N-Desethyl vardenafil is a metabolite of vardenafil , a phosphodiesterase 5 inhibitor, that is formed by the action of cytochrome P450 (CYP)3A4 and CYP3A5.
N-Desethyl Bimatoprost (17-phenyl trinor PGF2α amide) is an F-series PG analog in which the C-1 carboxyl group has been modified to an unsubstituted amide. PG esters have been shown to have ocular hypotensive activity. PG N-ethyl amides were recently introduced as alternative PG hypotensive prodrugs. Although it has been claimed that PG amides are not converted to the free acids in vivo, studies have shown that bovine and human corneal tissue converts the amides of various PGs to the free acids with a conversion efficiency of about 10-20% relative to the hydrolysis of isopropyl esters. 17-phenyl trinor PGF2α amide would be expected to show the typical intraocular effects of latanoprost, but with the much slower hydrolysis pharmacokinetics of the PG N-amides.
N-desethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1It inhibits CAII and CAIV activities (IC50s = 1.28 and 128 nM, respectively). 1.Kim, C.-Y., Whittington, D.A., Chang, J.S., et al.Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IVJ. Med. Chem.45(4)888-893(2002)
N-Desethyl-N-methyl Vardenafil, a potential impurity in commercial vardenafil preparations, functions as a phosphodiesterase 5 (PDE5) inhibitor, similar to its parent compound. With an IC50 value of 2 nM, it exhibits potent inhibitory activity against PDE5.