N-Benzyl piperidine Fragment in Drug Discovery.

Autor: Sharma A; Natural Products & Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu, 180001, India.; Academy of Scientific & Innovative Research (AcSIR), Ghaziabad, 201002, India., Sharma M; Natural Products & Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu, 180001, India.; Academy of Scientific & Innovative Research (AcSIR), Ghaziabad, 201002, India., Bharate SB; Natural Products & Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu, 180001, India.; Academy of Scientific & Innovative Research (AcSIR), Ghaziabad, 201002, India.; Department of Natural Products & Medicinal Chemistry, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad, 500007, India.
Jazyk: angličtina
Zdroj: ChemMedChem [ChemMedChem] 2024 Oct 16; Vol. 19 (20), pp. e202400384. Date of Electronic Publication: 2024 Aug 23.
DOI: 10.1002/cmdc.202400384
Abstrakt: 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.
(© 2024 Wiley-VCH GmbH.)
Databáze: MEDLINE
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