Fentanyl and its analogs have been mainstays for the treatment of severe to moderate pain
for many years. In this review, we outline the structural and corresponding synthetic …

The ligand binding modes of a series of fentanyl derivatives are examined using a
combination of conformational analysis and molecular docking to the μ-opioid receptor …

Fentanyl rose to prominence as an alternative analgesic to morphine nearly 50 years ago;
today, fentanyl has re-emerged as a dangerous recreational substance. The increased …

Two series of fentanyl-derived hybrid molecules bearing potent I2–imidazoline binding site
(IBS) ligands (ie, guanidine and BU224 moieties) linked with an aliphatic (m= 2, 3, 4, 6, 7, 8 …

Fentanyl is the prototype of the 4-anilidopiperidine class of synthetic opioid analgesics. This
study was aimed to review the structure-activity-relationship (SAR) of fentanyl analogs …

Substituted fentanyls are abused and cause rapid fatal overdose. As their pharmacology is
not well characterized, we examined in vitro pharmacology and structure–activity …

A series of pyrido-and pyrimidomorphinans (6a− h and 7a− g) were synthesized from
naltrexone and evaluated for binding and biological activity at the opioid receptors. The …

The alternate and optimized syntheses of the parent opioid fentanyl and its analogs are
described. The routes presented exhibit high-yielding transformations leading to these …

STRONGHOLDS FOR DRUG DISCOVERY Historically, natural products (NPs) have played
a key role in the development of chemotherapy, 1, 2 and to this very day numerous marketed …

Because of the problems associated with opioids, drug discovery efforts have been
employed to develop opioids with reduced side effects using approaches such as biased …