Healthcare careers for chemists are once again largely based in laboratories, although increasingly there is opportunity to work at the point of care, helping with patient investigation. 4330-21-6, Name is Hoffer’s chlorosugar, SMILES is O=C(O[C@@H]1[C@@H](COC(C2=CC=C(C)C=C2)=O)O[C@H](Cl)C1)C3=CC=C(C)C=C3, in an article , author is Lafite, Pierre, once mentioned of 4330-21-6, Name: Hoffer’s chlorosugar.
Twenty five derivatives of the drugs terfenadine and ebastine have been designed, synthesized and evaluated as inhibitors of recombinant human CYP2J2. Compound 14, which has an imidazole substituent, is a good non-competitive inhibitor of CYP2.12 (IC50 – 400 nM). It is not selective towards CYP2.12 as it also efficiently inhibits the other main vascular CYPs, such as CYP2B6, 2C8. 2C9 and 3A4: however, it could be an interesting tool to inhibit all these vascular CYPs. Compounds 4, 5 and 13, which have a propyl, allyl and benzo-1,3-dioxole terminal group, respectively, are selective CYP2J2 inhibitors. Compound 4 is a high-affinity, competitive inhibitor and alternative substrate of CYP2J2 (K-i = 160 50 nM). Compounds 5 and 13 are efficient mechanism-based inhibitors of CYP2J2 (k(inact)/K-i values similar to 3000 L mol(-1) s(-1)). Inactivation of CYP2J2 by 13 is due to the formation of a stable iron-carbene bond which occurs upon CYP2J2-catalyzed oxidation of 13 with a partition ratio of 18 +/- 3. These new selective inhibitors should be interesting tools to study the biological roles of CYP2J2. Published by Elsevier Inc.
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Reference:
1,3-Benzodioxole – Wikipedia,
,Dioxole | C3H4O2 – PubChem