Antibiotici Naturali e Semisintetici

<p>Cilastatin (MK0791): protects imipenem from renal breakdown; inhibits leukotriene D4 metabolism.</p>

<p>Amprenavir (KVX-478) is a synthetic derivative of hydroxyethylamine sulfonamide that selectively binds to and inhibits human immunodeficiency virus (HIV)</p>

<p>Biapenem (CLI 86815), a carbapenem antibiotic, has broad antibacterial effects, stable kidney enzyme resistance, and low neurotoxicity.</p>

<p>Ceftobiprole medocaril: injectable prodrug; its active form fights broad-range infections including MRSA.</p>

<p>Zearalenone (F2 toxin) is a mycotoxin produced mainly by fungi belonging to the genus Fusarium in foods and feeds.</p>

<p>Tedizolid (DA-7157)is a novel oxazolidinone-class antibiotic that inhibits bacterial protein synthesis by binding to the 23S ribosomal RNA of the 50S subunit of</p>

<p>Cefazedone (Refosporen) is a semisynthetic first-generation cephalosporin with activity against Gram-positive and Gram-negative bacteria[1].</p>

<p>Pleuromutilin (Drosophilin B) is an inhibitor of bacterial protein synthesis by binding to the 50S ribosomal subunit of bacteria.</p>

<p>Ceftezole sodium (Falomesin) is a broad-spectrum cephalosporin antibiotic active gram-negative and gram-positive bacteria except for Proteus vulgaris,</p>

<p>Brevianamide F (Cyclo(L-Pro-L-Trp)), also known as cyclo-(L-Trp-L-Pro), belongs to a class of naturally occurring 2,5-diketopiperazines.</p>

<p>Oral 3rd-gen cephalosporin antibiotic; treats ear, throat, sinus infections; active vs. Gram+ &amp; Gram- bacteria; Cefpodoxime proxetil is a prodrug.</p>

<p>Zotarolimus (ABT-578), an analogue of rapamycin, inhibits FKBP-12 (IC50= 2.8 nM).</p>

<p>Ticarcillin sodium: a semisynthetic, broad-spectrum antibiotic effective against various aerobic and anaerobic bacteria.</p>

<p>Ertapenem sodium (MK-826) is a long-acting carbapenem antibiotic effective against a wide range of bacteria, including ESBL producers.</p>

<p>Doripenem is a new parenteral carbapenem antibiotic with broad-spectrum activity against gram-negative and gram-positive pathogens.</p>

<p>Cadazolid (ACT-179811) is an oxazolidinone-type antibiotic, with activity against gram-positive bacteria, including Clostridium difficile.</p>

<p>Gatifloxacin hydrochloride, a fourth-gen fluoroquinolone antibiotic, blocks bacterial DNA rotase and topoisomerase IV.</p>

<p>Fosfomycin sodium is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria.</p>

<p>Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults.</p>

<p>Tedizolid Phosphate (TR-701FA) is an oxazolidinone-class antibiotic. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid.</p>

<p>Pivmecillinam HCl, an oral prodrug of mecillinam, is a broad-spectrum penicillin effective against gram-negative bacteria.</p>

<p>Ceftiofur is a semisynthetic antibiotic, with activity against various gram-positive/negative, anaerobic and aerobic bacteria encountered by domestic animals.</p>

<p>Neomycin, an antibiotic from Streptomyces fradiae, inhibits protein synthesis; comprises types A, B, C.</p>

<p>Amdinocillin pivoxil, an oral prodrug of amdinocillin, targets gram-negative bacteria.</p>

<p>Cefotaxime is an inhibitor of penicillin binding protein.</p>

<p>Tiamulin (Thiamutilin) is a semisynthetic pleuromutilin antibiotic</p>

<p>Tenidap Sodium is a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory agent.</p>

<p>Amoxicillin Sodium (Clavulanate) is a moderate- spectrum, bacteriolytic, β-lactam antibiotic.</p>

<p>Nystatin (Fungicidin) is a topical and oral antifungal agent with activity against many species of yeast and candida albicans, which is used largely to treat</p>

<p>Fumagillin (Amebacilin) is a selective and potent irreversible inhibitor of Methionine aminopeptidase 2 (MetAP2), used as an antibiotic to treat</p>

<p>Tilmicosin phosphate, a macrolide antibiotic, is used to treat cattle for pathogens that cause Bovine Respiratory Disease.</p>

<p>Carbenicillin disodium (BRL-2064) is a broad-spectrum, semi-synthetic penicillin antibiotic with bactericidal and beta-lactamase resistant activity.</p>

<p>Eribulin mesylate (E7389), a microtubule inhibitor, treats metastatic breast cancer by halting cell division.</p>

<p>Puromycin dihydrochloride, from Streptomyces alboniger, blocks protein synthesis, acting as an antineoplastic and antitrypanosomal agent.</p>

<p>Lumefantrine, an antimalarial, treats malaria with artemether, effective against Plasmodium spp. including in chloroquine-resistant areas.</p>

<p>Mecillinam, an antibiotic, targets Gram-negative bacteria, mainly for urinary infections and some fevers.</p>

<p>Cefotetan, a cephamycin antibiotic, fights various bacteria by disrupting cell wall synthesis.</p>

<p>Pipecolic acid is a lysine metabolite in urine, plasma, CSF, and regulates immunity in plants and humans.</p>

<p>Impurity Azithromycin EP Impurity I<br>Stability Hygroscopic<br>Applications N’-Desmethyl Azithromycin (Azithromycin EP Impurity I) is a metabolite of Azithromycin (A927000) as potential anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agent.<br>References Bright, G., et al.: J. Antibiot., 41, 1029 (1988), Goldman, R., et al.: Antimicrob. Agents Chemother., 34, 426 (1990), Gandhi, R., et al.: J. Pharm. Biomed. Anal., 23, 1073 (2000),<br></p>

<p>Applications Lumefantrine-d9, is the labeled analogue of Lumefantrine (L474000), which Inhibits hemozoin formation, used as Antimalarial.<br>References Kumar, N., et al.: Parasitol Res., 76, 214 (1990), Pradines, B., et al.: Antimicrob. Agents Chemother., 43, 418 (1999), Chotivanich, K., et al.: J. Infect. Dis., 182, 629 (2000), Mutabingwa, T., et al.: Lancet, 365, 1474 (2005),<br></p>

<p>Applications Chloramphenicol Succinate Sodium is a derivative of Chloramphenicol (C325030) which are broad spectrum antibiotic obtained from cultures of the soil bacterium Streptomyces venezuelae. It has a broad spectrum of activity against Gram-positive and gram-negative bacteria. Antibacterial; antirickettsial.<br>References Bartz, et al.: J. Biol. Chem., et al.: 172, 445 (1948), Gottlieb, et al.: J. Bacteriol., 55, 409 (1948), Szulczewski, D., et al.: Anal. Profiles Drug Subs., 4, 47 (1975), Price, A., et al.: J. Antibiot., 43, 118 (1981), Shalit, I., et al.: Drugs, 28, 281 (1984),<br></p>

<p>Impurity Moxifloxacin EP Impurity B<br>Applications Moxifloxacin (M745000) impurity B.<br>References Langlois, M., et al.: J. Pharm. Biomed. Anal., 37, 389 (2005), Salem, M., et al.: Chem. Pharm. Bull., 54, 1625 (2006),<br></p>

<p>Applications Tulathromycin B is an antibiotic pharmaceutical and also a part of various veterinary compounds. This compound is used for treatment of bacterial and protozoal infections.<br>References Benchaoui, H.A., et al.: J. Vet. Pharmacol. Ther., 27, 203 (2004), Nowakowski, M.A., et al.: Vet. Ther., 5, 60 (2004),<br></p>

<p>Impurity Clarithromycin EP Impurity D<br>Applications N-Desmethyl Clarithromycin (Clarithromycin EP Impurity D) is a metabolite of Clarithromycin (C559750).<br>References Jenuwein, T., et al.: Science, 293, 1074 (2001), Somech, R., et al.: Cancer Treat. Rev., 30, 461 (2004),<br></p>

<p>Applications N-Methyl-N-(1-naphthalenylmethyl)-1-naphthalenemethanamine is a reagent used in the synthesis of Butenafine Hydrochloride (B690195) an anti-fungal.<br>References Maeda, T., et al.: Yakugaku Zasshi, 111, 126 (1991).<br></p>

<p>Stability Hygroscopic, Light Sensitive<br>Applications Polyene antifungal antibiotic.<br>References Levinskas, G.J., et al.: Toxicol. Appl. Pharmacol., 8, 97 (1966), Pandey, R.C., et al.: J. Antibiot., 29, 1035 (1976), Brik, H., et al.: Anal. Profiles Drug Subs. Excip., 23, 399 (1994),<br></p>

<p>Impurity Linezolid USP Related Compound D<br>Applications (5R)-3-[3-Fluoro-4-(4-morpholinyl)phenyl]-5-[[(methylsulfonyl)oxy]methyl]-2-oxazolidinone (Linezolid USP Related Compound D) is an intermediate in the synthesis of Linezolid Dimer (L466520), an impurity of the antibacterial agent Linezolid (L466500).<br>References Xu, Heteroatom, Chem., 19, 316 (2008); Wang, J.W., et al.: Lett. Org. Chem., 5, 336 (2008);<br></p>

<p>Stability Unstable in Solution<br>Applications Meropenem-d6 is the labeled analogue of Meropenem, a carbapenem antibiotic. Antibacterial.<br>References Adams, M.D., et al.: J. Bacteriol., 190, 8053 (2008); Pattanaik, P., et al.: J. Biol. Chem., 284, 945 (2009); Mendes, R., et al.: J. Antimicrob. Chemother., 63, 55 (2009)<br></p>

<p>Applications Ledipasvir is most commonly used in combination with sofosbuvir for treatment in chronic hepatitis C genotype 1 patients. It inhibits an important viral phosphoprotein, NS5A, which is involved in viral replication, assembly, and secretion.<br>References Lawitz, E., et al.: J. Hepatol., 57, 24 (2012); Afdhal, N., et al.: New England J. Med., 370, 1889 (2014)<br></p>

<p>Applications D-Serine Methyl Ester Hydrochloride (cas# 5874-57-7) is a compound useful in organic synthesis.<br></p>

<p>Applications Erythromycin B is a co-metabolite of Erythromycin A (E649950), an antibacterial agent.<br>References Minh, N. et al.: Int. Food. Res. J., 18, 95 (2011); Koch, W.L. et al.: Anal. Profiles Drug Subs., 8, 157 (1979);<br></p>

<p>Applications Polyene antifungal antibiotic complex containing 3 biologically active components, A1, A2, A3. Increases the permeability of the cell membrane of sensitive fungi by binding to sterols. Cell culture tested. Growth promotant.Nystatin A1 is shown.<br>References Brautaset, T., et al.: Chem. Biol., 7, 395 (2000), Brautaset, T., et al.: J. Biol. Chem., 278, 14913 (2003), Bruheim, P., et al.: Antimicrob. Agents Chemother., 48, 4120 (2004), Scott, L., et al.: Drugs, 67, 269 (2007),<br></p>

<p>Applications Rifampicin N-4’-Oxide is a metabolite of Rifampicin (R508000).<br>References Gryaznova, N.S. et al.: Curr. Chemother. Immunother., Proc. Int. Congr. Chemother., 12, 984 (1982); Subbotina, N.A. et al.: Antibiotiki, 24, 590 (1979);<br></p>

<p>Applications Intermediate in the preparation of Moxifloxacin derivatives.<br>References Zhang, Z., et al.: Bioorg. Med. Chem. Lett., 14, 393 (2004), Zhang, Z., et al.: Bioorg. Med. Chem., 15, 7274 (2007),<br></p>

<p>Applications PNU 142586 Sodium Salt is an inactive metabolite of Linezolid (L466500).<br>References Shinabarger, D., et al.: Antimicrob. Agents Chemother., 41, 2132 (1997), Wynalda, M., et al.: Drug Metab. Dispos., 28, 1014 (2000),<br></p>

<p>Stability Hygroscopic<br>Applications 25-Deacetyl-23-acetyl Rifampicin is a structural isomer, and impurity, of Rifampicin (R508000), a semisynthetic antibiotic. Antibacerial (tuberculostatic).<br>References Furesz, et al.: Antibiot. Chemother., 16, 316 (1970), Gallo, G.G., et al.: Anal. Profiles Drug Subs., 5, 467 (1976),<br></p>

<p>Applications Bacitracin A is a peptide antibiotic.<br>References Eppelmann, K., et al.: J. Biol. Chem., 276, 34824 (2001); Mei, L., et al.: Biomat., 34, 10328 (2013);<br></p>

<p>Applications An impurity of Gatifloxacin.<br>References Naber, C., et al.: Antimicrob. Agents Chemother., 45, 293 (2001), Herzler, M., et al.: J. Anal. Toxicol., 27, 233(2003), Pragst, F., et al.: Clin. Chem. Lab. Med., 42, 1325 (2004),<br></p>

<p>Applications Spinetoram J is a component of Spinetoram (S683650), a compound that belongs to the spinosyn family of insecticides and shows potential of natural products research. Useful in cannabis testing kits as a component of pesticide mixes (P698240).<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Kirst H. A.: J. Antibiot., 63, 101-111 (2010)<br></p>

<p>Stability Hygroscopic<br>Applications A labelled metabolite of Cephapirin (C261500) in bovine milk.<br>References Moats, W., et al.: J. Agric. Food Chem., 48, 498 (2000),<br></p>

<p>Applications N-Ethylpiperazine is an intermediate in the production of Enrofloxacin.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Chao, Q., et al.: J. Med. Chem., 52, 7808 (2009), Bebbington, D., et al.: Bioorg. Med. Chem. Lett., 19, 3586 (2009),<br></p>

<p>Applications Labelled Cefetamet is a third-generation cephalosporin antibiotic and the active agent of Cefeamet pivoxil (C242780) after hydrolysis.<br>References Bryson, H.M., et al.: Drugs., 45, 589 (1993); Sharma, R.K., et al.: Asian. J. Biochem. Pharmaceut. Res., 1, 443 (2011); Waters, N.J., et al.: Drug. Metabolism. Disposit., 38, 1159 (2010);<br></p>

<p>Applications Pneumocandin B0 is the major analogue of a family of lipopeptides isolated from several species of several different genera, such as Cryptosporiopsis, Glarea and Pezicula. Pneumocandin B0 is a potent antifungal and acts by inhibition of the synthesis of β-(1,3)-D-glucan, an essential component of the cell wall of susceptible fungi.<br>References Schwartz, R., et al.: J. Antibiot., 45, 1853 (1992); Petersen, L., et al.: Appl. Microbiol. Biotechnol., 62, 263 (2003), Petersen, L., et al.: Appl. Microbiol. Biotechnol., 62, 263 (2003),<br></p>

<p>Applications Isotope labelled Erythromycin (E649950), an antibiotic useful for the treatment of a number of bacterial infection, usually prescribed to patients with allergy to penicillin.<br>References Koch, W.L., et al.: Anal. Profiles Drug Subs., 8, 157 (1979),<br></p>

<p>Impurity Moxidectin EP Impurity D<br>Applications 2-epi-Moxidectin is stereoisomer of Moxidectin, a macrocyclic lactone and semisynthetic derivative of nemadectin. Moxidectin is a parasiticide used for the prevention and control of heartworm and intestinal worms. Moxidectin is found in veterinary medicine used to treat animals such as dogs, cats, horses, cattle and sheep.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Bisset, S.A. et al.: New Zeal. Vet. J., 40, 97 (1992); Monahan, C.M. et al.: Vet. Parasitol., 63, 225 (1996); Glickman, L.T. et al.: Int. J. Appl. Res. Vet. Med., 3, 49 (2005);<br></p>

<p>Impurity Oxytetracycline Hydrochloride EP Impurity A<br>Stability Hygroscopic, Unstable in solution<br>Applications A metabolite of Oxytetracycline (OTC); also a Tetracycline analogue as inhibitor of amyloid fibrils.<br>References Eisner, H., et al.: J. Pharm. Exp. Ther., 142, 122 (1963), Nelis, H., et al.: Drug Metab. Dispos., 10, 142 (1982), Boecker, R., et al.: Drugs Exp. Clin. Res., 9, 813 (1983),<br></p>