An analysis of successful hit-to-clinical candidate pairs

DG Brown - Journal of medicinal chemistry, 2023 - ACS Publications
An analysis of 156 published clinical candidates from the Journal of Medicinal Chemistry
between 2018 and 2021 was conducted to identify lead generation strategies most …

Recent advances in Alzheimer's disease: Mechanisms, clinical trials and new drug development strategies

J Zhang, Y Zhang, J Wang, Y Xia, J Zhang… - Signal transduction and …, 2024 - nature.com
Alzheimer's disease (AD) stands as the predominant form of dementia, presenting significant
and escalating global challenges. Its etiology is intricate and diverse, stemming from a …

Therapeutic targeting of α7 nicotinic acetylcholine receptors

RL Papke, NA Horenstein - Pharmacological Reviews, 2021 - ASPET
The α 7-type nicotinic acetylcholine receptor is one of the most unique and interesting of all
the members of the cys-loop superfamily of ligand-gated ion channels. Since it was first …

Recent advances in the discovery of nicotinic acetylcholine receptor allosteric modulators

D Manetti, S Dei, HR Arias, L Braconi, A Gabellini… - Molecules, 2023 - mdpi.com
Positive allosteric modulators (PAMs), negative allosteric modulators (NAMs), silent
agonists, allosteric activating PAMs and neutral or silent allosteric modulators are …

Allosteric activation of α7 nicotinic acetylcholine receptors by novel 2-arylamino-thiazole-5-carboxylic acid amide derivatives for the improvement of cognitive deficits …

C Yang, Y Meng, X Wang, X Li, T Yu… - Journal of Medicinal …, 2024 - ACS Publications
Enhancing α7 nAChR function serves as a therapeutic strategy for cognitive disorders. Here,
we report the synthesis and evaluation of 2-arylamino-thiazole-5-carboxylic acid amide …

Catalytic enantioselective domino alkenylation-alkynylation of alkenes: stereoselective synthesis of 5–7 membered azacycles and carbocycles

Z Ma, L Sun, JS Zhou - Science China Chemistry, 2023 - Springer
Catalytic enantioselective domino alkenylation-alkynylation of alkenes: stereoselective
synthesis of 5–7 membered azacycles an Page 1 •COMMUNICATIONS• June 2023 Vol.66 …

Nicotinic receptors in airway disease

NA Borkar, MA Thompson… - … of Physiology-Lung …, 2024 - journals.physiology.org
With continued smoking of tobacco products and expanded use of nicotine delivery devices
worldwide, understanding the impact of smoking and vaping on respiratory health remains a …

Pro-cognitive effects of the GlyT1 inhibitor Bitopertin in rodents

S Deiana, W Hauber, A Munster, S Sommer… - European Journal of …, 2022 - Elsevier
Abstract N-methyl-D-aspartate-receptor (NMDAR) hypofunction contributes to cognitive
impairments in neuropsychiatric disorders such as schizophrenia. Reduced NMDAR …

Synthesis and biological evaluation of novel triazine derivatives as positive allosteric modulators of α7 nicotinic acetylcholine receptors

X Wang, H Xiao, J Wang, Z Huang… - Journal of Medicinal …, 2021 - ACS Publications
Enhancing neuronal α7 nicotinic acetylcholine receptor (α7 nAChR) function can alleviate
cognitive deficits. Here, we report the design, synthesis, and evaluation of N-(4 …

An approach to pharmacological targets of pyrrole family from medicinal chemistry viewpoint

ES Moghadam, K Mireskandari… - Mini Reviews in …, 2022 - ingentaconnect.com
Pyrrole is one of the most widely used heterocycles in the pharmaceutical industry. Due to
the importance of pyrrole structure in drug design and development, herein, we tried to …