A Dipolar Cycloaddition Reaction To Access 6‑Methyl-4,5,6,7-tetrahydro‑1H‑[1,2,3]triazolo[4,5‑c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate - Chrovian, Christa C; Soyode-Johnson, Akinola; Peterson, Alexander A; Gelin, Christine F; Deng, Xiaohu; Dvorak, Curt A; Carruthers, Nicholas I; Lord, Brian; Fraser, Ian; Aluisio, Leah; Coe, Kevin J; Scott, Brian; et al. (Journal of medicinal chemistry, 2018)
Keywords: Animals; Chemistry, Medicinal; Cycloaddition Reaction; Dogs; Drug Design; Humans; Life Sciences & Biomedicine; Male; Mice; Models, Molecular; Molecular Conformation; Pharmacology & Pharmacy; Purinergic P2X Receptor Antagonists - chemical synthesis; Purinergic P2X Receptor Antagonists - chemistry; Purinergic P2X Receptor Antagonists - pharmacokinetics; Purinergic P2X Receptor Antagonists - pharmacology; Pyridines - chemical synthesis; Pyridines - chemistry; Pyridines - pharmacokinetics; Pyridines - pharmacology; Rats; Receptors, Purinergic P2X7 - metabolism; Science & Technology; Stereoisomerism; Tissue Distribution; RHEUMATOID-ARTHRITIS; EFFICACY; SAFETY; PHARMACOLOGICAL CHARACTERIZATION; CLICK CHEMISTRY; DISEASE; RECEPTOR; IDENTIFICATION; AZIDE