2,6-Dichlorodiphenylamine is an analogue of Diclofenac Sodium (HY-15037) and has anti-Candida albicans activity. Diclofenac Sodium is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells.
Tedizolid is a novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome.
Taurolidine is a broad-spectrum antimicrobial for the prevention of central venous catheter-related infections. Taurolidine has a direct and selective antineoplastic effect on brain tumor cells by the induction of apoptosis[1].
Methylisothiazolinone-d3 (hydrochloride) is the deuterium labeled Methylisothiazolinone (hydrochloride). Methylisothiazolinone hydrochloride is the constituent of the biocide Kathon CG. Methylisothiazolinone hydrochloride is an isothiazolone derivative widely used as a preservative. Methylisothiazolinone hydrochloride is also a moderate sensitizer and reacts with GSH.
AcrB-IN-1 (Compound H6) is a potent AcrB inhibitor. AcrB-IN-1 can be used for the reversal of bacterial multidrug resistance[1].
NAG-thiazoline is a O-GlcNAcase inhibitor with a Ki of 180 nM. NAG-thiazoline is a potent GH20 GlcNAcase (VhGlcNAcase) inhibitor with an IC50 of 11.9 μM and a Ki of 62 µM[1].
SABA1 possesses antibacterial properties against Pseudomonas aeruginosa and Escherichia coli, with an IC50 of 4.0 µM against E. coli ACC[1].
Fusidic acid (Fusidate) is a bacteriostatic antibiotic[1][2][3].
Vitamin D3-d3 is the deuterium labeled Vitamin D3. Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.
Urease is produced by many types of bacteria and is an effective virulence factor for some pathogenic bacteria. Urease is also central to the metabolism and virulence of Helicobacter pylori, helping it colonize the stomach lining[1].
Gatifloxacin (hydrochloride) is an antibiotic of the fourth-generation fluoroquinolone family, it inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.Target: AntibacterialGatifloxacin (hydrochloride) is the hydrochloride salt of Gatifloxacin which is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Gatifloxacin had activity equal to that of tosufloxacin and activity more potent than those of norfloxacin, ofloxacin, ciprofloxacin, and sparfloxacin against the second-step mutants (grlA gyrA; gatifloxacin MIC range, 1.56 to 3.13 microg/ml) and had the most potent activity against the third-step mutants (grlA gyrA grlA; gatifloxacin MIC range, 1.56 to 6.25 microg/ml), suggesting that gatifloxacin possesses the most potent inhibitory activity against singly mutated topo IV and singly mutated DNA gyrase among the quinolones tested [1].Ophthalmic gatifloxacin 0.3% is at least as effective as ciprofloxacin at healing corneal ulcers infected with Pseudomonas aeruginosa when gatifloxacin is administered less frequently than ciprofloxacin. Trends favored gatifloxacin in fluorescein retention scores [2].Clinical indications: Bacterial infection FDA Approved Date: Toxicity: Hepatotoxicity; Acute pancreatitis [3]; Torsades de pointes [4]
Aurein 1.1 is an antibiotic peptide that can be found in the Australian Bell Frogs Litoria raniformis[1].
Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.Target: AntibacterialEthambutol directly affects two polymers, arabinogalactan (AG) and lipoarabinomannan (LAM) in Mycobacterium smegmatis. In M. smegmatis, Ethambutol inhibits synthesis of arabinan completely and inhibits AG synthesis most likely as a consequence of this; more than 50% of the cell arabinan is released from the bacteria following Ethambutol treatment, whereas no galactan is released. Ethambutol main targets against embB gene product in M. avium. Ethambutol induces 60% changes in the embB gene in M. tuberculosis resistant mutants [1]. Ethambutol is effective against actively growing microorganisms of the genus Mycobacterium, including M. tuberculosis. Nearly all strains of M. tuberculosis and M. kansasii as well as a number of strains of the M. aviumcomplex (MAC) are sensitive to Ethambutol. [1] Ethambutol is potency against M. tuberculosis (H37Rv) with MIC of 0.5 μg/mL in vitro [2]. Ethambutol is efficient on treatment of mycobacterial-infected macrophages. When M. tuberculosis infected macrophages are treated with 6 μg/mL Ethambutol, the log CFUs following treatment for 3 days is 4.17, while value in control group is 4.8. The MICs for M. avium (MTCC 1723) and M. smegmatis (MTCC 6) are 15 μg/mL and 0.18 μg/mL, respectively. Ethambutol is efficient in animal model. 100 mg/kg Ethambutol given orally 15 days post i.v. infection 1 ×/week for 5 weeks, induces a lower log CFU compared with untreatment (4.59 vs 5.07) [3].
Fenvalerate-d6 is the deuterium-labeled Fenvalerate (HY-B2006)[1].
pBD-1 is an endogenous and constitutively expressed antimicrobial peptide (AMP) from porcine tissues, particularly expresses in pig mucosal epithelial sites. pBD-1 has antimicrobial activities and contributes to mucosal and systemic host defenses in pigs[1].
Hexahydrofarnesyl acetone (6,10,14-Trimethyl-2-pentadecanone), a sesquiterpene isolated from Launaea mucronata, is the major constituents of the essential oil. Hexahydrofarnesyl acetone has antibacterial, anti-nociceptive and anti-inflammation activities[1][2].
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca2+ influx through voltage-dependent calcium channels. Antimycobacterial activity[1][2].
Altromycin A is a natural Pluramycin-like antibacterial agent[1].
Polymyxin B nonapeptide TFA is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue[1]. Polymyxin B nonapeptide TFA is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes[2].
Zifanocycline (KBP-7072) is a semisynthetic third-generation aminomethylcycline antibiotic that inhibits the normal function of the bacterial ribosome. Zifanocycline exhibits a broad spectrum of in vitro antibacterial activity against Gram-positive and Gram-negative bacteria, including many multidrug-resistant pathogens. Zifanocycline is available in both oral and injectable formulations. Zifanocycline can be used for the research of acute bacterial skin and skin structure infections, community-acquired bacterial pneumonia, and complicated intra-abdominal infections[1][2].
5-Geranoxy-7-methoxycoumarin is a coumarin with anti-cancer, antifungal, and antibacterial activities. 5-Geranoxy-7-methoxycoumarin induces cell apoptosis[1][2].
Bio-AMS is a chemical inhibitor of Mycobacterium tuberculosis biotin protein ligase ( MtBPL) with Kd of 0.865 nM; possesses selective activity against Mycobacterium tuberculosis ( Mtb) and arrests fatty acid and lipid biosynthesis, enhances tuberculosis chemotherapy (rifampicin and ethambutol).
1-Tetradecanol, isolated from Myristica fragrans, is a straight-chain saturated fatty alcohol. 1-Tetradecanol possesses antibacterial and anti-inflammatory (periodontitis) activity[1].
Morinidazole is a novel 5-nitroimidazole antimicrobial drug that undergoes extensive metabolism in humans via N+-glucuronidation and sulfation, for the treatment of bacterial infections including appendicitis and pelvic inflammatory disease (PID) caused by anaerobic bacteria.
Macrocarpal E is a potent antibacterial agent. Macrocarpal E is a phloroglucinol dialdehyde diterpene derivatives that can be found in the leaves of Eucalyptus macrocarpa[1].
NC00075159 is an opener of human KCNQ4 (Kv7.4) potassium channel.
The minimum inhibitory concentration (MIC) of a new 2- (quinoline-4-methoxy) acetamide antituberculotic agent against the reference strain of Mycobacterium tuberculosis H37Rv was as low as 0.3 μ M. It also inhibited the growth of Mycobacterium tuberculosis in the macrophage model of tuberculosis infection.
Eupatarone (Caleprunin B) is a bacterial inhibitor. Eupatarone can be obtained from Calea platylepis[1].
Tolfenpyrad is a pesticide that was first approved in 2002 in Japan under the trade name of Hachi-hachi.
Demethyl linezolid is a impurity of linezolid. Demethyl linezolid is a useful antimicrobial agent extracted from patent WO1995007271A1, example 9, effective against a number of human and veterinary pathogens[1].