Difloxacin is an antimicrobial agent[1].
Anisofolin A is a flavonoid that can be isolated from Anisomeles indica. Anisofolin A has antimalarial activity (IC50: 4.39 μM), and antimycobacterium activity (IC50: 4.50 μM) against M. tuberculosis H37Ra[1].
A mixture of uvaretin and isouvaretin (HY-N10130) exhibits significant antibacterial activity against B. subtilis (EC50 8.7 μM) and S. epidermidis (IC50 7.9 μM).
PqsR/LasR-IN-3 (Compound 7a) is a potent inhibitor of PqsR and LasR systems in P. aeruginosa. PqsR/LasR-IN-3 also inhibits hERG with the IC50 of 109.01 µM[1].
Benzothiohydrazide is an analogue of anti–tubercular agent Isoniazid. Benzothiohydrazide exhibits anti–tubercular activity, with MICs of 132 μM and 264 μM for M. tuberculosis wild type (H37Rv) and clinical mutant strains (IC1 and IC2)[1].
MurA-IN-4 has antibacterial activity and is a MurA inhibitor that inhibits bacterial cell wall synthesis[1].
Bedaquiline is a diarylquinoline antibiotic that inhibits mycobacterial ATP synthase.
Octyl gallate (Progallin O) is widely used as a food additive, with antimicrobial and antioxidant activity[1][2]. Octyl gallate (Progallin O) shows selective and sensitive fluorescent property[2].
Rabeprazole Sulfide is an active metabolite of Rabeprazole. Rabeprazole is a proton pump inhibitor that suppresses gastric acid secretion through an interaction with (H+/K+)-ATPase in gastric parietal cells. Rabeprazole markedly inhibits the motility of H. pylori. Rabeprazole has the potential for various peptic diseases treatment[1][2].
Almurtide (nor-MDP), a muramyl dipeptide derivative with anti-inflammatory and anti-tumor activity. Almurtide also shows protective effects against intraperitoneal Pseudomonas aeruginosa infection or intravenously Candida albicans infection in mice. Almurtide also inhibits the carcinogenic Friend leukemia virus[1][2][3].
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains[1][2].
MCB-3681 is the antibacterial Oxaquin's active substance, active against gram-positive bacterium[1].
Tunicamycin is a N-acetylglucosamine containing antibiotic from Streptomyces lysosuperijkus which inhibits protein glycosylation.
Moxalactam sodium salt is an antibiotic compound more effective against Escherichia coli and Pseudomonas aeruginosathan cephalosporins.
Methyl 2-amino-5-bromobenzoate (compound 8/12) can be used for synthesis of 2-benzamidobenzoic acids, which are known FabH inhibitors. The derivates also inhibit PqsD, the pqs quorum sensing (QS) system of Pseudomonas aeruginosa, involving the production of a number of virulence factors and biofilm formation[1].
7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae)[1]. 7-O-Methylaloeresin A exhibits good activity against multiple drug resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively[2].7-O-Methylaloeresin A has antioxidant activities, gives IC50 values of 0.026 mM and 0.021 mM for DPPH and 2-deoxyribose degradation assay, respectively[2].
Cyclosporin C is a fungal metabolite that has been found in T. inflatum and has diverse biological activities, including antifungal, antiviral, and immunosuppressant properties. Cyclosporin C is active against isolates of B. cinerea, A. niger, and Alternaria, Mucor, and Penicillium species (MICs=0.1-5 μg/ml).
Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase[1][2].
Antitubercular agent-32 is a derivate of Benzothiazinone (HY-13579A), inhibits M. tuberculosis, and shows improved metabolic stability and enhanced water solubility. Antitubercular agent-32 exerts antitubercular effect by targeting decaprenylphosphoryl-β-D-ribose 2’-oxidase (DprE1, IC50=3.9 μM)[1].
Protein kinase G inhibitor-2 (Compound 266) is a mycobacterial protein kinase G inhibitor, with an IC50 of 3 μM. Protein kinase G inhibitor-2 can be used for mycobacterial infection research[1].
pleuromutilin inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit of bacteria.
Penthiopyrad(MTF-753) is a carboxamide fungicide used to control a broad spectrum of diseases on large variety of corps; inhibits fungal respiration by binding to mitochondrial respiratory complex II.
Sulfasymazine is a sulfonamide drug and displays antibacterial properties.
5-hydroxypyrazine-2-carboxylic acid , a metabolite of anti-tuberculosis drug pyrazinamide (PZA).
Aurein 2.2 is a major component of the skin secretion of L.aurea. Aurein 2.2 is an antibiotic with broad-spectrum antibacterial activity against Gram positive bacteria such as Staphylococcus aureus and S. epidermidis[1][2].
Isoniazid is an antibacterial agent used primarily as a tuberculostatic.Target: AntibacterialIsoniazid is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme that in M. tuberculosis is called KatG [1]. KatG couples the isonicotinic acyl with NADH to form isonicotinic acyl-NADH complex. This complex binds tightly to the enoyl-acyl carrier protein reductase known as InhA, thereby blocking the natural enoyl-AcpM substrate and the action of fatty acid synthase. This process inhibits the synthesis of mycolic acid, required for the mycobacterial cell wall. A range of radicals are produced by KatG activation of isoniazid, including nitric oxide, which has also been shown to be important in the action of another antimycobacterial prodrug PA-824 [2, 3]. Isoniazid is bactericidal to rapidly dividing mycobacteria, but is bacteriostatic if the mycobacteria are slow-growing [4].
Rifaximin-d6 is the deuterium labeled Rifaximin. Rifaximin is an orally administered, semi-synthetic, nonsystemic antibiotic derived from rifamycin SV with antibacterial activity[1][2].
Girinimbine (Girinimbin) is a carbazole alkaloid with a variety of biological effects. Girinimbine can induce apoptosis, and has antitrypanosomal, antiplatelet activity, antibacterial activity, anti-inflammatory, antioxidant and antitumor activities[1][2][3].
Tigecycline-d9 is deuterium labeled Tigecycline. Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL[1]. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively[2].
Moxifloxacin is a synthetic fluoroquinolone antibiotic agent.Target: AntibacterialMoxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. The antibacterial spectrum of moxifloxacin includes all major upper and lower respiratory tract pathogens; it is one of the most active fluoroquinolones against pneumococci, including penicillin- and macrolide-resistant strains [1]. Moxifloxacin has limited phototoxic potential. In clinical trials, moxifloxacin had clinical success rates of 88-97% and bacteriologic eradication rates of 90-97%. Moxifloxacin is a safe and effective antimicrobial that will be useful for treating acute sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia [2]. Moxifloxacin possibly stimulates lipid peroxidation and enhances phagocytosis, as depicted by MDA production and survival prolongation, without being toxic as depicted by white blood cell count [3]. Clinical indications: Abdominal abscess; Acute bronchitis; Acute sinusitis; Bacterial infectionToxicity: Symptoms of overdose include CNS and gastrointestinal effects such as decreased activity, somnolence, tremor, convulsions, vomiting, and diarrhea. The minimal lethal intravenous dose in mice and rats is 100 mg/kg.