Sorbic acid, isolated from Sorbus aucuparia, is a naturally occurring, highly efficient, and nonpoisonous food preservative. Sorbic acid generally is an effective inhibitor of most molds and yeasts and some bacteria[1].
Tigecycline hydrochloride is a first-in-class, broad spectrum antibiotic with activity against antibiotic-resistant organisms.Target: AntibacterialTigecycline hydrochloride is active against a broad range of gram-negative and gram-positive bacterial species including clinically important multidrug-resistant nosocomial and community-acquired bacterial pathogens. Tigecycline hydrochloride has been shown to inhibit the translation elongation step by binding to the ribosome 30S subunit and preventing aminoacylated tRNAs to accommodate in the ribosomal A site [1]. Tigecycline hydrochloride has also been found to be effective for the treatment of community- as well as hospital-acquired and ventilator-associated pneumonia and bacteremia, sepsis with shock and urinary tract infections. Tigecycline hydrochloride appears to be a valuable treatment option for the management of superbugs, especially where conventional therapy has failed [2].Fifteen patients received tigecycline hydrochloride for 16 episodes of CPKP infection. The main infections were pneumonia (31%), urinary tract infection (31%), peritonitis (20%), catheter-related bacteraemia (12%), and meningitis (6%). Most infections were complicated with severe sepsis (44%), septic shock (12%), and/or bacteraemia (19%). The daily maintenance dose of tigecycline hydrochloride was 200 mg in 10 episodes and 100 mg in 6 episodes. The overall 30-day mortality rate was 25%. Univariate analysis showed that mortality was significantly associated (p < 0.01) with mean APACHE II and SOFA scores and the presence of immunosuppression, but not with the tigecycline hydrochloride dose [3].Clinical indications: Acinetobacter infection; Bacterial infection; Bacterial pneumonia; Bacterial skin infection; Bacteroides fragilis infection; Bacteroides infection; Citrobacter infection; Clostridiaceae infection; Clostridium difficile infection; Clostridium infection; Enterobacter infectionFDA Approved Date: June 17, 2005 Toxicity: nausea; vomiting; diarrhea; local IV-site reaction; infection; fever; headache
Imipenem monohydrate, a member of the carbapenem class of antibiotics isolated from the soil organism Streptomyces cattleya[1], is an intravenous β-lactam antibiotic effective against a wide range of Gram-positive and Gram-negative bacteria, including several multi-drug resistant bacterial species. Imipenem acts as cell wall-targeting antibiotic[2][3].
Lauric acid-d23 is the deuterium labeled Lauric acid. Lauric acid is a middle chain-free fatty acid with strong bactericidal properties. The EC50s for P. acnes, S.aureus, S. epidermidis, are 2, 6, 4 μg/mL, respectively.
Edoxudine is an antiviral drug, is an analog of thymidine, shows effectiveness against herpes simplex virus.
Sulfadiazine sodium belongs to the class of sulfonamide antibiotics that are used for veterinary purposes worldwide, mainly in pig production. Sulfadiazine sodium is also used for toxoplasmosis[1][2].
Robinetin (3,3',4',5',7-Pentahydroxyflavone), a naturally occurring flavonoid with remarkable ‘two color’ intrinsic fluorescence properties, has antifungal, antiviral, antibacterial, antimutagenesis, and antioxidant activity. Robinetin also can inhibit lipid peroxidation and protein glycosylation[1][2][3][4][5].
Florfenicol amine hydrochloride is a metabolite of Florfenicol (HY-B1374). Florfenicol inhibits bacterial protein synthesis by binding to 50S and 70S subunits in the ribosome to abolish the activity of peptidyltransferase. Florfenicol, is a veterinary antibiotic, can be used in aquaculture to control susceptible bacterial diseases[1][2].
(-)-Corypalmine (Discretinine), an alkaloid that could be isolated from the stem of Guatteriopsis friesiana, possesses antimicrobial activity[1].
Anti-inflammatory agent 11 (compound 16) is a potent antimycobacterial and anti-inflammatory agent. Anti-inflammatory agent 11 inhibits Mtb H37Rv and M299 growth, with MIC50 (minimum inhibitory concentration 50%) of 1.3 and 6.9 μM, respectively. Anti-inflammatory agent 11 inhibits NO through the suppression of iNOS expression, and also inhibited the production of TNF-α and IL-1β. Anti-inflammatory agent 11 can be used for tuberculosis (TB) research[1].
Cathepsin G(1-5) is an antimicrobial peptide that can be found in the clostripain-digested cathepsin G mixture[1].
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al[1].
Cochliodone A is an active compound extracted from cultures of the deep-sea derived fungus Chaetomium sp. and has antibacterial and anticancer activity. Cochliodone A is toxic to a variety of bacteria, with MICs of 15.3 μg/mL (V. vulnificus), 32.7 μg/mL (V. rotiferianus), 15.9 μg/mL (S. aureus ATCC 43300), and 16.3 μg/mL (S . aureus CGMCC 1.12409). Cochliodone A also inhibits a variety of cancer cell lines, with IC50s of 28.1 μM (A549), 20.7 μM (HeLa), and 23.2 μM (Hep G2)[1].
Tobramycin sulfate (Nebramycin Factor 6 sulfate) is a parenterally administered, broad spectrum aminoglycoside antibiotic that is widely used in the treatment of moderate to severe bacterial infections due to sensitive organisms[1].
Acetylazide is a synthetic broad-spectrum bacteriostatic antibiotic.
Saccharothrixin K, a glycosylated saccharothrixin, shows moderate inhibition against Helicobacter pylori G27, H. pylori 159, and Staphylococcus aureus ATCC25923 with MIC values of 16 μg/mL[1].
Pazufloxacin (T-3761) is a fluoroquinolone antibiotic.Target: AntibacterialPazufloxacin (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus [1]. T-3761 had a broad spectrum of activity and had potent activity against gram-positive and -negative bacteria. The MICs of T-3761 against 90% of the methicillin-susceptible Staphylococcus aureus, methicillin-susceptible and -resistant Staphylococcus epidermidis, and Clostridium spp. tested were 0.39 to 6.25 micrograms/ml. The MBCs of T-3761 were either equal to or twofold greater than the MICs. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively [2].
S.pombe lumazine synthase-IN-1 is an inhibitor of lumazine synthases with Ki values of 243 μM and 9.6 μM for Schizosaccharomyces pombe and Mycobacterium tuberculosis lumazine synthases, respectively[1].
Octacosane is an endogenous metabolite with antibacterial activity. Octacosane shows high cytotoxicity against murine melanoma B16F10-Nex2 cells besides inducing protection against a grafted subcutaneous melanoma. Octacosane has the larvicidal activity against mosquito Culex quinquefasciatus with the LC50 concentration of 7.2 mg/l[1][2][3].
Pseudouridimycin (PUM), an antibiotic, is a selective bacterial RNA polymerase (RNAP) inhibitor. Pseudouridimycin is a C-nucleoside analogue that is effective against both Gram-negative and Gram-positive bacteria[1].
Sulfamethazine sodium (Sulfadimidine sodium) is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections). In China and the European Commission, the maximum residue level for Sulfamethazine sodium in animal product is set at 100 µg/kg[1][2].
Antistaphylococcal agent 1 is an antistaphylococcal therapeutic agent.
BO3482 has Antimicrobial activity and can inhibit the growth of methicillin-resistant Staphylococci (MRS) with an MIC90 of 6.25 mg/mL.
Fmoc-Glu-OMe a glutamic acid derivative, shows antibacterial activity and gelation property in AgNO3 solution. Fmoc-Glu-OMe is a mouldable wound healing biomaterial[1].
Doripenem monohydrate is a new member of the carbapenem class of beta-lactam antibiotics with broad-spectrum coverage of Gram-positive, Gram-negative and anaerobic pathogens.Target: AntibacterialDoripenem is an ultra-broad-spectrum injectable antibiotic. It is a beta-lactam and belongs to the subgroup of carbapenems. It was launched by Shionogi Co. of Japan under the brand name Finibax in 2005 and is being marketed outside Japan by Johnson & Johnson. It is particularly active against Pseudomonas aeruginosa. It is recommended that those allergic to doripenem or to any type of beta-lactam antibiotics such as cephalosporin or other Carbapenems not receive doripenem.Doripenem appears as crystalline powder anywhere from a white to somewhat yellowish colour.Doripenem is moderately soluble in water, slightly soluble in methanol, and virtually insoluble in ethanol. Doripenem is also solution in N,N-dimethylformamide. Doripenem's chemical configuration has 6 asymmetrical carbon atoms (6 stereocentres) and is most commonly supplied as one pure isomer. In terms of doripenem for injection, the crystallized powered drug can form a monohydrate when mixed with water. However, Doripenem has not been proven to possess polymorphism.
Metallo-beta-lactamase ligand 1 is a class B β-lactamase inhibitor with antibacterial activity extracted from patent WO2019221122A1, compound A[1].
Pazufloxacin (T-3761) mesylate is a fluoroquinolone antibiotic.Target: AntibacterialPazufloxacin (T-3761), a new quinolone derivative, showed broad and potent antibacterial activity. T-3761 showed good efficacy in mice against systemic, pulmonary, and urinary tract infections with gram-positive and gram-negative bacteria, including quinolone-resistant Serratia marcescens and Pseudomonas aeruginosa. The in vivo activity of T-3761 was comparable to or greater than those of ofloxacin, ciprofloxacin, norfloxacin, and tosufloxacin against most infection models in mice. The activities of T-3761 were lower than those of tosufloxacin against gram-positive bacterial systemic and pulmonary infections in mice but not against infections with methicillin-resistant Staphylococcus aureus [1]. T-3761 had a broad spectrum of activity and had potent activity against gram-positive and -negative bacteria. The MICs of T-3761 against 90% of the methicillin-susceptible Staphylococcus aureus, methicillin-susceptible and -resistant Staphylococcus epidermidis, and Clostridium spp. tested were 0.39 to 6.25 micrograms/ml. The MBCs of T-3761 were either equal to or twofold greater than the MICs. The 50% inhibitory concentrations of T-3761 for DNA gyrases isolated from E. coli and P. aeruginosa were 0.88 and 1.9 micrograms/ml, respectively [2].
Antibacterial agent 54 (example 20) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
Defensin HNP-3 human is a cytotoxic antibiotic peptide known as "defensin". Defensin HNP-3 human has inhibitory activity against Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. Defensin HNP-3 human is initially synthesized as the 94 amino acids preproHNP(1-94), which is hydrolyzed to proHNP(20-94) and converted to mature HNP(65-94) after the removal of anion precursors[1][2].
4(3H)-Quinazolinone is a building block in chemical synthesis. Biologically active nitrogen heterocyclic compounds. Possesses a wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant, anti-inflammatory, anti-HIV, anticancerous and analgesic activities[1][2].