1,4‐Dihydropyridinebutyrolactone‐derived ring‐opened ester and amide analogs targeting BET bromodomains
Sign Up to like & getrecommendations! Published in 2022 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.202200288
Abstract: Based on a previously reported 1,4‐dihydropyridinebutyrolactone virtual screening hit, nine lactone ring‐opened ester and seven amide analogs were prepared. The analogs were designed to provide interactions with residues at the entrance of the ZA loop… read more here.
Keywords: bet; bet bromodomains; amide analogs; opened ester ... See more keywords
Metabolism of a new synthetic opioid tetrahydrofuranylfentanyl in fresh isolated human hepatocytes: detection and confirmation of ring-opened metabolites.
Sign Up to like & getrecommendations! Published in 2019 at "Drug testing and analysis"
DOI: 10.1002/dta.2743
Abstract: The metabolism of a new synthetic opioid tetrahydrofuranylfentanyl (THF-fentanyl) was investigated using fresh human hepatocytes. Fourteen metabolites of THF-fentanyl, such as tetrahydrofuran ring-opened metabolites, desphenethylated metabolites, hydroxylated metabolites, and hydroxylated and methoxylated metabolites and their… read more here.
Keywords: thf fentanyl; metabolism new; ring; ring opened ... See more keywords
Detection and confirmation of the ring-opened carboxylic acid metabolite of a new synthetic opioid furanylfentanyl
Sign Up to like & getrecommendations! Published in 2020 at "Forensic Toxicology"
DOI: 10.1007/s11419-020-00546-7
Abstract: Purpose Recently, the opioid epidemic has become a serious problem, particularly in North America and Europe. The aim of this study was to clarifyQuery the metabolic fate of a new synthetic opioid furanylfentanyl. Methods The… read more here.
Keywords: opened carboxylic; carboxylic acid; ring opened; acid metabolite ... See more keywords
Design and synthesis of the ring-opened derivative of 3-n-butylphthalide-ferulic acid-glucose trihybrids as potential anti-ischemic agents
Sign Up to like & getrecommendations! Published in 2020 at "Chinese Chemical Letters"
DOI: 10.1016/j.cclet.2020.02.031
Abstract: Abstract To improve aqueous solubility and anti-ischemic activity of 3-n-butylphthalide (NBP), we designed and synthesized the ring-opened derivative of NBP-ferulic acid-glucose trihybrids (S1-S8). These hybrids inhibited adenosine diphosphate (ADP)- or arachidonic acid (AA)-induced platelet aggregation,… read more here.
Keywords: anti ischemic; ring opened; acid glucose; ferulic acid ... See more keywords
Design, synthesis and biological evaluation of novel ring-opened cromakalim analogues with relaxant effects on vascular and respiratory smooth muscles and as stimulators of elastin synthesis.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.12.071
Abstract: Two new series of ring-opened analogues of cromakalim bearing sulfonylurea moieties (series A: with N-unmethylated sulfonylureas, series B: with N-methylated sulfonylureas) were synthesized and tested as relaxants of vascular and respiratory smooth muscles (rat aorta… read more here.
Keywords: respiratory smooth; smooth muscles; ring opened; series ... See more keywords
Electrochemical Benzylation of [60]Fullerene-Fused Lactones: Unexpected Formation of Ring-Opened Adducts and Their Photovoltaic Performance.
Sign Up to like & getrecommendations! Published in 2019 at "Organic letters"
DOI: 10.1021/acs.orglett.9b02635
Abstract: Electrochemical benzylation of [60]fullerene-fused lactones with different motifs unexpectedly affords three types of ring-opened benzylated adducts under different conditions. Both [60]fullerene-fused δ- and γ-lactones can be benzylated to generate ring-opened mono- and bis-benzylated adducts in… read more here.
Keywords: fullerene fused; benzylation fullerene; fused lactones; ring opened ... See more keywords
Diprotonative stabilization of ring-opened carbocationic intermediates: conversion of tetrahydroisoquinoline to triarylmethanes.
Sign Up to like & getrecommendations! Published in 2020 at "Chemical communications"
DOI: 10.1039/d0cc01969k
Abstract: Superacid-promoted conversion of tetrahydroisoquinolines to triarylmethanes via tandem reactions of C-N bond scission, Friedel-Crafts alkylation, C-O bond scission, and electrophilic aromatic amidation was developed. Dication formation was important for stabilizing the ring-opened carbocationic intermediate, which… read more here.
Keywords: stabilization ring; diprotonative stabilization; ring opened; carbocationic intermediates ... See more keywords
Synthesis of Ring-Opened Analogues of Oxysterol-Binding Protein-Inhibiting Piperidinyl-thiazole Fungicides
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DOI: 10.1055/s-0036-1588473
Abstract: Novel aminoethyl-, aminopropyl-, and aminobutyl-substituted thiazole-4-carboxamides have been prepared which are ring-opened analogues of piperidinyl-thiazole fungicides. Depending of the chain length, completely different synthetic approaches had to be chosen which vary from a Sonogashira coupling… read more here.
Keywords: thiazole fungicides; ring opened; synthesis ring; piperidinyl thiazole ... See more keywords
Synthesis, Biological Evaluation and Docking Studies of Ring-Opened Analogues of Ipomoeassin F
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DOI: 10.3390/molecules27144419
Abstract: The plant-derived macrocyclic resin glycoside ipomoeassin F (Ipom-F) binds to Sec61α and significantly disrupts multiple aspects of Sec61-mediated protein biogenesis at the endoplasmic reticulum, ultimately leading to cell death. However, extensive assessment of Ipom-F as… read more here.
Keywords: synthesis biological; docking studies; opened analogues; biological evaluation ... See more keywords