[HTML][HTML] Biased opioid ligands

A Faouzi, BR Varga, S Majumdar - Molecules, 2020 - mdpi.com
Achieving effective pain management is one of the major challenges associated with
modern day medicine. Opioids, such as morphine, have been the reference treatment for …

Multicomponent reactions as a potent tool for the synthesis of benzodiazepines

H Farhid, V Khodkari, MT Nazeri… - Organic & …, 2021 - pubs.rsc.org
Benzodiazepines (BZDs), a diverse class of benzofused seven-membered N-heterocycles,
display essential pharmacological properties and play vital roles in some biochemical …

Mitragynine/corynantheidine pseudoindoxyls as opioid analgesics with mu agonism and delta antagonism, which do not recruit β-arrestin-2

A Váradi, GF Marrone, TC Palmer… - Journal of medicinal …, 2016 - ACS Publications
Natural products found in Mitragyna speciosa, commonly known as kratom, represent
diverse scaffolds (indole, indolenine, and spiro pseudoindoxyl) with opioid activity, providing …

[HTML][HTML] Isocyanide-based multicomponent reactions for the synthesis of heterocycles

A Váradi, TC Palmer, R Notis Dardashti, S Majumdar - Molecules, 2015 - mdpi.com
Multicomponent reactions (MCRs) are extremely popular owing to their facile execution,
high atom-efficiency and the high diversity of products. MCRs can be used to access various …

Oxidative metabolism as a modulator of kratom's biological actions

S Chakraborty, R Uprety, ST Slocum, T Irie… - Journal of medicinal …, 2021 - ACS Publications
The leaves of Mitragyna speciosa (kratom), a plant native to Southeast Asia, are increasingly
used as a pain reliever and for attenuation of opioid withdrawal symptoms. Using the tools of …

Strategies towards safer opioid analgesics—A review of old and upcoming targets

BR Varga, JM Streicher… - British journal of …, 2023 - Wiley Online Library
Opioids continue to be of use for the treatment of pain. Most clinically used analgesics target
the μ opioid receptor whose activation results in adverse effects like respiratory depression …

Controlling opioid receptor functional selectivity by targeting distinct subpockets of the orthosteric site

R Uprety, T Che, SA Zaidi, SG Grinnell, BR Varga… - Elife, 2021 - elifesciences.org
Controlling receptor functional selectivity profiles for opioid receptors is a promising
approach for discovering safer analgesics; however, the structural determinants conferring …

[HTML][HTML] Multicomponent reactions for the synthesis of active pharmaceutical ingredients

Á Cores, J Clerigué, E Orocio-Rodríguez… - Pharmaceuticals, 2022 - mdpi.com
Multicomponent reactions 9i. e., those that engage three or more starting materials to form a
product that contains significant fragments of all of them), have been widely employed in the …

[HTML][HTML] Fentanyls continue to replace heroin in the drug arena: the cases of ocfentanil and carfentanil

N Misailidi, I Papoutsis, P Nikolaou, A Dona… - Forensic toxicology, 2018 - Springer
Purpose Ocfentanil and carfentanil are two potent synthetic opioids that are analogues of
fentanyl and are actively involved in the recent fentanyl crisis. The aim of this review is to …

Synthesis of polysubstituted pyrroles via isocyanide-based multicomponent reactions as an efficient synthesis tool

MT Nazeri, A Shaabani - New Journal of Chemistry, 2021 - pubs.rsc.org
Pyrroles are among the most privileged and influential small N-heterocycles at the core of
many commercial drugs, biological composition, natural compounds, agrochemicals, and …