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7β-Methyl substituent is a structural locus associated with activity cliff for nepenthone analogues.
Sun HJ, Wang YH, Yuan CM, Kong LH, Xu XJ, Wang YJ, Wu HH, Lin C, Qian YY, Huang HM, Xiao L, Liu X, He Q, Fang SY, Xue DQ, Yang XC, Chen H, Zheng YL, Zheng L, Yu LQ, Xie Q, Fu W, Li W, Liu JG, Qiu ZB, Shao LM. Sun HJ, et al. Bioorg Med Chem. 2018 Aug 7;26(14):4254-4263. doi: 10.1016/j.bmc.2018.07.020. Epub 2018 Jul 24. Bioorg Med Chem. 2018. PMID: 30054192
Discovery of a Highly Selective and Potent κ Opioid Receptor Agonist from N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaines with Reduced Central Nervous System (CNS) Side Effects Navigated by the Message-Address Concept.
Xiao L, Wang Y, Zhang M, Wu W, Kong L, Ma Y, Xu X, Liu X, He Q, Qian Y, Sun H, Wu H, Lin C, Huang H, Ye R, Jiang S, Ye RF, Yuan C, Fang S, Xue D, Yang X, Chen H, Zheng Y, Yu L, Xie Q, Zheng L, Fu W, Li W, Qiu Z, Liu J, Shao L. Xiao L, et al. J Med Chem. 2019 Dec 26;62(24):11054-11070. doi: 10.1021/acs.jmedchem.9b00857. Epub 2019 Dec 6. J Med Chem. 2019. PMID: 31738550
Discovery, synthesis, biological evaluation and structure-based optimization of novel piperidine derivatives as acetylcholine-binding protein ligands.
Shen J, Yang XC, Yu MC, Xiao L, Zhang XJ, Sun HJ, Chen H, Pan GX, Yan YR, Wang SC, Li W, Zhou L, Xie Q, Yu LQ, Wang YH, Shao LM. Shen J, et al. Among authors: sun hj. Acta Pharmacol Sin. 2017 Jan;38(1):146-155. doi: 10.1038/aps.2016.124. Epub 2016 Dec 5. Acta Pharmacol Sin. 2017. PMID: 27917874 Free PMC article.
474 results