NSC 55655 (5-[(2-Nitrophenyl)methylene]-2,4-thiazolidinedione) 具有抗菌和抗氧化活性,抑制 B. subtilis, S. aureus, K. pneumonia, E. coli, S. typhi ,A. niger 和 C. albicans 的增殖,可用于糖尿病。
Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains(MIC of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively).
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。
Frequentin, an antibiotic originally isolated from P. frequentans, is active against bacteria (MICs = 200 and 300 µg/ml for B. subtilis and S. aureus, respectively) and fungi.
Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1]
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)
Deoxyviolacein is a bacterial metabolite and byproduct in the biosynthesis of the bisindole alkaloid violacein that has anticancer, antibacterial, and antifungal properties. It inhibits proliferation of hepatocellular carcinoma cells when used at concentrations ranging from 0.1 to 1 μM. Deoxyviolacein (125 μg/ml) has antibacterial activity against Gram-positive bacteria, including S. aureus, B. subtilis, and B. megaterium. It also has antifungal activity against R. solani when used at a concentration of 2 mg/ml.
17-hydroxy Venturicidin A is a macrolide fungal metabolite originally isolated from Streptomyces. It has antibiotic activity against M. luteus, B. subtilis, and S. aureus and antifungal activity against V. dahlia, Fusarium, and C. tropicalis in a disc assay.
Thiocoraline is a depsipeptide and DNAbis-intercalator originally isolated fromMicromonosporawith antibacterial and anticancer activities.1,2It is active against the Gram-positive bacteriaS. aureus,B. subtilis, andM. luteus(MICs = 0.05, 0.05, and 0.03 μg/ml, respectively) but not Gram-negativeE. coli,K. pneumoniae, orP. aeruginosa(MICs = >100 μg/ml for all).1Thiocoraline inhibits RNA and DNA polymerase and thymidylate synthase (IC50s = 6, 6, and 15 μg/ml, respectively), as well as RNA and DNA synthesisin vitro(IC50s = 0.008 and 0.4 μg/ml, respectively). It is cytotoxic to P388, A549, HT-29, and MEL-28 cancer cells (IC50s = 0.002, 0.002, 0.01, and 0.002 μg/ml, respectively).
1.Romero, F., Espilego, F., Pérez Baz, J., et al.Thiocoraline, a new depsipeptide with antitumor activity produced by a marine Micromonospora. I. Taxonomy, fermentation, isolation, and biological activitiesJ. Antibiot. (Tokyo)50(9)734-737(1997) 2.Negri, A., Marco, E., García-Hernández, V., et al.Antitumor activity, X-ray crystal structure, and DNA binding properties of thiocoraline A, a natural bisintercalating thiodepsipeptideJ. Med. Chem.50(14)3322-3333(2007)