JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00935
Abstract: The discovery of a novel 2-aminotetrahydropyridine class of BACE1 inhibitors is described. Their pKa and lipophilicity were modulated by a pending sulfonyl group, while good permeability and brain penetration were achieved via intramolecular hydrogen bonding.… read more here.
Keywords: bace1 inhibitor; selective bace1; jnj 67569762; discovery ... See more keywords
Discovery of an Extremely Potent Thiazine-Based β-Secretase (BACE1) Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01140
Abstract: Genetic evidence points to deposition of amyloid-β (Aβ) as a causal factor for Alzheimer's disease. Aβ generation is ini-tiated when β-secretase (BACE1) cleaves the amyloid precursor protein. Starting with an oxazine lead 1, we describe… read more here.
Keywords: bace1 inhibitor; thiazine based; low projected; secretase bace1 ... See more keywords
Discovery of Sulforaphane as a Potent BACE1 Inhibitor Based on Kinetics and Computational Studies
Sign Up to like & getrecommendations! Published in 2020 at "Nutrients"
DOI: 10.3390/nu12103026
Abstract: BACE1 is the rate-limiting enzyme involved in the production and deposition of β-amyloid (Aβ). Since neurotoxic Aβ plays a critical role in Alzheimer’s disease (AD) pathogenesis, BACE1 has emerged as a key target for preventing… read more here.
Keywords: discovery sulforaphane; bace1 inhibitor; sulforaphane; potent ... See more keywords