Antifongiques

<p>Itraconazole is an anti-fungal drug that inhibits the synthesis of ergosterol, a component of the fungal cell membrane. Itraconazole is in a class of antifungals called triazoles. The drug binds to ergosterol in the fungal cell membrane and prevents it from being inserted into the membrane. This decreases the permeability of the plasma membrane, causing leakage of cellular contents. Additionally, it has been shown to have a glucose-lowering effect in the treatment of acute leukaemia and may be used for research in aiding to diagnose hematopoietic stem cell or leukaemia.</p>

<p>A fungicide</p>

<p>Folpet-d4 is a deuterated compound of Folpet. Folpet has a CAS number of 133-07-3. Folpet,a widely used dicarboximide fungicide,induces tumors in the mouse gastrointestinal tract,primarily in the duodenum,and is also cytotoxic effect on human bronchial epithelial cells.</p>

<p>Applications A bactericidal and fungicidal.<br>References Schoppelrei, J., et al.: J. Phys. Chem., 100, 14343 (1996), Kolb, H., et al.: Drug Discovery Today, 8, 1128 (2003),<br></p>

<p>Applications 5-​(2-​Chlorophenyl)​-​3-​cyclopropyl-​4,​5-​dihydro-1H-​pyrazole is an intermediate in synthesizing Sedaxane (S242000), a broad-spectrum seed treatment fungicide used for control of seed- and soil-borne diseases in a broad range of crops. It inhibits fungal respiration by binding to the succinate dehydrogenase complex in the fungal mitochondrium.<br>References Zeun, R., et al.: Pest Manag. Sci., 69, 527 (2013); Oostendorp, M., et al.: Phytopathology, 101, S133 (2011); Olaya, G., et al.: Phytopathology, 101, S132 (2011)<br></p>

<p>Applications Rhein Methylate 3-(2,3,4,6-Tetraacetate β-D-Glucopyranose) is an intermediate in synthesizing Rhein 8-Glucoside (R318520), which has been seen to exhibit cytotoxic and DNA-damaging properties towards tumor and normal human cells. In addition it has been shown to be an inhibitor of PTP1B (Human Protein Tyrosine Kinase 1B) in vitro. It is an analog of Rhein (318500) which is found in the free state and as glucoside in Rheum spp, Polygonaceae (rhubarb) and in Senna leaves. It is a potential antioxidant resource: endophytic fungi from medicinal plants.<br>References Wanitschke, Pharmacology, 20, Suppl. 1, 21 (1980); Raimondi, L., et al.: Pharmacol. Res. Commun., 14, 103 (1982); Franchi-Micheli, S., et al.: J. Pharm. Pharmacol., 35, 262 (1983); Li, S. et al.: J. Asian Nat. Prod. Res., 8, 281 (2006); Shi, Y.Q. et al.: Anticancer. Res., 21, 2847 (2001)<br></p>

<p>Applications 3-Methyl-3-phenylamino-1-butyne is an intermediate in the synthesis of Endophenazine A which is a new phenazine antibiotic isolated from the arthropod associated endosymbiont Streptomyces anulatus and shows antimicrobial activities against Gram-positive bacteria and some filamentous fungi, and herbicidal activity against Lemna minor (duckweed).<br>References Gebhardt, K., et al.: J. Antibiot., 55, 794 (2002)<br></p>

<p>Applications 2-[(6-Chloro-4-pyrimidinyl)oxy]-α-(dimethoxymethyl)benzeneacetic Acid Methyl Ester is an impurity of Azoxystrobin (A965150), an strobilurin fungicide.<br>References Liu H.J., et al.: J. Chin. Chem. Soc., 60, 27 (2013);<br></p>

<p>Applications o-Tolylglyoxylic Acid Methyl Ester is an intermediate in the synthesis of Trifloxystrobin (T778900), a broad-spectrum foliar fungicide used in plant protection.<br></p>

<p>Applications 2-Demethyl Mandestrobin is an intermediate used in the synthesis of Mandestrobin (M162555), which is a novel fungicide having a methoxyacetamid structure. Mandestrobin also shows safer profiles for human health and the environment.<br>References Hirotomi, D., &amp; Kiguchi, S.: PCT Int. Appl., WO 2017026526 A1 20170216 (2017)<br></p>

<p>Applications R406 is a potent Syk inhibitor which affects Dectin-1-mediated signalling in mammilian cells. R406 thus acts an anti-fungal agent. Also a potential anti-leukemia agent, through modulation of sphingosine-1 phosphate receptor 1 (S1PR1).<br>References Borge, M. et al.: J. Immunol., 193, 3165 (2014); Kimura, Y. et al.: J. Biol. Chem., 289, 31565 (2014);<br></p>

<p>Applications (5E)-5-(3-Bromopropylidene)-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-ol is an intermediate in the synthesis of 10-Hydroxy (E)-Amitriptyline (D462790). (5E)-5-[3-(dimethylamino)propylidene]-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-ol is a metabolite of amitriptyline (A633350) which is a dibenzocycloheptadiene derivative and an antidepressant (1). Amitriptyline is also a TrkA and TrkB receptor agonist and exhibits neurotrophic and anti-inflammatory activities (2,3). Drinking water contaminant candidate list 3 (CCL 3) compound as per United States Environmental Protection Agency (EPA).<br></p>

<p>Applications 2-[[[1-(4-Chlorophenyl)-1H-pyrazol-3-yl]oxy]methyl]benzenamine is an intermediate used in the synthesis of (P840402), which is an isotope labelled Pyraclostrobin, a fungicide for use in seed grass and food crops.<br>References Gyldenkaerne, S., et al.: Pestic Sci., 55, 1210 (1999), Pennington, D., et al.: Environ. Sci. Technol., 39, 1119 (2005), Wang, S., et al.: Food Control., 18, 731 (2007),<br></p>

<p>Applications (5E)-5-(3-Bromopropylidene)-5,11-dihydro-10H-dibenzo[a,d]cyclohepten-10-one is an intermediate in the synthesis of 10-Hydroxy (E)-Amitriptyline (D462790). (5E)-5-[3-(dimethylamino)propylidene]-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-10-ol is a metabolite of amitriptyline (A633350) which is a dibenzocycloheptadiene derivative and an antidepressant (1). Amitriptyline is also a TrkA and TrkB receptor agonist and exhibits neurotrophic and anti-inflammatory activities (2,3). Drinking water contaminant candidate list 3 (CCL 3) compound as per United States Environmental Protection Agency (EPA).<br></p>

<p>Applications Methyl 2-[2-[(2,5-Dimethylphenoxy)methyl]phenyl]-2-(hydroxy)acetic Acid Ester is an intermediate used in the synthesis of Mandestrobin (M162555), which is a novel fungicide having a methoxyacetamid structure. Mandestrobin also shows safer profiles for human health and the environment.<br>References Hirotomi, D., &amp; Kiguchi, S.: PCT Int. Appl., WO 2017026526 A1 20170216 (2017)<br></p>