Toxicologie

<p>Applications [[(1R)-2-(6-Amino-9H-purin-9-yl)-1-methylethoxy]methyl]monophenylester is an antiviral agent and a Tenofovir (T018500) intermediate. Tenofovir is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor, used as an anti-HIV agent.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997); Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005); Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006); Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007);<br></p>

<p>Applications (1R,​4S)​-3-​Oxo-2-​azabicyclo[2.2.1]​hept-​5-​ene-​2-​carboxylic acid 1,​1-​Dimethylethyl Ester is an intermediate in synthesizing ent-Abacavir (Abacavir EP Impurity A) (A105015), an enatiomer of Abacavir (A105000). Abacavir is a carbocyclic 2'-deoxyguanosine nucleoside reverse transcriptase inhibitor and an anti-HIV drug used to treat HIV infection (1). Intracellular enzymes convert Abacavir to its active form, carbovir-triphosphate (CBV-TP), which then selectively inhibits HIV reverse transcriptase by incorporating into viral DNA (2). Abacavir is metabolized in the liver by uridine diphosphate glucuronyltransferase and alcohol dehydrogenase resulting in inactive glucuronide and carboxylate metabolites, respectively.<br></p>

<p>Applications 5-Amino-1-N-methylindole (CAS# 102308-97-4) is an indole derivative and building block, used in the copper-catalyzed synthesis of sulfonamides.<br>References Chen, Y.; et al.: J. Am. Chem. Soc., 140, 8781 (2018);<br></p>

<p>Applications 2-methoxy-3-pyridinesulfonyl chloride is patented as a reactant used to prepare erythromycin macrolide antibiotics as antibacterial and antiprotozoal agents.<br></p>

<p>Applications 4-(2-Propyn-1-yloxy) Trimethoprim is an analog of T795615, which is an antibacterial compound and a contaminant of emerging concern (CECs).<br>References Manius, G.J., et al.: Anal. Profiles Drug Subs., 7, 445 (1978), Roth, B., et al.: J. Med. Chem., 23, 379 (1980), Brogden, R.N., et al.: Drugs, 23, 405 (1982),<br></p>

<p>Applications Ganciclovir derivative.<br>References Albers, E., et al.: J. Pharm. Sci., 81, 756 (1992), Dias, C., et al.: J. Pharm. Sci., 91, 6607 (2002), Macha, S., et al.: Drug Metab. Dispos., 30, 670 (2002),<br></p>

<p>Applications 7-[[(2Z)-2-(2-Amino-4-thiazolyl)-2-[(carboxymethoxy)imino]acetyl]amino]-cefixime is a cefixime impurity. Cefixime (C242800) is an 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 2,5-Thiazolylmethyl Diacarbonate is an impurity of Ritonavir (R535000), a selective HIV protease inhibitor.<br>References Daluge, S., et al.: Antimicrob. Agents Chemother., 38, 1590 (1994); Ammaranond, P., et al.: J. Clin. Virol., 26, 153 (2003); Harrigan, P., et al.: J. Infect. Dis., 191, 339 (2005); Miller, J., et al.: Bioorg. Med. Chem. Lett., 16, 1788 (2006); Koppala, S., et al.: J. Chromatogr. Sci., 53, 662 (2015);<br></p>

<p>Stability Temperature Sensitive<br>Applications Antibiotic A21 is a new polyene macrolide Amphotericin amide antibiotic with antimycotic effectiveness.<br>References Flores-Romero, J. D., et al.: Org. Process Res. Dev., 20, 1529 (2016), Antillon, A., et al.: PLoS One, 11, 9 (2016)<br></p>

<p>Applications N-Hydroxy-methyl Methoxy Tenofovir Alfenamide is an impurity of Tenofovir (T018500) which is an acyclic phosphonate nucleotide analogue and reverse transcriptase inhibitor. It is used as an anti-HIV agent. Antiviral.<br>References Shaw, J.-P., et al.: Pharm. Res., 14, 1824 (1997); Wyles, D., et al.: Clin Infect. Dis., 40, 174 (2005), Peng, J., et al.: J. Clin. Pharmacol., 46, 265 (2006), Seminari, E., et al.: J. Antimicrob. Chemother., 60, 831 (2007);<br></p>

<p>Applications (±)-Miconazole-d5 Nitrate (2,4-dichlorobenzyloxy-d5) (CAS# 1398065-80-9) is the labelled version of Miconazole Nitrate (M342500(P)), which is an anti-fungal. Miconazole Nitrate’s corrosion inhibition performance has been studied with 5083 aluminum alloy.<br>References Godefroi, E.F., et al.: J. Med. Chem., 12, 784 (1969); Brugmans, et al.: Arch. Dermatol., 102, 428 (1970); Heel, R.C., et al.: Drugs, 19, 7 (1980); Zhang, T., et al.: Corros. Sci., 176, 108930 (2020)<br></p>

<p>Applications Carboxylic acid derivative of Bifendate (B382890), a synthetic intermediate of Schisandrin C and also a anti-HBV drug used in the treatment of chronic hepatitis B.<br>References Pan, S.Y., et al.: Euro. J. Pharmacol. 522, 170 (2006); Zeng, Y., et al.: Acta. Pharmacol. Sinica., 30, 478 (2009);<br></p>

<p>Applications α-[2-[Methyl(1-naphthalenylmethyl)amino]ethyl]-Benzenemethanol is an impurity of naftifine (N213100) an antifungal.<br>References Stuetz, A., et al.: Journal of Medicinal Chemistry, 29, 112 (1986)<br></p>

<p>Applications β-Amyrin is used as a protein tyrosine phosphatase 1B inhibitor with potential treatment towards diabetes. Also used in the synthesis of HIV-1 integrase inhibitory compounds based upon plant extracts.<br>References Zhang, Y. et al.: Bioorg, Med. Chem., 16, 8697 (2008); Tewtrakul, S. et al.: Phytother. Res., 17, 232 (2003);<br></p>

<p>Applications An Efavirenz (E425000) impurity.<br></p>

<p>Applications (R)-8-Hydroxy-3-methyl-1,2,3,4-tetrahydrobenz[a]anthracene-7,12-dione (cas# 681001-30-9) is a compound useful in organic synthesis.<br></p>