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- W2005087793 endingPage "419" @default.
- W2005087793 startingPage "379" @default.
- W2005087793 abstract "Aliphatic nitrogen heterocycles such as piperazine, piperidine, pyrrolidine, morpholine, aziridine, azetidine, and azepane are well known building blocks in drug design and important core structures in approved drug therapies. These core units have been targets for metabolic attack by P450s and other drug metabolizing enzymes such as aldehyde oxidase and monoamine oxidase (MAOs). The electron rich nitrogen and/or α-carbons are often major sites of metabolism of alicyclic amines. The most common biotransformations include N-oxidation, N-conjugation, oxidative N-dealkylation, ring oxidation, and ring opening. In some instances, the metabolic pathways generate electrophilic reactive intermediates and cause bioactivation. However, potential bioactivation related adverse events can be attenuated by structural modifications. Hence it is important to understand the biotransformation pathways to design stable drug candidates that are devoid of metabolic liabilities early in the discovery stage. The current review provides a comprehensive summary of biotransformation and bioactivation pathways of aliphatic nitrogen containing heterocycles and strategies to mitigate metabolic liabilities." @default.
- W2005087793 created "2016-06-24" @default.
- W2005087793 creator A5022853919 @default.
- W2005087793 creator A5027600676 @default.
- W2005087793 creator A5029214116 @default.
- W2005087793 creator A5041334425 @default.
- W2005087793 creator A5047096854 @default.
- W2005087793 creator A5049065288 @default.
- W2005087793 date "2014-06-09" @default.
- W2005087793 modified "2023-10-08" @default.
- W2005087793 title "Biotransformation and bioactivation reactions of alicyclic amines in drug molecules" @default.
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