Synthesis and biological evaluation of fentanyl acrylic derivatives

Shaohua Li; Devora Cohen-Karni; Marina Kovaliov; Nestor Tomycz; Boyle Cheng; Donald Whiting; Saadyah Averick

doi:10.1039/C7RA01346A

Synthesis and biological evaluation of fentanyl acrylic derivatives

Shaohua Li, Devora Cohen-Karni, Marina Kovaliov, Nestor Tomycz, Boyle Cheng, Donald Whiting, Saadyah Averick

Allegheny General Hospital

Research output: Contribution to journal › Article › peer-review

10 Scopus citations

Abstract

The synthesis of novel fentanyl acrylate derivatives via bromo-fentanyl using Heck coupling is described. The synthesis is concise and represents an efficient and useful method for functionalizing fentanyl for medicinal chemistry investigations. The agonistic and analgesic activities are evaluated by Mu opioid receptor activation and hot plate assays in mice.

Original language	English
Pages (from-to)	20015-20019
Number of pages	5
Journal	RSC Advances
Volume	7
Issue number	32
DOIs	https://doi.org/10.1039/C7RA01346A
State	Published - 2017
Externally published	Yes

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© The Royal Society of Chemistry.

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10.1039/C7RA01346A

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title = "Synthesis and biological evaluation of fentanyl acrylic derivatives",

abstract = "The synthesis of novel fentanyl acrylate derivatives via bromo-fentanyl using Heck coupling is described. The synthesis is concise and represents an efficient and useful method for functionalizing fentanyl for medicinal chemistry investigations. The agonistic and analgesic activities are evaluated by Mu opioid receptor activation and hot plate assays in mice.",

author = "Shaohua Li and Devora Cohen-Karni and Marina Kovaliov and Nestor Tomycz and Boyle Cheng and Donald Whiting and Saadyah Averick",

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AU - Cohen-Karni, Devora

AU - Kovaliov, Marina

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AU - Cheng, Boyle

AU - Whiting, Donald

AU - Averick, Saadyah

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AB - The synthesis of novel fentanyl acrylate derivatives via bromo-fentanyl using Heck coupling is described. The synthesis is concise and represents an efficient and useful method for functionalizing fentanyl for medicinal chemistry investigations. The agonistic and analgesic activities are evaluated by Mu opioid receptor activation and hot plate assays in mice.

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Synthesis and biological evaluation of fentanyl acrylic derivatives

Abstract

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