-ATPase 的活性。