… -Substituted N-Cyclopropylmethyl-7α-phenyl-6,14-endoethano-tetrahydronorthebaine Derivative as a Selective and Potent Kappa Opioid Receptor Agonist with …

Z Li, R Ye, Q He, J Lu, Y Sun, X Sun… - Journal of Medicinal …, 2024 - ACS Publications
Research into kappa opioid receptor (KOR) agonists with attenuated central-nervous-system
side effects is a critical focus for developing productive and safe analgesics. Herein, a …

Morphinan derivatives with an oxabicyclo [3.2. 1] octane structure as dual agonists toward δ and κ opioid receptors

Y Uenohara, S Tsumura, S Hirayama, E Higashi… - Bioorganic & Medicinal …, 2022 - Elsevier
… Herein, we report an attempt to design and synthesize novel KOR agonists with an oxabicyclo[…
Synthesis of new opioid derivatives with a propellane skeleton and their pharmacologies: …

Synthesis of 2, 4, 6, 8, 10-pentaaza [3.3. 3] propellane substituted with different groups

L Zhang, Q Zhang, Y Xue, G Zhou… - E3S Web of …, 2020 - e3s-conferences.org
… Because aza[3.3.3]propellanes have good symmetry and compact skeleton, they … derivatives
substituted with different groups at nitrogen atoms. Therefore, we describe the preparation

[PDF][PDF] Unique reactions of naltrexone derivatives and their application to the synthesis of galanthamine

岡田卓大, オカダタカヒロ - 2019 - tsukuba.repo.nii.ac.jp
skeleton, which possesses a useful Tyr-Gly partial structure at message sites for opioid
receptors, and designed and synthesized … a [4.4.3]propellane skeleton intermediate containing a …

SLL-627 is a highly selective and potent κ opioid receptor (KOR) agonist with an unexpected nonreduction in locomotor activity

L Kong, X Shu, S Tang, R Ye, H Sun… - Journal of Medicinal …, 2022 - ACS Publications
… nepenthone derivative SLL-020ACP (Figure 3), an intermediate to some semisynthetic opioids,
… investigated, we designed, synthesized, and assayed a series of C7α-methyl derivatives. …

New small-molecule analgesics

SS Laev, NF Salakhutdinov - Current Medicinal Chemistry, 2021 - ingentaconnect.com
skeleton, the N-substituent also plays an important role in opioid activities and, thus, new
14-… Pentacyclic propellane derivatives were designed and synthesized to afford agents with …

Isolation, biosynthesis, and chemical syntheses of the hasubanan and acutumine alkaloids: A historical perspective

DC Grünenfelder, SE Reisman, R Navarro - Tetrahedron, 2023 - Elsevier
derivatives. In the context of propellane alkaloids, the authors targeted the synthesis of … to
afford hemiaminal 104, an intermediate bearing the skeletal framework of the closely related …

Discovery of a Highly Selective and Potent κ Opioid Receptor Agonist from N-Cyclopropylmethyl-7α-phenyl-6,14-endoethanotetrahydronorthebaines with Reduced …

L Xiao, Y Wang, M Zhang, W Wu, L Kong… - Journal of Medicinal …, 2019 - ACS Publications
… and pharmacology of Diels–Alder adducts of thebaine derivatives on opioid receptors. In …
receptor among all the series of compounds synthesized in this study. In contrast, when SLL-…

Friedlӓnder's synthesis of quinolines as a pivotal step in the development of bioactive heterocyclic derivatives in the current era of medicinal chemistry

S Rajendran, K Sivalingam… - Chemical Biology & …, 2022 - Wiley Online Library
their derivatives in pharmacology constantly drives the search for new procedures for their
construction and for the preparation … quinoline alkaloids, and its skeleton used as the design …

Enantioselective Total Synthesis of (+)-Stephadiamine

B Yang, G Li, Q Wang, J Zhu - Journal of the American Chemical …, 2023 - ACS Publications
… of 1 as well as its 4-bromobenzoylated derivative. Different from the … of the aza[4.3.3]propellane
skeleton. (16) Based on … Synthesis of pentacyclic propellane 4 is detailed in Scheme 2…