Pyrrolnitrin is an antibiotic isolated from Pseudomonas pyrrocinia. Pyrrolnitrin shows a broad spectrum of antibiotic activity against fungi, yeast and gram-positive bacteria[1].
Marbofloxacin is a potent antibiotic of which depends upon its inhibition of DNA-gyrase. Marbofloxacin is a synthetic, broad spectrum bactericidal agent.Target: DNA-gyraseMarbofloxacin is a third-generation fluoroquinolone for veterinary use, the antimicrobial of which depends upon its inhibition of DNA-gyrase and topoisomerase IV. With a broad spectrum bactericidal activity and good efficacy, marbofloxacin is indicated for dermatological, respiratory and urinary tract infections due to both Gram-positive and Gram-negative bacteria and Mycoplasma [1].Administration of Marbofloxacin at 6 mg/kg once daily for 7 days in a Staphylococcus aureus infection in tissue cages in ponies is not effective for the elimination of S. aureus infections from secluded sites [2]. The pharmacokinetic properties of marbofloxacin were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed for bacteria isolated from equine infectious pathologies. The clearance of marbofloxacin was mean +/- s.d. 0.25 +/- 0.05 l/kg/h and the terminal half-life 756 +/- 1.99 h. The marbofloxacin absolute bioavailabilities after subcutaneous and oral administration were 98 +/- 11% and 62 +/- 8%, respectively. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus [3]. Toxicity: cramps; vomiting; anorexia; soft stools; diarrhoea
Halocarban is a chemical with antibacterial properties sometimes used in deodorant and soap[1].
Proanthocyanidins are a class of polyphenols with antibacterial, antifungal and antiviral activities, which can be used in the treatment of chronic venous insufficiency, capillary fragility, sunburn and retinopathy.
Linopristin is a kind of type B streptogramin antibiotics. Linopristin, together with type A, Flopristin, to form the streptogramin combination NXL 103. Linopristin exhibit synergistic antimicrobial activity against certain pathogenic bacteria with Flopristin. The preference ratio of Linopristin/Flopristin is 30:70 (w/w) or 70 μM Linopristin +120 μM Flopristin[1].
Ceftaroline fosamil is a cephalosporin with activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA).
GNF179 is an optimized 8,8-dimethyl IP analog that exhibited the potency(4.8 nM against the multidrug resistant strain W2) in vitro metabolic stability and in vivo oral bioavailability.IC50 value: 4.8 nM [1]Target: Anti-parasitic agent GNF179 exhibits a low clearance (CL=22 ml/min/kg, ~25% of hepatic blood flow in mice), a large volume of distribution (steady-state volume of distribution, Vss=11.8 l/kg), a moderate residence time (MRT=9 hours) and suitable terminal half-life (t1/2=8.9 hours). GNF179 reduced Plasmodium berghei parasitemia levels by 99.7% with a single 100 mg/kg oral dose, and prolonged mouse survival by an average of 19 days. GNF179 was able to protect against an infectious P. berghei sporozoite challenge with a single oral dose at 15 mg/kg while NITD609 was not.
Quinine sulfate (2:1) (Qualaquin) is an orally active alkaloid extracted from cinchona bark and can be used in anti-malarial studies. Quinine sulfate (2:1) is a potassium channel inhibitor that inhibits WT mouse Slo3 (KCa5.1) channel currents evoked by voltage pulses to +100 mV with an IC50 of 169 μM[1][2].
Majoranaquinone exhibits a high antibacterial effect against 4 Staphylococcus, 1 Moraxella, and 1 Enterococcus strains. Majoranaquinone shows substantial efflux pump inhibitory activity in Escherichia coliATCC 25922 strain. Majoranaquinone is found to be an effective biofilm formation inhibitor on E.coli, ATCC 25922 and E. coli K-12 AG100 bacteria[1].
Toonaciliatin M (compound 6) is a pmaradiene-type diterpenoid that can be isolated from Toona ciliate. Toonaciliatin M show antifungal activity against Trichophyton rubrum with an MIC value of 12.5 µg/mL[1].
Malabaricone B, a naturally occurring plant phenolic, is an orally active α-glucosidase inhibitor with an IC50 of 63.7 µM. Malabaricone B has anticancer, antimicrobial, anti-oxidation and antidiabetic activities[1][2][3].
Melilotigenin C can be isolated from genus Erythrina. Melilotigenin C can be used for research on antiplasmodial activity, antimycobacterial activity and cytotoxicity[1].
Tritrpticin is an antimicrobial peptide derived from pig bone marrow. Tritrpticin shows activity against Aspergillus fumigatus and Candida albicans (MIC=250 and 1000 μg/ml, respectively)[1].
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env[1][2].
Chitin synthase inhibitor 3 (compound 2d) is a potent chitin synthase inhibitor with an IC50 value of 0.16 mM, and MIC of 1 µg/mL against candida albicans. Antifungal activity[1].
Ys-II (Compound 1) is a spirostanol glycoside that can be isolated from the stem of Yucca elephantipe. Ys-II has antifungal activity against the growth of Candida albicans and Cryptococcus neoformans (IC50: 5 and 6 μg/mL respectively)[1].
cis-ccc_R08 (compound 1) is a flavonoid derivative that can be used in the study of hepatitis B virus (HBV) infection. cis-ccc_R08 is a cccDNA (covalently closed circular DNA) inhibitor[1].
Chloramphenicol palmitate is an orally active broad spectrum antibiotic and has a broad spectrum of activity against gram positive and gram negative bacteria. Chloramphenicol palmitate inhibits bacterial protein synthesis by blocking the peptidyl transferase step. Chloramphenicol palmitate can be used as bacterial selection agent in transformed cells containing chloramphenicol resistance genes[1].
Euptox A (9-Oxo-10, 11-dehydroageraphorone), a cadenine sesquiterpene, is the main toxin that can be isolated from Eupatorium adenophorum. Euptox A induces apoptosis by improving the gene expression level of apoptotic proteases such as caspase-10 in HeLa cells[1].
Nucleozin targets influenza A nucleoprotein (NP), a multifunctional, RNA-binding protein necessary for virus replication. IC50 Value: Target: Influenza Virus NPNucleozin targets influenza A nucleoprotein, a multifunctional, RNA-binding protein necessary for virus replication. It induces the formation of nucleoptotein aggregates and inhibits its accumulation, interfering with viral replication. EC50 is in the nM range. Nucleozin is effective in H1N1, H3N2, and H5N1 flu virus strains.
Isosativan is a natural product that can be found in Trifolium hybridum. Isosativan shows antifungal activity[1].
10,11-Dehydrocurvularin is a prevalent fungal phytotoxin and an antibiotic. 10,11-Dehydrocurvularin is a strong activator of the heat shock response. 10,11-Dehydrocurvularin inhibits TGF-β signalling pathway. Anti-tumorous activity[1][2].
Sapienic acid is a fatty acid commonly found on the skin and in mucosa. Sapienic acid has variable antimicrobial activities against Gram-positive and Gram-negative bacteria found on the skin and in the oral cavity. Sapienic acid is active against Streptococcus sanguinis, Streptococcus mitis and Fusobacterium nucleatum with MBC values of 31.3 μg/mL, 375.0 μg/mL and 93.8 μg/mL, respectively[1].
Natamycin (pimaricin) is an antifungal macrolide polyene that binds to cell membrane sterols.Target: AntifungalNatamycin (INN), also known as pimaricin and sometimes sold as Natacyn, is a naturally occurring antifungal agent produced during fermentation by the bacterium Streptomyces natalensis, commonly found in soil. Natamycin has a very low solubility in water; however, natamycin is effective at very low levels. There is an MIC (minimum inhibitory concentration) of less than 10 ppm for most molds. Natamycin is classified as a macrolide polyene antifungal and, as a drug, is used to treat fungal keratitis. It is especially effective against Aspergillus and Fusarium corneal infections. Other common members of the polyene macrolide antifungal family are amphotericin B, nystatin, and filipin. Natamycin is also used in the food industry as a natural preservative.Natamycin is used to treat fungal infections, including Candida, Aspergillus, Cephalosporium, Fusarium and Penicillium. It is applied as a cream, in eyedrops, or (for oral infections) in a lozenge. Natamycin shows negligible absorption into the body when administered in these ways. When taken orally, little or none is absorbed from the gastrointestinal tract, making it inappropriate for systemic infections.
CB2R/FAAH modulator-3 (compound 27) is a dual targeting modulator that acts as a CB2R agonist and FAAH inhibitor. The Ki values for CB2R/FAAH modulator-3 are 20.1 and 67.6 nM for CB2R and CB1R, respectively, and the IC50 value for FAAH is 3.4 μM. CB2R/FAAH modulator-3 can be used in studies related to cancer, deleterious inflammatory cascades occurring in neurodegenerative diseases, and COVID-19 infection[1].
Norfloxacin nicotinate (MK-0366 nicotinate) is a fluoroquinolones antibiotic, an adduct of Norfloxacin (NOR) and nicotinic acid. Norfloxacin nicotinate has been widely used for replacing NOR in animal husbandry and fishery industry. Norfloxacin nicotinate can induce innate immune response at a high concentration[1].
Usaramine is a pyrrolizidine alkaloid isolated from seeds of Crolatalaria pallida. Usaramine demonstrates a highlighted antibiofilm activity against Staphylococcus epidermidis by reducing more than 50% of biofilm formation without killing the bacteria[1].
KAMP-19, a keratin-derived antimicrobial peptide, is an antimicrobial peptide against P. aeruginosa. [1].
Adeninobananin, a negative control tool, does not show any inhibitory activity of the SARS Coronavirus helicase.
Antiparasitic agent-8 (Compound 9) is an antiparasitic agent against Hymenolepis nana with low cytotoxicity[1].