期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 3, 页码 1550-1555出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm5013243
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资金
- National Health and Medical Research Council (NHMRC) [APP1049564, APP1055134]
Herein we describe the hybridization of a benzoxazinone M-1 scaffold with D-2 privileged structures derived from putative and clinically relevant antipsychotics to develop designed multiple ligands. The M-1 mAChR is an attractive target for the cognitive deficits in key CNS disorders. Moreover, activity at D-2 and 5-HT2A receptors has proven useful for antipsychotic efficacy. We identified 9 which retained functional activity at the target M-1 mAChR and D2R and demonstrated high affinity for the 5-HT2AR.
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