Chlorhexidine diacetate is a biguanide disinfectant with rapid bactericidal activity against both Gram-positive and Gram-negative organism. The antibacterial effect of chlorhexidine diacetate is related to its action on the bacterial cell membrane and to precipitation of intracellular contents[1].
Bictegravir is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
Esculentin 1A is a frog skin-derived antimicrobial peptide (AMP) with potent in vitro anti-Pseudomonas activity[1].
Piperlonguminine is an alkaloid amide isolated from the Piper species. Piperlonguminine shows various biological properties, including anti-inflammatory, antitumor, neuroprotective, anti-platelet, anti-melanogenic, antifungal and antibacterial activities[1][2][3][4].
GS-6620 is a HCV nonstructural protein 5B (NS5B) inhibitor.
Lactobionic acid is a bionic acid naturally found in the Caspian Sea yogurt and chemically constituted of a gluconic acid bonded to a galactose. Lactobionic acid has antioxidant, antimicrobial, chelating, stabilizer, acidulant, and moisturizing properties[1].
Chlorothalonil is a broad spectrum fungicide and is effective in protecting plants against fungal diseases caused mainly by Phytophthora infestans and Alternaria solani. Chlorothalonil is used for controlling of fungal foliar diseases of vegetables and crops[1][2].
N-(Hydroxymethyl)nicotinamide is an antimicrobic agent[1].
Iodobananin is an effective inhibitor of the ATPase activity of the SARS Coronavirus helicase with an IC50 value of 0.54 μM.
G-418 (Geneticin) is an aminoglycoside antibiotic with a structure similar to gentamicin. It is toxic to both eukaryotic and prokaryotic cells and works by interfering with protein synthesis[1].
Ofloxacin-d8 (Hoe-280-d8) is the deuterium labeled Ofloxacin. Ofloxacin (Hoe-280) is a fluoroquinolone whose primary mechanism of action is inhibition of bacterial DNA gyrase.
Cephalexin (Cefalexin) lysine is a derivative of Cephalexin with lysine. Cephalexin is a potent, orally active and the first-generation cephalosporin antibiotic. Cephalexin kills gram-positive and some gram-negative bacteria by disrupting the growth of the bacterial cell wall. Cephalexin monohydrate is used for the research of pneumonia, strep throat, and bacterial endocarditis, et al[1].
Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS)[1].
Sinapaldehyde, isolated from the stems of Rhodamnia dumetorum, exhibits moderate antibacterial against Methicillin resistant S. aureus (MRSA) and E. coli with MIC values of 128 and 128 μg/mL[1].
(1R)-Tenofovir amibufenamide ((1R)-HS-10234) is the isomer of Tenofovir amibufenamide, is an orally active antiviral agent. (1R)-Tenofovir amibufenamide ((1R)-HS-10234) is a HIV infection inhibitor and HBV infection inhibitor. (1R)-Tenofovir amibufenamide ((1R)-HS-10234) can be used for HIV infections, hepatitis B research[1].
Pyrrolnitrin is an antibiotic isolated from Pseudomonas pyrrocinia. Pyrrolnitrin shows a broad spectrum of antibiotic activity against fungi, yeast and gram-positive bacteria[1].
trans-Cinnamic acid-d5 is the deuterium labeled trans-Cinnamic acid[1]. trans-Cinnamic acid is a natural antimicrobial, with minimal inhibitory concentration (MIC) of 250 μg/mL against fish pathogen A. sobria, SY-AS1[2].
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).
Retro-indolicidin is a biological active peptide. (Reverse peptide of indolicidin (Rev4) is a 13-amino acid residue peptide based on the sequence of indolicidin. Indolicidin, a member of the cathelicidin protein family, is a 13-amino acid residue cationic, antimicrobial peptide-amide isolated from the cytoplasmic granules of bovine neutrophils. The synthetic peptide Rev4 has been shown to possess strong antimicrobial as well as protease inhibitory activities in vitro.)
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.
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].
Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.
Undecanoic acid-d3 is the deuterium labeled Undecanoic acid. Undecanoic acid (Undecanoate) is a monocarboxylic acid with antimycotic property, which inhibits the production of exocellular keratinase, lipase and the biosynthesis of several phospholipids in T. rubrum[1].
Melilotigenin C can be isolated from genus Erythrina. Melilotigenin C can be used for research on antiplasmodial activity, antimycobacterial activity and cytotoxicity[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].