A later team at Zambon modified the pyrrolidine with a pyrrolidone could produce an analogue some 318x morphine in its analgesic activity in animal studies ( the latter overlays beta hydroxy fentanyl ).
22.
Some trials have been made, e . g . by replacing the pyrrolidine with a polar negatively charged side-chains as well as hydrophilic substitution can lead to excellent inhibitory activity.
23.
The polar reaction, N-cyclo " pen " tenyl pyrrolidine nucleophilic addition to the diazo compound, proceeds 1, 500 times faster in polar DMSO than in non-polar decalin.
24.
Then hydroxylation of both the aromatic ring and side chain takes place followed by an oxidation of the pyrrolidine ring to the corresponding lactam, with subsequent detachment and ring opening to the corresponding carboxylic acid.
25.
The development and modification of Enders'hydrazone alkylation reaction mainly focus on the addition of more steric hindrance on the pyrrolidine rings of both SAMP and RAMP, while preserving the methoxy group for lithium chelation.
26.
Ring A is synthesized from L-proline through the nonribosomal peptide synthase ( NRPS ) pathway ( figure 2 ), wherein the pyrrolidine ring of proline is oxidized twice through FAD + to yield pyrrole ring A.
27.
Like its more toxic relatives, " Nicandra physalodes " is alkaloidal, analyses having revealed the presence of the tropane alkaloid tropinone and the pyrrolidine alkaloid hygrine ( 0.1 %, in the root ).
28.
The main metabolic steps are thought to be demethylenation followed by methylation of one hydroxy group, aromatic and side chain hydroxylation, oxidation of the pyrrolidine ring to the corresponding lactam as well as ring opening to the corresponding carboxylic acid.
29.
On the other hand, a close analog of this reaction, N-cyclo " hex " enyl pyrrolidine 1, 3-dipolar cycloaddition to dimethyl diazomalonate, is sped up only 41-fold in DMSO relative to decalin.
30.
In addition, a salt bridge between Glu-97 of thrombin and the amidine group fixed in the pyrrolidine ring of DX-9065a reduces the flexibility of the DX-9065a molecule, which now cannot rotate enough to avoid the electrostatic clash.
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