Phenol isosteres
Web1. aug 2007 · The more potent phenol and indazole di-anilino pyrimidines did not show submicromolar inhibition of Ser/Thr kinases tested, including GSK-3β, IKK-β and JNK3. … Web19. feb 2024 · The principles of phenolic isostere replacement demonstrated here may benefit future investigations. This study also provided evidence that imidazolone …
Phenol isosteres
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Web8. apr 2004 · A series of aminothiazole-derived morphinans, benzomorphans, and morphine were synthesized. Although their affinities were somewhat lower than their phenol prototypes, one compound (9a, ATPM) has been identified possessing high affinity and selectivity at the kappa receptor. Functional assays showed … WebN-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics Paul Bamborough 2007, Bioorganic & Medicinal Chemistry Letters 2,4-Dianilino pyrimidines are …
WebB. Divalent Isosteres 3155 1. Divalent Replacements Involving Double Bonds 3155 2. Divalent Replacements Involving Two Single Bonds 3155 C. Trivalent Atoms or Groups … WebPhenyl bioisosteres in medicinal chemistry: discovery of novel γ-secretase modulators as a potential treatment for Alzheimer's disease † H. Ratni, *a K. Baumann,a P. Bellotti, a X. A. …
Web13. okt 2013 · Sulphonamide Bioisosteres A gem-dimethylsulphone has been used as a bioisosteric replacement for a metabolically labile sulphonamide, retaining Cav2.2 potency but reducing the metabolic liability 10.1021/ml4002612">DOI Last updated 13 October 2013 Web1. jan 2014 · The phenol 256 is a short-acting calcium-sensing receptor antagonist that was examined for its potential as a treatment for osteoporosis [363, 364]. However, CYP …
Web3. feb 2012 · The proof of the pudding: A proof-of-concept study using γ-secretase inhibitors as a model has shown that sulfonimidamides act as bioisosteres for sulfonamides. …
Web5 Bioisosteres of the Phenol Function The optimal bioisosteres of the phenolic function should have approximately the same size as the hydroxyl itself and should have … technology holdings limitedWebSeveral heterocyclic systems containing an N−H hydrogen bond donor were synthesized and evaluated as phenol isosteres. The preference orientation of the hydrogen bond was established by comparison of analogues containing different NH vectors. technology high school nycWeb10. feb 2005 · Several heterocyclic systems containing an N-H hydrogen bond donor were synthesized and evaluated as phenol isosteres. The preference orientation of the … technology history for kidsWeb30. sep 2024 · Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design. Murugaiah A. M. Subbaiah*. and. Nicholas A. Meanwell*. Cite this: J. Med. Chem. 2024, 64, 19, 14046–14128. Publication Date: September 30, 2024. … American Chemical Society pubs.acs.org technology holdings llcWeb27. jan 2024 · Phenolic amino-oxetanes were identified as strategic intermediates that, after triflation, could be used as coupling partners in cross-coupling reactions, hence expanding … spds scotland hrWeb28. jan 2024 · Phenols are prone to glucuronidation. The CF 2 H group has been proposed as a bioisosteric replacement for the phenol group, it can act as a similar hydrogen bond donor, as confirmed by crystallographic, … spdsw clpWeb1. sep 2007 · As phenols are known to be detrimental for the pharmacokinetic properties of drugs, 11, 12 we decided to remove the hydroxyl group at position R 4 . In addition, replacement of the anisidine side ... technology hiring news