Buforin II, derived from buforin I, a protein isolated from the stomach of the Asian toad Bufo bufo gargarizans, is a potent antimicrobial peptide. Buforin II has antimicrobial activity against a broad spectrum of Gram-positive and Gram-negative bacteria[1].
Hexachlorophene(Hexachlorofen) is a potent KCNQ1/KCNE1 potassium channel activator with EC50 of 4.61 ± 1.29 μM; also is an inhibitor of Wnt/beta-catenin signaling.IC50 value: 4.61 ± 1.29 μM(EC50) [1]Target: KCNQ1 activatorin vitro: HCP potently increases the current amplitude of KCNQ1/KCNE1 expressed by stabilizing the channel in an open state with an EC(50) of 4.61 ± 1.29 μM. Further studies in cardiomyocytes showed that HCP significantly shortens the action potential duration at 1 μM. In addition, HCP is capable of rescuing the loss of function of the LQTs mutants caused by either impaired activation gating or phosphatidylinositol-4,5-bisphosphate (PIP2) binding affinity [1]. Hexachlorophene antagonized CRT that was stimulated by Wnt3a-conditioned medium by promoting the degradation of beta-catenin. hexachlorophene represses the expression of cyclin D1 [2]. Triclosan and hexachlorophene inhibited both ecFabI and saFabI. hexachlorophene prevented the formation of a stable FabI-NAD(P)(+)-drug ternary complex [3].
1,3,7-Trihydroxy-2-prenylxanthone, a xanthone, shows weaker antibacterial activity. 1,3,7-Trihydroxy-2-prenylxanthone exhibits the MIC value of 6.25 mg/ml against VREs strains (E. faecalis, E. faecium, and E. gallinarum)[1].
FAAL-IN-1 (compound 32) is a selective inhibitor of fatty acyl-AMP ligase (FAAL), with a Ki of 0.7 μM for FAAL28. FAAL-IN-1 shows antimycobacterial activity[1].
Antibacterial agent 114 (compound 1) is a potent antibacterial agent. Antibacterial agent 114 shows antibacterial activity against P.aeruginosa, B.subtilis, E.coli, E.faecalis, S.typhimuriumand, S.mutans, and S.aureus microorganisms, with MIC values of 625, 625, 625, 625, 625, 1250 and 1250 μM, respectively[1].
Antibacterial agent 53 (example 19) is a antibacterial agent (extracted from patent WO2013030735A1)[1].
NOSO-502 (NOSO502) is a novel inhibitor of bacterial translation, has MIC values of 0.5-4 ug/ml against standard Enterobacteriaceae strains and carbapenem-resistant Enterobacteriaceae (CRE) isolates that produce KPC, AmpC, or OXA enzymes and metallo-β-lactamases; interacts strongly with a specific site on the 30S subunit of bacterial ribosomes but has no significant activity against any of the 55 cell surface receptors, transporters, or ion channels; NOSO-502 is active against a panel of Gram-positive and Gram-negative bacteria, including carbapenem-resistant and polymyxin-resistant strains, and exhibits promising in vivo activity in various murine infection models, a favorable in vitro safety profile, and a low potential for resistance development.
Rifaquizinone (CBR-2092) is a Rifamycin-Quinolone Hybrid Antibiotic. Rifaquizinone inhibits wild-type S. aureus RNA polymerase with an IC50 of 34 nM. Rifaquizinone is effective against S. aureus infections, with MICs ranged from 0.008 to 0.5 μg/mL for 300 clinical isolates of staphylococci and streptococci[1][2].
Cephalothin sodium is a first generation cephem antibiotic with a wide range antibacterial activity, is active against gram-positive and gram-negative bacteria.
L18-MDP is a derivative of muramyl dipeptide, an antibacterial agent. L18-MDP has antibacterial activity and has potential applications in bacterial and fungal infections[1].
Ethylparaben-d4 is the deuterium labeled Ethylparaben[1].
Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity[1][2].
Temafloxacin (TMFX) hydrochloride is an orally active quinolone broad-spectrum antibacterial agent. Temafloxacin hydrochloride is well tolerated in lower respiratory and genitourinary tract infections[1][2].
Aurein 2.3 is an antibiotic antimicrobial peptide. Aurein 2.3 partially inhibits E.coli ATPase activity and inhibits cell growth[1][2].
d-Atabrine dihydrochloride is an active enantiomer of quinacrine which displays antiprion activity.
Himastatin is a antitumor antibiotic produced by a strain of S. hygroscopicus sp. Himastatin is a dimeric cyclohexadepsipeptide containing piperazic acid and a unique central aromatic core[1].
Netilmicin Sulfate is an active aminoglycoside antibiotic against most Gram-negative and some Gram-positive bacteria, including certain strains resistant to gentamicin.
Novel Inhibitor of Bacterial Cytokinesis, inhibiting FtsZ
Sulfamerazine Sodium is a sulfonamide antibacterial.Target: AntibacterialSulfamerazine, the monomethyl derivative of sulfadiazine, is 2-sulfanilamido-4-methylpyrimidine. Sulfamerazine is a sulfonamide drug that inhibits bacterial synthesis of dihydrofolic acid by competing with para-aminobenzoic acid (PABA) for binding to dihydropteroate synthetase (dihydrofolate synthetase). Sulfamerazine is bacteriostatic in nature. Inhibition of dihydrofolic acid synthesis decreases the synthesis of bacterial nucleotides and DNA [1].
Allergen Gal d 4 (46-61), chicken is a hen egg white lysozyme peptide.
1-Methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone is a potent antibacterial agent with an MIC50 value of 22 µM and an MIC90 value of 50 µM for Helicobacter pyloriStrain 51. 1-Methyl-2-(8E)-8-tridecenyl-4(1H)-quinolinone has the potential for the research of gastric and duodenal ulcers[1].
Polyphemusin I is a natural antimicrobial peptide with excellent antimicrobial activity against Gram-negative and Gram-positive bacteria. Polyphemusin I contains 18 amino acids and is stabilized into an amphiphilic, antiparallel β-hairpin by two disulfide bridges[1].
Phleomycin is a wide-spectrum glycopeptide antibiotic found in Streptomyces verticillus. Phleomycin, an effective DNA-cleaving agent, binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A)[1].
TH-Z145, a lipophilic bisphosphonate, is a FPPS inhibitor (IC50: 210 nM)[1].
Tobramycin is an aminoglycoside, broad-spectrum antibiotic produced by Streptomyces tenebrarius.Target: AntibacterialTobramycin is an aminoglycoside antibiotic derived from Streptomyces tenebrarius and used to treat various types of bacterial infections, particularly Gram-negative infections. It is especially effective against species of Pseudomonas [1]. Tobramycin works by binding to a site on the bacterial 30S and 50S ribosome, preventing formation of the 70S complex. As a result, mRNA cannot be translated into protein and cell death ensues. Tobramycin is preferred over gentamicin for Pseudomonas aeruginosa pneumonia due to better lung penetration. From Wikipedia [2].
Cyproconazole is a triazole fungicide that is used agriculturally for protection of crops against a wide variety of fungal pathogens.In vitro: Cyproconazole has been shown to cause a dose dependent inhibition of progesterone production in human placental cells in vitro. cyproconazole exhibited the lowest capacity to increase CYP1A1 and were not able to activate the AhR in the transactivation assay. [1]In vivo: Cyproconazole, a triazole fungicide, causes hepatocellular adenomas and carcinomas in CD-1 mice at dose levels of 100 and 200 ppm. In wild-type mice, 200 ppm cyproconazole caused liver hypertrophy, increased liver weight and cell proliferation, single-cell necrosis and fat vacuolation. [2]
Salannin, a limonoid bitter principle of the seed oil of Azadirachta indica, shows antiulcer and spermicidal activities. Salannin displays antibacterial activity towards both Gram-positive and Gram-negative bacteria[1][2].
Antitubercular agent-14 (Compound 1) is an antitubercular agent with an MIC of 0.3 µg/mL against M. tuberculosis[1].