Huang, Boshi published the artcileVerifying the role of 3-hydroxy of 17-cyclopropylmethyl-4,5α-epoxy-3,14β-dihydroxy-6β-[(4′-pyridyl)carboxamido]morphinan derivatives via their binding affinity and selectivity profiles on opioid receptors, Application of 2-Chloroisonicotinic acid, the publication is Bioorganic Chemistry (2021), 104702, database is CAplus and MEDLINE.
In the present study, the role of 3-hydroxy group of a series of epoxymorphinan derivatives I (R1 = H, OH; R2 = Cl, Br, CN, Me, OMe) in their binding affinity and selectivity profiles toward the opioid receptors (ORs) has been investigated. It was found that the 3-hydroxy group was crucial for the binding affinity of these derivatives for all three ORs due to the fact that all the analogs I (R1 = OH) exhibited significantly higher binding affinities compared to their counterpart 3-dehydroxy ones I (R1 = H). Meanwhile most compounds carrying the 3-hydroxy group possessed similar selectivity profiles for the kappa opioid receptor over the mu opioid receptor as their corresponding 3-dehydroxy derivatives The [35S]-GTPγS functional assay results indicated that the 3-hydroxy group of these epoxymorphinan derivatives I was important for maintaining their potency on the ORs with various effects. Further mol. modeling studies helped comprehend the remarkably different binding affinity and functional profiles between compound I (R1 = H, R2 = CN)(NCP) and its 3-dehydroxy analog I (R1 = OH, R2 = CN).
Bioorganic Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Application of 2-Chloroisonicotinic acid.
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