Antibacterial

Picloxydine has antiplaque and antibacterial activity.

Amikacin disulfate (BAY-416651 sulfate) is a semi-synthetic aminoglycoside antibiotic derived from kanamycin A.

Sulfamethazine sodium (Sulfadimethyldiazine Sodium Salt) salt is a sodium salt form of sulfamethazine, a sulfonamide antibiotic used in the livestock industry.

Stability Hygroscopic Applications Neomycin B Trisulfate is a trisulfate salt analog of Neomycin B (N389983), which is an aminoglycoside antibiotic. References Quader, S., et al.: J. Org. Chem., 72, 1962 (2007);

Pyraclostrobin is one of the most heavily used fungicides that inhibits mitochondrial complex III of fungal and mammalian cells.

(±)15-HEPE is a racemic mixture of monohydroxy fatty acids 15 (R) -HEPE and 15 (S) -HEPE, with antibacterial activity.

Lauramine oxide (Refan) is effective against common bacteria such as E. coli and S. aureus, however it is non-denaturing and may be used to solubilize proteins.

D-(+)-Melezitose hydrate (melicitose) is a nonreducing trisaccharide sugar that is produced by many plant sap-eating insects, including aphids.

Applications N-Demethyl-N-(ethylsuccinyl) Erythromycin is an impurity of Erythromycin (E649950), an antibiotic that has a wider spectrum than penicillin (P223500). References Koch, W.L., et al.: Anal. Profiles Drug Subs., 8, 157 (1979),

Applications Levofloxacin-d3, is the labeled analogue of Levofloxacin (L360000), an antibiotic used against gram-negative organisms. References Kato, M., et al.: Arzneim.-Forsch., 42, 365 (1992), North, D.S., et al.: Pharmacotherapy, 18, 915 (1998), Hwang, D.G., et al.: Br. J. Ophthalmol., 87, 1004 (2003),

Applications Colistin A Sulfate Hydrate is used as an antibiotic in the treatment of infectious diseases resulting from multi-drug resistant (MDR) gram-negative bacteria. References Wallace, S. et al.: J. Pharm. Sci., 102, 1578 (2013); Suzuki, T., et al.: J. Biochem., 54, 25 (1963); Barnett, M., et al.: Br. J. Pharmacol. Chemother., 23, 552 (1964); Littlewood, J, M., et al.: Respir. Med., 94, 632 (2000); Li, J., et al.: Int. J. Antimicrob. Ag., 25, 11 (2005); Tsubery, H. et al.: Antimicrob. Agents Chemother., 49, 3122 (2005)

Streptomycin (Agrept) is an aminoglycoside antibiotic isolated from Streptomyces species, a blocker of stretch-activated in neurons and cardiomyocytes.

Applications Third generation cephalosporin antibiotic. Antibacterial. References Brodie, A., et al.: Antimicrob. Agents Chemother., 17, 876 (1980), Richards, D.M., et al.: Drugs, 29, 105 (1985), Abounassif, M.A., et al.: Anal. Profiles Drug Subs., 19, 95 (1990),

Chlorobutanol hemihydrate (Chlorbutol hemihydrate) is an antiseptic with antimicrobial activity, inhibiting Gram-positive and fungi.

DuP 105 is an oral oxazolidinone, a novel synthetic antimicrobial compound effective against gram-positive bacteria.

Applications Antibacterial agent. References Gribble, G.W., et al.: J. Med. Chem., 31, 1746 (1988), Maeda, U., et al.: Phytochemistry, 34, 1633 (1993),

Cefoselis Sulfate is a widely used beta-lactam antibiotic.

β-Lactamase-IN-2 is an inhibitor of β-Lactamase with anti-microbial and anti-bacterial effects.

PC190723 is an inhibitor of the bacterial cytosolic protein FtsZ with antimicrobial activity against Staphylococcus spp.

Impurity Clarithromycin Impurity O EP Stability Hygroscopic Applications Clarithromycin (9Z)-O-Methyloxime is an impurity of Clarithromycin (C559750); a semi-synthetic macrolide antibiotic and derivative of Erythromycin (E650000). References Morgan, D., et al.: J. Chromatogr., 502, 351 (1990); Benson, C., et al.: Eur. J. Clin. Microbiol., 6, 173 (1987); Boyanova, L., et al.: J. Med. Microb., 61, 85 (2012); Lin, Z., et al.: Toxicol. Sci., 126, 114 (2012)

Phenoxyethanol (NSC-1864) is germicidal. It often used together with quaternary ammonium compounds.

Nithiamide (CL-5279) is an orally available antiprotozoan agent used in the treatment of vaginal trichomoniasis.

Stability Hygroscopic Applications Phenethicillin is a semisynthetic penicillin based β-lactam antibiotic and are used in the treatment of bacterial infections caused by susceptible, usually Gram-positive bacteria. References Lucien, C., et al.: Can. med. Assoc. J., 84, 535 (1961); Timmers, G.J., et al.: Clin. Microbiol. Infect., 13, 497 (2007);

Stability Hygroscopic Applications The antibiotics Fosmidomycin and FR900098 are members of a unique class of phosphonic acid natural products that inhibit the nonmevalonate pathway for isoprenoid biosynthesis. Both are potent antibacterial and antimalarial compounds. References Altschul, S., et al.: J. Mol. Biol., 215, 403 (1990), Altschul, S., et al.: J. Mol. Biol., 215, 403 (1990), Noda, M., et al.: J. Biol. Chem., 279, 46143 (2004), Snow, R., et al.: Nature, 434, 214 (2005),

LtaS-IN-1 inhibits LTA synthesis in MDR E. faecium; alters cell walls; MIC: 0.5-64 μg/mL for 28 Enterococcus strains.

1. Agrimol B is a main active ingredient isolated from Agrimonia pilosa Ledeb.

Meptyldinocap (2,4-DNOPC) functions as an innovative fungicide against powdery mildew (Erysiphe necator), exhibiting both protectant and post-infective

Bromperidol (R-11333) is a butyrophenone derivative and it is a potent and long-acting neuroleptic.

Miconazole nitrate, an antifungal, targets fungal cell membranes rich in ergosterol, distinct from mammalian cells.

Avibactam sodium (NXL-104) is a β-lactamase inhibitor that inhibits TEM-1, P99, and KPC-2. Avibactam sodium has antimicrobial activity. Cost-effective and quality-assured.

Betamipron (CS-443) is used combination with panipenem to prevent nephrotoxicity and inhibit panipenem uptake into the renal tubule.

Isobavachromene is an inhibitor of NADH-Ubiquinone oxidoreductase and ornithine decarboxylase. Isobavachromene has antifungal activity.

2-Butyldecanoic acid has potential antibacterial and antiviral activity, with high activity against mosquito larvae.

Applications An antibacterial used in veterinary medicine. Used in the treatment of infections caused by pathogens such as S. aureus, E. coli, Streptococcus, P. multocida and A. pleuropneumoniae. Also used to treat mastitis in dairy cows. References Bottner, A. et al.: J. Vet. Med., 42, 377 (1995); Fan, X. et al.: Xumu Yu Shouyi, 40, 78 (2008); Shpigel, N.Y. et al.: J. Dairy Sci., 80, 318 (1997);

Chlorquinaldol (5,7-Dichloro-8-hydroxy-2-methylquinoline) is an antimicrobial agent with potential for study of topical skin conditions and vaginal infections.

Cetylpyridinium chloride: an antiseptic used in oral care and pesticides; may stain teeth.

Sulfacetamide sodium monohydrate is a sulfonamide antibiotic. It has been investigated for the treatment of rosacea and pityriasis versicolor.

Nadifloxacin (OPC7251) has been used in trials studying the treatment of Acne Vulgaris.

Impurity Clarithromycin EP Impurity C Applications Clarithromycin 9-Oxime (Clarithromycin EP Impurity C) is an impurity of Clarithromycin (C559750), a macrolide antibiotic. References Stephanic, V. et al.: J. Med. Chem., 54, 719 (2011); Chen, X. et al.: Zhong. Yao., 17, 32 (2008);

Durlobactam Triethylamine inhibits A, C, D β-lactamases and possesses antifungal properties.

2-Methoxy-1,4-naphthoquinone triggers A549 cell apoptosis via JNK/p38 MAPK pathways, independent of cell cycle arrest, due to oxidative DNA damage from ROS.

Applications N-Acetyl Cefixime is the N-acetylated analogue and impurity of the third generation cephalosporin antibiotic, Cefixime (C242800).

Stability Hygroscopic Applications Furagin (a nitrofurantoin analog) has the same efficacy in treating acute cystitis as Ciprofloxacin, however the duration of therapy is longer. Antibacterial. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Agace, W., et al.: J. Clin. Invest., 92, 780 (1993); Lawrenson, R., et al.: J. Antimicrob. Chemother., 48, 895 (2001); Dalhoff, A., et al.: Lancet Infect. Dis., 3, 359 (2003); Thumbikat, P., et al.: J. Immunol., 176, 3080 (2006);

Mafenide hydrochloride (4-Aminomethylbenzenesulfonamide hydrochloride) is a sulfonamide that inhibits the enzyme carbonic anhydrase and is used as topical anti-

Sulfamethoxypyridazine (CL 13494) is a sulfanilamide antibacterial agent.

Sulfamethoxazole sodium (Ro 4-2130 sodium) is a sulfonamide bacteriostatic antibiotic

Dalbavancin (BI-397) is a lipoglycopeptide antibiotic effective against Gram-positive pathogens, MRSA, MRSE, with MIC90s of 0.06-0.25 μg/mL.

Bedaquiline, an anti-TB drug, blocks mycobacterial ATP synthesis, effective against all Mycobacterium tuberculosis states.

Olanexidine HCl (OPB-2045) kills both Gram-positive/negative bacteria, damaging S. aureus membranes.

Bederocin (REP8839), a METS inhibitor, has strong activity against S. aureus, S. pyogenes, and Gram-positive bacteria.

Ceftaroline fosamil (TAK-599) is a cephalosporin, with activity against Gram-positive pathogens.

Antimycobacterial agent-4 (4-nitro-N-[4-(2-pyridyl)thiazol-2-yl]benzamide) has antibacterial activity against Mycobacterium tuberculosis.

Nemonoxacin (TG-873870), a potent oral antibiotic, treats various bacterial infections and pneumonia.

BTZ043 Racemate (Benzothiazinone 10526038) is a decaprenylphosphoryl-β-D-ribose 2'-epimerase (DprE1) inhibitor, used as a new antimycobacterial agent.

Carabrone, a botanical bicyclic sesquiterpenic lactone, is a promising fungicidal agent that can effectively control G. tritici.

Sulfadimethoxine (Sulphadimethoxine) is a sulfanilamide that is used as an anti-infective agent.

Bronopol (BNPD): Low-toxicity antimicrobial, highly effective against Gram-negative bacteria.

Cefmenoxime hydrochloride: cephalosporin antibiotic, IV/IM, targets gram-positive/negative bacteria, beta-lactamase resistant, effective, low side effects.

Impurity Bupropion Des-t-Butylamino Impurity Applications 3'-Chloropropiophenone is a reagent used in the vinylation, alkylation and dienylation of ketones. It is also used in the preparation of thizaine derivatives that show antibacterial activity. References Li, H. et al.: J. Am. Chem. Soc., 127, 8355 (2005); Deepika, G. et al.: J. Pharm. Res., 5, 1105 (2012);

Sanguisorbigenin (Tomentosolic acid) is a natural antimicrobial agent that inhibits methicillin-resistant Staphylococcus aureus (MRSA).

Eperezolid (PNU-100592), an oxazolidinone antibiotic, inhibits staphylococci (MIC90=1-4 mg/ml) effectively, methicillin resistance notwithstanding.

NSC-60339: AcrAB-TolC substrate, efflux pump inhibitor, potential cancer drug.

CHEMBL1380345 fights S. aureus, B. cereus, E. coli; pMICs: 3.64, 3.56, 3.70.

DprE1-IN-2 is an effective DprE1 inhibitor.

Antimicrobial agent-22 (THI 6c) constitutes a broad-spectrum, multi-target antibacterial with notable rapid bactericidal efficacy and effective anti-biofilm

Impurity Ofloxacin EP Impurity E Applications Desmethyl Ofloxacin (Ofloxacin EP Impurity E) is a metabolite of Ofoxacin (O245750), a fluorinated quinolone antibacterial. References Leysen, D., et al.: Antimicrob. Agents Chemother., 33, 1 (1989); Polk, R., et al.: J. Antimicrob. Chemother., 27, 17 (1991); Todo, Y., et al.: Chem. Pharm. Bull., 42, 2049 (1994); Furuhata, K., et al.: Biol. Pharm. Bull., 21, 456 (1998); Monk, J.P., et al.: Drugs, 33, 346 (1987); Drlica, K., Curr. Opin. Microbiol. 2, 504 (1990)

Stability Hygroscopic Applications A isothiazolidin-3-one derivative as antimicrobial. It was tested for inhibition of PCAF activity. 5-Chloroisothiazolinones showed the most potent inhibition of PCAF. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Sadhale, P.P., et al.: J. Biol. Chem., 279, 33716 (2004), Thomsen, R., et al.: J. Med. Chem., 49, 3315 (2006),

Stability Hygroscopic Applications Ethyl (Z)-[2-amino-4-thiazolyl](methoxyimino)acetate is used in the preparation of ceftriaxone-d3 (C245002), which is a labelled antibacterial. References Reiner, R., et al.: J. Antibiot., 33, 783 (1980)

Leucomycin (Turimycin) is a macrolide antibiotic.

Stability Hygroscopic Applications Azlocillin Sodium Salt is the sodium salt form of Azlocillin which is a semisynthetic ampicillin-derived acylureido penicillin with antibacterial activity against a broad range of bacteria including haemophilus influenzae, bacteroides and pseudomonas aeruginosa. References Reeves, D., et al.: Arzneimittel-Forschung, 29, 1920 (1979); Opalchenova, G., et al.: Int. J. Pharm.,153, 263 (1997);

Furagin (Furazidine) is a Nitrofuran derivative with anti-infective activity used for urinary tract infections.

Cloxiquine (Dermofongin) is a monohalogenated 8-hydroxyquinoline with activity against bacteria, fungi, and protozoa.

Sulbactam (CP45899) is a semi-synthetic inhibitor that enhances antibiotics by blocking beta-lactamase.

Applications A macrolide isolated from Penicillium brefeldianum. It affects the vesticular transport of the Golgi apparatus and induces DNA fragmentation which leads to apoptosis. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Misumi, Y., et al.: J. Biol. Chem., 261 (1986), Mordente, J.A., et al.: J. Urol., 159, 275 (1998), Erokhina, M.V., et al.: Membr. Cell Biol., 12, 871 (1999), Nojiri, H., et al.: FEBS Letters, 453, 140 (1999),

Chlorphenesin (Chlorophenesin) is an antigen-associated immunosuppressant that inhibits IgE-mediated histamine release. It is also used as an antimycotic agent.

Applications Labelled Cephradine is a first generation cephalosporin antibiotic. Cephradine has broad spectrum of bactericidal activity against infections caused by Streptococcus, Staphylococcus, Diplococcus pneumoniae, Escherichia, Klebsiella, Salmonella, and indole-negative Proteus. References Poutsiaka, J.W. et al.: Prog. Chemother. (Antibacterial, Antiviral, Antineoplast.), Proc. Int. Congr. Chemother., 2, 142 (1974); Florey, K. et al.: Anal. Prof. Drug Subs., 5, 21 (1976);