Alternatives to P450 to produce Histamine H1 regioselectively APM. Although some P450 is known to bind substrates st Stronger than pharmaceutical Führungskr Forces with K m values between 1 and 70 mM is assigned, they generally have relatively low values of Kcat in the N Height of 0.2 or less s1 . Consequently, the catalytic efficiency for the oxidation of pharmaceutical AaeAPO in the same range as those of P450, as shown by our values for the hydroxylation of propranolol, metoprolol and O dealkylation of phenacetin O dealkylation. The value of k cat / K m, we obtain for acetanilide is much h Ago than the corresponding value for the P450-catalyzed reaction exists. ASA have some advantages over P450, P450 including currently available laboratory developed, where the reaction yields are affected. For example, led the conversion of diclofenac to 4 hydroxydiclofenac of mutants of P450cam in full conversion of 15 to 44% and the Pft GE by 10%. In contrast, wild-type was completely AaeAPO one Requests reference requests getting conversion of 78% and a yield of 68% for this reaction. In addition, APOs fungal P450 to be better than in practice for several other reasons: they use a little ben Co Co Teux substrate, H2O2, they term no reagents such as pyridine nucleotides Co Co Teux for examine the transient nature of the DAAC and AAC prodrugs of paracetamol and NTX the kinetics of hydrolysis of certain members of the series was examined. The t1 / 2 of the prodrugs are shown in Table 3. The presence of an amino group activates the acyl group to the hydroxide ion f attack due to the action of the amine function and Promotes the general base-catalyzed intramolecular hydrolysis.15, 16 The t1 / 2 of this activated ester is much smaller than the non-activated ester groups which these compounds to attractive candidate prodrug can. The kinetics of esters which an acyl group such as activated has been studied in detail. Bungaard et al. and other investigators have shown that the protonated and unprotonated prodrug hydrolysis subjected to Topoisomerase II different rates.17 19/2 lives of aminos acid esters of a dependence dependence of the pKa of the amine in the molecule that regulates the ratio ratio of protonated to unprotonated form at a certain pH. The shortest t1 / 2 of all prodrugs evaluated was 14.9 min for prodrug-PRO APAP HCl, 7c. This is an unexpected result on the basis of steric factors alone. However, it has been observed that piperazine dione 2 5 easily from dipeptide esters particularly those N-methylamino S Acids or proline. Be in the case of peptides, the proline, geometric factors control.20 To is the cyclization of dipeptide esters piperazines to occur, the peptide bond in the cis conformation, so can the terminal amino group and the carbonyl carbon ester interact k To the six cha form NONS. For example, ethyl ester cyclized glycylproline prolylglycine lighter than the ester due to the simplification Candesartan of the cis conformation. The case of 7c can utert through anything similar explanation Tion explained. Presence of proline ring system IX The NH group in an orientation that is more effective general base by f NH Promoted. In this context it is mentioned Interesting to note that Wu et al.