Synthesis and pharmacological evaluation of DHβE analogs as neuronal nicotinic acetylcholine receptor antagonists
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Synthesis and pharmacological evaluation of DHβE analogs as neuronal nicotinic acetylcholine receptor antagonists. / Jepsen, Tue H.; Jensen, Anders A.; Lund, Mads Henrik; Glibstrup, Emil; Kristensen, Jesper Langgaard.
In: A C S Medicinal Chemistry Letters, Vol. 5, No. 7, 2014, p. 766-770.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Synthesis and pharmacological evaluation of DHβE analogs as neuronal nicotinic acetylcholine receptor antagonists
AU - Jepsen, Tue H.
AU - Jensen, Anders A.
AU - Lund, Mads Henrik
AU - Glibstrup, Emil
AU - Kristensen, Jesper Langgaard
PY - 2014
Y1 - 2014
N2 - Dihydro-β-erythroidine (DHβE) is a member of the Erythrina family of alkaloids and a potent competitive antagonist of the α4β2-subtype of the nicotinic acetylcholine receptors (nAChRs). Guided by an X-ray structure of DHβE in complex with an ACh binding protein, we detail the design, synthesis, and pharmacological characterization of a series of DHβE analogues in which two of the four rings in the natural product has been excluded. We found that the direct analogue of DHβE maintains affinity for the α4β2-subtype, but further modifications of the simplified analogues were detrimental to their activities on the nAChRs.
AB - Dihydro-β-erythroidine (DHβE) is a member of the Erythrina family of alkaloids and a potent competitive antagonist of the α4β2-subtype of the nicotinic acetylcholine receptors (nAChRs). Guided by an X-ray structure of DHβE in complex with an ACh binding protein, we detail the design, synthesis, and pharmacological characterization of a series of DHβE analogues in which two of the four rings in the natural product has been excluded. We found that the direct analogue of DHβE maintains affinity for the α4β2-subtype, but further modifications of the simplified analogues were detrimental to their activities on the nAChRs.
U2 - 10.1021/ml500094c
DO - 10.1021/ml500094c
M3 - Journal article
C2 - 25050162
VL - 5
SP - 766
EP - 770
JO - ACS Medicinal Chemistry Letters
JF - ACS Medicinal Chemistry Letters
SN - 1948-5875
IS - 7
ER -
ID: 111182137