Molecular modelling of fentanyl analogs
نویسندگان
چکیده
منابع مشابه
Conformationally Restricted Fentanyl Analogs
Synthesis, analgesic activity and preliminary molecular modeling studies of the cisand trans-fused octahydro-l,2,3,4,4a,5,11,1 la-pyrido[3,4-c][1,5]benzoxazepines 8 and 9, the first rigid fentanyl analogs with a conformationally restricted 4-anilido group that retain antinociceptive properties, are reported. Fentanyl (1) is the prototype of the highly potent 4-anilidopiperidine class of synthet...
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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 powerful analgesics after optimization studies were carried out for each synthetic step. The general three-step strategy produced a panel of four fentanyls in excellent yields (73-78%) along with their more commonly encoun...
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Preliminary estimates of U.S. drug overdose deaths exceeded 60,000 in 2016 and were partially driven by a fivefold increase in overdose deaths involving synthetic opioids (excluding methadone), from 3,105 in 2013 to approximately 20,000 in 2016 (1,2). Illicitly manufactured fentanyl, a synthetic opioid 50-100 times more potent than morphine, is primarily responsible for this rapid increase (3,4...
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Fentanyl, and its structural analogs lofentanil and sufentanil, are potent analgesics used clinically in the management of pain. However, the high analgesic potency of these compounds is limited by the development of tolerance after chronic use. To investigate whether their tolerance development may be related to mu receptor desensitization, the cloned mouse mu receptor as well as mutant forms ...
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A similarity between chemical reactions and self-assembly of nanoparticles offers a strategy that can enrich both the synthetic chemistry and the nanoscience fields. Synthetic methods should enable quantitative control of the structural characteristics of nanoparticle ensembles such as their aggregation number or directionality, whereas the capability to visualize and analyze emerging nanostruc...
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ژورنال
عنوان ژورنال: Journal of the Serbian Chemical Society
سال: 2004
ISSN: 0352-5139,1820-7421
DOI: 10.2298/jsc0411843d