Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives
The 7-benzylidenenaltrexone (BNTX) derivatives 2a–v, 3a–c, 13a–c, and 14a were synthesized from naltrexone (1) and evaluated for their antitrichomonal activity. The structure-activity-relationship studies found that 4-iodo-BNTX (2g) showed the highest act
Synthesis and stereochemical assignment of 7-arylidene and 7-heteroarylidene morphinan-6-ones
A number of (E)-7-arylidenenaltrexones were synthesized by azeotropic distillation of water from a benzene solution of naltrexone and an aromatic aldehyde (benzaldehyde, 4-chloro- and 4-fluorobenzaldehyde, 3- and 4-pyridinecarboxaldehyde and 1-methyl-2-im
Nan, Yang,Upadhyaya, Subhash P.,Xu, Wei,Hughes, Kathrine E.,Dunn III, William J.,Bauer, Ludwig,Bhargava, Hemendra N.,Doss, George A.
(E)- and (Z)-7-arylidenenaltrexones: Synthesis and opioid receptor radioligand displacement assays
The E-isomer of 7-benzylidenenaltrexone (BNTX, 1a) was reported by Portoghese as a highly selective δ-opioid antagonist. The corresponding Z- isomer 1b was not readily available through direct aldol condensation of naltrexone (6) with benzaldehyde. Using
Palmer, Robert B.,Upthagrove, Alana L.,Nelson, Wendel L.
PRACTICAL SYNTHESIS AND CHARACTERIZATION OF 7-BENZYLIDENENALTREXONE (BNTX)
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Lewin, Anita H.,Nilsson, Melanie R.,Burgess, Jason P.,Carroll, F. Ivy
p. 621 - 624
(2007/10/03)
Synthesis of Naltrexone-Derived δ-Opioid Antagonists. Role of Conformation of the δ Address Moiety
Naltrindole (1) (NTI) is a highly potent and selective δ-opioid receptor antagonist.In an effort to understand the origin of the high potency, affinity, and selectivity of NTI, we have examined the conformational role of its indolic benzene moiety through
Portoghese, P. S.,Sultana, M.,Moe, S. T.,Takemori, A. E.
p. 579 - 585
(2007/10/02)
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