WebWhat are some utilities of bioisosteres? improving potency, enhancing selectivity, altering physical properties, reducing/redirecting metabolism, eliminating/modifying toxicophores, acquiring novel intellectual property ________ represent the result of an early appreciation of the concept and encompass structurally simple atoms or groups. WebThis result is consistent with the increased affinity of other thiophene-based amidines, in comparison to furan counterparts, and this may be attributed to the differences in van der Waals radii between S and O atoms. 10,33 The weak DNA cleavage ability of the aza derivatives 1g and 1c, compared against the phenyl counterparts 1e and 1a , is ...
[2]-Ladderanes as isosteres for meta-substituted aromatic rings …
WebApr 12, 2024 · The authors also mention the use of tertiary alkyl chlorides as tert-butyl isosteres in passing. I believe they could have spent a bit more time on this also. ... Not your run-of-the-mill phenyl ... WebMay 5, 2024 · A gram-scale synthesis, physico-chemical characterization, and lead-likeness assessment of 4-di/trifluoromethyl-2-heterabicyclo [2.1.1]hexanes as fluorinated bicyclic proline analogues and phenyl isosteres are disclosed. meta writer
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WebAnother example is aromatic rings, where a phenyl -C 6 H 5 ring can often be replaced by a different aromatic ring such as thiophene or naphthalene which may improve efficacy, change specificity of binding or reduce metabolically labile sites on the molecule, resulting in better pharmacokinetic properties. WebNov 5, 2024 · A series of adenosine and 2′-deoxyadenosine pairs modified with a 1,12-dicarba-closo-dodecaborane cluster or alternatively with a phenyl group at the same position was synthesized, and their affinity was determined at A 1, A 2A, A 2B and A 3 adenosine receptors (ARs).While AR affinity differences were noted, a general tendency to … WebNov 5, 2024 · Synthesis and evaluation of adenosine derivatives as A 1, A 2A, A 2B and A 3 adenosine receptor ligands containing boron clusters as phenyl isosteres and selective A 3 agonists Eur J Med Chem. 2024 Nov 5;223:113607. doi: 10.1016/j.ejmech.2024.113607. Epub 2024 Jun 11. Authors metaworth