N‐Benzyl piperidine Fragment in Drug Discovery

• Published in: ChemMedChem Vol. 19; no. 20; pp. e202400384 - n/a
• Main Authors: Sharma, Ankita, Sharma, Mohit, Bharate, Sandip B.
• Format: Journal Article
• Language: English
• Published: Germany Wiley Subscription Services, Inc 16-10-2024
• Subjects: ADME; Drug development; Drug Discovery; Drug interaction; Drugs; Heterocycles; Humans; Medicinal chemistry; Molecular Structure; N-Benzyl piperidine; Physicochemical properties; Piperidine; Piperidines - chemical synthesis; Piperidines - chemistry; Piperidines - pharmacology; Protein structure; Therapeutic targets; Toxicity; Heterocycles; N-Benzyl piperidine; Medicinal chemistry; Drug discovery; ADME
• ISSN: 1860-7179; 1860-7187; 1860-7187
• DOI: 10.1002/cmdc.202400384

The N‐benzyl piperidine (N‐BP) structural motif is commonly employed in drug discovery due to its structural flexibility and three‐dimensional nature. Medicinal chemists frequently utilize the N‐BP motif as a versatile tool to fine‐tune both efficacy and physicochemical properties in drug development. It provides crucial cation‐π interactions with the target protein and also serves as a platform for optimizing stereochemical aspects of potency and toxicity. This motif is found in numerous approved drugs and clinical/preclinical candidates. This review focuses on the applications of the N‐BP motif in drug discovery campaigns, emphasizing its role in imparting medicinally relevant properties. The review also provides an overview of approved drugs, the clinical and preclinical pipeline, and discusses its utility for specific therapeutic targets and indications, along with potential challenges.
This review focuses on the significance of the N‐BP motif in drug discovery efforts, emphasizing its contribution in imparting medicinally relevant properties. The article covers approved drugs, the current clinical and preclinical pipelines, and explores its applicability to specific therapeutic targets and indications, while also addressing potential challenges.