Liu, Xiao published the artcileExploration of the SAR Connection between Morphinan- and Arylacetamide-Based ¦Ê Opioid Receptor (¦ÊOR) Agonists Using the Strategy of Bridging, Recommanded Product: 4-Nitrophenylacetic acid, the publication is ACS Chemical Neuroscience (2021), 12(6), 1018-1030, database is CAplus and MEDLINE.
¦Ê Opioid receptor (¦ÊOR) is a subtype of opioid receptors, and there are two major ¦ÊOR agonists currently available, morphinans and arylacetamides, which are structurally distinct from each other. Numerous efforts had been made to correlate these series of compounds in order to establish a consensus binding pattern for ¦ÊOR agonists. Unfortunately, no morphinan-based agent with an arylacetamidyl substituent has been identified as a ¦ÊOR agonist with a pharmacol. profile similar to arylacetamides. Since the recently described morphinan-based compound SLL-039 was identified as a selective and potent ¦ÊOR agonist that contains a unique benzamidyl substituent in structure similar to arylacetamides, numerous arylacetamidyl substituents were introduced to this scaffold to examine whether the structure-activity relationships (SARs) of arylacetamides in conferring ¦ÊOR agonistic activities could be reproduced by these analogs. Thus, a series of N-cyclopropylmethyl-7¦Á-arylacetamidylphenyl-6,14-endoethanotetrahydronorthebaine analogs were designed, synthesized, and assayed for biol. activities. Among these compounds, compound 4j with a 3′,4′-dimethylphenylacetamidyl substituent showed a single digit low nanomolar affinity to the ¦ÊOR and relatively high subtype selectivity in binding assays, but this profile was not reproduced in functional assays. In contrast, compound 4i displayed moderately selective ¦ÊOR agonistic activities in functional assays, which was inconsistent with its nonselective nature in binding assays. Overall, introduction of an arylacetamidyl substituent to the morphinan-based scaffold was associated with pharmacol. diversity in both binding and functional activities on opioid receptors in vitro. The resultant SARs were inconsistent with that of classical arylacetamides as ¦ÊOR agonists, despite bearing a similar arylacetamidyl substituent in the structure. Therefore, the arylacetamidyl substituent of the morphinan-based scaffold was found to be disconnected from that of arylacetamides in conferring ¦ÊOR activities.
ACS Chemical Neuroscience published new progress about 104-03-0. 104-03-0 belongs to catalysis-chemistry, auxiliary class Nitro Compound,Carboxylic acid,Benzene, name is 4-Nitrophenylacetic acid, and the molecular formula is C8H7NO4, Recommanded Product: 4-Nitrophenylacetic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia