Holladay, Mark W.; Bai, Hao; Li, Yihong; Lin, Nan-Horng; Daanen, Jerome F.; Ryther, Keith B.; Wasicak, James T.; Kincaid, John F.; He, Yun; Hettinger, Anne-Marie; Huang, Peggy; Anderson, David J.; Bannon, Anthony W.; Buckley, Michael J.; Campbell, Jeffrey E.; Donnelly-Roberts, Diana L.; Gunther, Karen L.; Kim, David J. B.; Kuntzweiler, Theresa A.; Sullivan, James P.; Decker, Michael W.; Arneric, Stephen P. published the artcile< Structure-activity studies related to ABT-594, a potent nonopioid analgesic agent: effect of pyridine and azetidine ring substitutions on nicotinic acetylcholine receptor binding affinity and analgesic activity in mice>, Application of C5H4ClNO, the main research area is ABT594 analog nonopioid analgesic structure; nicotinic receptor binding ABT594 analog structure.
Analogs of A-98593 (I) and its enantiomer ABT-594 (II) with diverse substituents on the pyridine ring were prepared and tested for affinity to nicotinic acetylcholine receptor binding sites in rat brain and for analgesic activity in the mouse hot plate assay. Numerous types of modifications were consistent with high affinity for [3H]cytisine binding sites. By contrast, only selected modifications resulted in retention of analgesic potency in the same range as I and II. Analogs of II with one or two Me substituents at the 3-position of the azetidine ring also were prepared and substantially less active in both assays.
Bioorganic & Medicinal Chemistry Letters published new progress about Analgesics. 96630-88-5 belongs to class pyridine-derivatives, and the molecular formula is C5H4ClNO, Application of C5H4ClNO.