Natural and semi-synthetic antibiotics

<p>Lurbinectedin (PM01183) is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity.</p>

<p>Cefapirin sodium is the sodium salt of Cephapirin, an antimicrobial agent.</p>

<p>Cloxacillin, a β-lactamase inhibitor, tackles S. aureus inflammation and has an IC50 of 0.04 µM.</p>

<p>Cefpirome sulfate (HR-810 sulfate) is a fourth generation cephalosporin antibiotic.</p>

<p>Doxycycline (Doxiciclina) belongs to the tetracycline class of antibiotics and is a broad-spectrum metalloproteinase (MMP) inhibitor with oral activity.</p>

<p>Ixabepilone (Azaepothilone B) is an orally bioavailable microtubule inhibitor.</p>

<p>Maduramicin ammonium (Maduramycin Ammonium) is an anticoccidial agent for the the treatment of Eimeria spp., E.</p>

<p>Fosfomycin sodium is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria.</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>Tacrolimus monohydrate (LCP-Tacro) is a macrolide from the culture broth of a strain of Streptomyces tsukubaensis, binds to FKBP to form a complex.</p>

<p>Faropenem sodium: Oral penem antibiotic for tuberculosis, pneumonia.</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>Josamycin (EN-141) is a macrolide antibiotic exhibiting antimicrobial activity. The dissociation constant Kd from ribosome for Josamycin is 5.5 nM.</p>

<p>Epothilone B (EPO 906) is a compound isolated from the myxobacterium Sorangium cellulosum.</p>

<p>Doxycycline hyclate (WC2031) is a synthetic tetracycline derivative with similar antimicrobial activity. Doxycycline hyclate is also an inhibitor of MMP.</p>

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

<p>Spinosad: natural insecticide from S. spinosa, mix of spinosyn A &amp; D, targets insect nAChRs.</p>

<p>Azithromycin (CP 62993) is a macrolide antibiotic that primarily targets the 50S subunit of bacterial ribosomes. High-Quality, Low-Cost!</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>Dalbavancin (BI-397) is a lipoglycopeptide antibiotic effective against Gram-positive pathogens, MRSA, MRSE, with MIC90s of 0.06-0.25 μg/mL.</p>

<p>Difloxacin hydrochloride (Difloxacin HCl) is a fluoroquinolone antibiotic, is a broad-spectrum antibacterial drug.</p>

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

<p>Pretomanid ((S)-PA 824) , a nitroimidazole, is used as an anti-tuberculosis drug for tuberculosis with MIC less than 2.8 μM.</p>

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

<p>Amifloxacin (Win49375) is a synthetic antibacterial compound and showed moderate activity against Staphylococcus aureus, with MICs of less than or equal to 2</p>

<p>Delafloxacin (WQ-3034, RX-3341, ABT-492) is a potent antibiotic for levofloxacin-resistant S. pneumoniae (MIC: 0.0078-0.125 μg/ml).</p>

<p>Oritavancin diphosphate, a novel semisynthetic glycopeptide antibiotic, targets serious Gram-positive infections.</p>

<p>Ivermectin B1a is the major (80%) component of commercially available ivermectin and a derivative of Avermectin B1a.</p>

<p>Ascomycin (Immunomycin)(Immunomycin, FR-900520, FK520) is an ethyl analog of tacrolimus (FK506) with strong immunosuppressant properties.</p>

<p>Ceftibuten dihydrate (Sch-39720 dihydrate) is the dihydrate form of ceftibuten, and is a third-generation cephalosporin with antibacterial activity.</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>Stability Hygroscopic<br>Applications An intermediate in the preparation of labelled FK-506 (Tacrolimus)<br>References Rokaw, M.D., et al.: Am. J. Physiol., 271, C194 (1996), Knoll, G.A., et al.: Brit. Med. J., 318, 1104 (1999),<br></p>

<p>Applications An antibacterial.<br>References Hirai, K., et al.: Antimicrob. Ag. Chemother., 29, 1059 (1986), Weidekamm, E., et al.: Antimicrob. Ag. Chemother., 31, 1909 (1987), Boerema, J.B.J., et al.: J. Antimicrob. Chemother., 21, 140 (1988)<br></p>

<p>Applications An metabolite of Aztreonam (A965200), the first totally synthetic monocyclic β-lactam antibiotic.<br>References Creasey, W.A., et al.: Brit. J. Clin. Pharmacol., 19, 233 (1985); Swabb, E.A., et al.: Antimicrob. Agent. Chemotherap., 24, 394 (1983);<br></p>

<p>Impurity Cefpodoxime Proxetil EP Impurity A<br>Stability Hygroscopic<br>Applications Cefpodoxime Acid (Cefpodoxime Proxetil EP Impurity A) is a metabolite of Cefpodoxime Proxetil (C243860). An antibacterial.<br>References Fujimoto, K., et al.: J. Antibiot., 40, 370 (1987), Utsui, Y., et al.: Antimicrob. Agents Chemother., 31, 1085 (1987),<br></p>

<p>Applications A fluoroquinolone used in the synthesis of Gatifloxacin (G250000).<br>References Sunderland, J., et al.: J. Antimicrob. Chemother., 47, 271 (2001), Herzler, M., et al.: J. Anal. Toxicol., 27, 233 (2003), Li, Y., et al.: J. Pharm. Biomed. Anal., 35, 1101 (2004),<br></p>

<p>Applications Semi-synthetic derivative of Erythromycin. Antibacterial.<br>References Firl, J., et al.: J. Antibiot., 43, 1271 (1990), Counter, et al.: Antimicrob. Agents Chemother., 35, 1116 (1991), Castaldo, R., et al.: Clin. Ther., 25, 542 (2003),<br></p>

<p>Applications Methyl(4-methylnaphthalen-1-ylmethyl)amine is a reagent in the preparation of heterocyclic compounds as enoyl-acyl carrier protein reductase FabI inhibitors and antibacterial agents.<br>References Stuetz, A., et al.: J. Med. Chem., 29, 112 (1986); Berman, J., et al.: PCT Int. Appl., 2004:515512 (2004)<br></p>

<p>Applications A dimer impurity of the antibacterial Cefpodoxime Proxetil (C243870).<br></p>

<p>Applications Mupirocin, is a major component of the pseudomonic acid, an antibiotic complex produced by Pseudomonas fluorescens NCIB 10586. Topical antibacterial.<br>References Hughes, J., et al.: J. Antibiot., 31, 330 (1978), Ward, A., et al.: Drugs, 32, 425 (1986), Casewell, M.W., et al.: J. Antimicrob. Chemother., 19, 1 (1987),<br></p>

<p>Applications (trans)-4-Propyl-1-methyl-L-proline (cas# 13380-36-4) is a compound useful in organic synthesis.<br></p>

<p>Applications Inhibits hemozoin formation. 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>Stability Unstable in basic solution<br>Applications Oxytetracycline metabolite (absolute stereochemistry unknown)<br>References Mackie, R., et al.: Animal Biotechnol., 17, 157 (2006), Smyrniotakis, C., et al.: J. Pharm. Biomed. Anal., 43, 506 (2007), Li, D., et al.: Env. Toxicol. Chem., 27, 80 (2008),<br></p>

<p>Applications Cefminox is a semisynthetic broad spectrum cephamycin antibiotic. Antibacterial.<br>References Inouye, S., et al.: Antimicrob. Agents Chemother., 26, 722 (1984), Watanabe, T., et al.: Drugs Exp. Clin. Res., 10, 293 (1984), Tsuruoka, T., et al.: Eur. J. Biochem., 151, 209 (1985),<br></p>

<p>Applications N-[(2R)-3-[[3-Fluoro-4-(4-morpholinyl)phenyl]amino]-2-hydroxypropyl]acetamide is an impurity of Linezolid (L466500).<br>References Gregory, W., et al.: J. Med. Chem., 32, 1673 (1989), Shinabarger, D., et al.: J. Antimicrob. Agents Chemother., 41, 2132 (1997),<br></p>

<p>Applications A derivatized of AMOZ (A634600), a metabolite of Nitrofuran.Environmental contaminants; Food contaminants; Heat processing contaminants<br>References Vroomen, L., et al.: Toxicol. Appl. Pharmacol., 95, 53 (1988), Delatour, T., et al.: J. Agric. Food Chem., 51, 6371 (2003), Stadler, R., et al.: Analyst, 129, 276 (2004),<br></p>

<p>Impurity Fosfomycin EP Impurity B<br>Stability Very Hygroscopic<br>Applications [2-[2-Amino-3-hydroxy-2-(hydroxymethyl)propoxy]-1-hydroxypropyl]phosphonic Acid (Fosfomycin EP Impurity B) is a Fosfomycin (F727500) impurity. Fosfomycin is an antibiotic that exerts a broad spectrum of antibacterial activity.<br>References McGrath, J.W., et al.: Org. Biomolec. Chem., 7, 9 (1944); Goto, M., et al.: Antimicrob. Agents Chemother., 20, 393 (1981);<br></p>

<p>Applications It is an antifungal drug. It is used both in animal and in humans, to treat rigworm infections of the skin and nails. It is derived from the mold Penicillium griseofulvum.Environmental contaminants; Food contaminants<br>References Oxford, et al.: Biochem. J., 33, 240 (1939), Townley, E.R., et al.: Anal. Profiles Drug Subs., 8, 219 (1979),<br></p>

<p>Applications Broad spectrum aminocyclitol antibiotic and component of the Nebramycin complex, produced by a strain of Streptomyces tenebrarius. Antibacterial.<br>References Thompson, R.Q., et al.: Antimicrob. Agents Chemother., 332 (1967), Ryden, R., et al.: J. Antimicrob. Chemother., 3, 609 (1977), Smith, P., et al.: Clin. Therap., 23, 1231 (2001),<br></p>

<p>Applications 3-Chloro-D-alanine Methyl Ester Hydrochloride is an intermediate in the preparation of antibiotic D-Cycloserine (C988815) which inhibits cell wall biosynthesis in bacteria.<br>References Lamb., J.W., et al.: Anal. Profiles Drug Subs., 1, 53 (1972); Gentry-Weeks, C., et al.: J. Biol. Chem., 268, 7298 (1993); Alexander, F., et al.: Eur. J. Biochem., 219, 953 (1994); Auger, S., et al.: Biochimie, 87, 231 (2005); Chem and Eng. News p. 12, Dec. 7/14 (2015);<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>Impurity Ivermectin EP Impurity K<br>Applications 3,4-Dihydro Ivermectin is an impurity of Ivermectin (I940800), an antiparasitic drug that is active against a wide variety of nematode and arthropod parasites and is used to treat scabies and lice in humans. An invitro inhibitor of SARS-CoV-2/ Covid-19.<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 Campbell, W., et al.: Science, 221, 823 (1983); Glaziou, P., et al.: Trop. Med. Parasitol., 45, 253 (1994); Meinking, T., et al.: New Engl. J. Med., 333, 26 (1995); Caly, L., et al.: Antivir. Res., 178<br></p>

<p>Stability Light Sensitive<br>Applications A glycylcycline antibiotic, used to treat infection by drug resistant bacteria such as Staphylococcus aureus (Staph aureus) and Acinetobacter baumannii.<br>References Lim, T., et al.: J. Antibiotics, 62, 675 (2009), Presterl, E., et al.: Antimicrob. Agents Chemother., 53, 3205 (2009), Varma, M., et al.: J. Med. Chem., 52, 4844 (2009),<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 The L-diastereomer of the β-lactam antibiotic Cephalexin (C256800). It is transported by PEPT1 (the oligopeptide transporter responsible for absorption of peptide nutrients in the small intestine) with high affinity, but is not metabolized by PEPT1 itself.<br>References Mitsuoka, K. et al.: Biol. Pharmac. Bull., 32, 1459 (2009); Snyder, N.J. et al.: Antimicrob. Agents Chemother., 41, 1649 (1997);<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>Stability Hygroscopic<br>Applications Orally active, third generation cephalosporin antibiotic.<br>References Kamimura, T., et al.: Antimicrob. Agents Chemother., 25, 98 (1984),Yamanaka, H., et al.: J. Antibiot., 38, 1738 (1985), Guay, D.R.P., et al.: Antimicrob. Agents Chemother., 30, 485 (1986),<br></p>

<p>Applications Semi-synthetic antibiotic related to Penicillin. Antimicrobial.<br>References Robinson, B., et al.: Biochem. Med. Metab. Biol., 48, 122 (1992), Lesnefsky, E., et al.: J. Biol. Chem., 279, 47961 (2004), Marroquin, L., et al.: Toxicol. Sci., 97, 539 (2007),<br></p>

<p>Applications Azithromycin Dihydrate is a semi-synthetic macrolide antibiotic; related to Erythromycin A. Antibacterial.<br>References Langtry, H.D., et al.: Drugs, 56, 273 (1998),<br></p>

<p>Impurity Clarithromycin EP Impurity N<br>Applications (10E)-10,11-Didehydro-11-deoxy-6-O-methylerythromycin (Clarithromycin EP Impurity N) is a Erythromycin (E649950) derivative.<br></p>

<p>Applications OP-1118 is a major metabolite of Fidaxomicin (F335400).<br>References Babakhani, F., et al.: J. Med. Microbiol., 60, 1213 (2011); Allen, C., et al.: Antimicrob. Agents Chemother., 57, 664 (2013)<br></p>

<p>Applications Desmycosin is a 16-membered macrolide antibiotic and a metabolite of Tylosin (T947650). Desmycosin is also a precursor to Tilmicosin (T440500).<br>References Wal, J.M. et al.: J. Antibiot., 26, 687 (1973); Hu, D. et al.: Environ. Toxicol. Chem., 26, 884 (2007); Min, Y. et al.: Proc. Biochem., 42, 729 (2007);<br></p>

<p>Impurity Ceftazidime EP Impurity A<br>Stability Hygroscopic, Light Sensitive<br>Applications ∆2-Ceftazidime, 90% (Ceftazidime EP Impurity A) is a Ceftazidime isomer, an impurity of Ceftazidime (C244100).<br>References Vilanova, B., et al.: Helv. Chim. Acta, 76, 2789 (1993), Zhou, M., et al.: J. Pharm. Sci., 84, 534 (1995), Baertschi, S., et al.: Chemother. 8, 353 (1997), Porra, R., et al.: J. Pharm. Biomed. Anal., 18, 241 (1998),<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 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>Applications L-Penicillamine is a metabolite of penicillin. L-Penicillamine is used in the treatment of Wilson’s disease, Cystinuria, Scleroderma and arsenic poisoning.<br>References Marti-Prats, L., et al.: Neurosci. Lett., 483, 143 (2010), Singh, A., et al.: J. Pharm. Sci., 99, 3931 (2010), Everette, J., et al.: J. Agric. Food Chem., 58, 8139 (2010),<br></p>

<p>Applications Florfenicol is a fluorinated derivative of thiamphenicol. Florfenicol inhibits bacterial protein synthesis by binding to ribosome 50S and 70S subunits. Florfenicol is used as an antibacterial.<br>References Kim, E and Aoki, T.: Microbiol. Immunol., 40, 665, (1996), Keyes, K.: Antimicrob. Agents Chemother., 44, 421 (2000)<br></p>

<p>Applications Linezolid is a prototype of the oxazolidinone antimicrobials; inhibits bacterial mRNA translation.<br>References Brickner, S.J., et al.: J. Med. Chem., 39, 673 (1996), Ford, C.W., et al.: Antimicrob. Agents Chemother., 40, 1508 (1996), Rybak, M.J., et al.: Pharmacotherapy, 18, 456 (1998), Stevens, D.L., et al.: Clin. Infect. Dis., 34, 1481 (2002),<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 Very Hygroscopic<br>Applications Nebramine is a degradation product of the antibiotic Tobramycin (T524000).<br>References Brandl, M. et al.: Drug Dev. Indust. Pharm., 18, 1423 (1992); Ghinami, C. et al.: J. Chrom. A, 1139, 52 (2007)<br></p>

<p>Applications Isotope labelled Ivermectin, is the labeled analogue of Ivermectin (I940800), which is a semi-synthetic derivative of Abamectin; consists of a mixture of not less than 80% component B1a and not more than 20% component B1b. Antihelmintic (Onchocerca). An invitro inhibitor of SARS-CoV-2/ Covid-19.<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 Chabala, J.C., et al.: J. Med. Chem., 23, 1134 (1980), Campbell, W.C., et al.: Science, 221, 823 (1983), Bennett, J.L., et al.: Parasitol. Today, 4, 226 (1988), Plaisier, A.P., et al.: J. Infect. Dis., 172, 204 (1995), ; Caly, L., et al.: Antivir. Res., 178<br></p>

<p>Impurity Tacrolimus 8-Propyl Analog (USP)<br>Applications A novel analog of FK-506 (F370000) macrocycle.<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 Kino, T., et al.: J. Antibiot., 40, 1249 (1987), Motamedi, H., et al.: J. Bacteriol., 178, 5243 (1996), Dai, Y., et al.: Drug Metab. Dispos., 34, 836 (2006),<br></p>

<p>Impurity Mupirocin EP Impurity E<br>Stability Hygroscopic<br>Applications Mupirocin (M794000) impurity. The rearrangement isomer of Mupirocin is prepared using an enzyme-catalyzed, selective deesterification.<br>References Sime, J.T., et al.: Tetrahedron Lett., 28, 5169 (1987),<br></p>