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Following a similar strategy, we designed a new series focused around an acidic hydroxybenzoisoxazole moiety, which was rationalised to mimic the benzoic acid role in the flufenamic scaffold.
This analysis led to the design of the initial lead compound, based on an azaindole ring moiety, which was then also evaluated computationally.
The second type of compound contained a 2-deoxy-2,3-dehydro-acetylneuraminic moiety which was linked to cytidine through its carboxylic acid and amide linkers.
The asymmetric allylation reactions of aldehydes catalyzed by a 10 mol % bisoxazoline complex bearing a phosphine oxide moiety, which was newly designed and synthesized from l-serine, afforded the corresponding homoallylic alcohols in 48 74% yields with 39 86% ee.
Chemical modification, that is, biotinylation, was conducted using Click chemistry at the 6-position (NMe-d-ProGly moiety), which was a plausible location selected on the basis of our SAR studies.
Most of the variability was in the 3-aroyl moiety, which was modified to incorporate methoxy (33 36), nitro (25 27), halogen (28 29), trifluoromethyl (30), or trifluoromethoxy (31 32) functionalities.
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As an antimalarial agent, artemisinin is well-known for its endoperoxide moiety, which is activated by the cellular iron.
The main reactivity takes place on N4 atoms linked to aromatic ring, and in the SO2NH moiety, which are influenced by substituents.
Probe compound 1 bears a photolabeling group on the 2′-position of the glycon moiety, which is near the potential binding site of the molecule with its receptor.
Antagonists of the human histamine H3 receptor (hH3R) often contain a second basic moiety, which is well known to boost affinity on this histamine receptor subtype.
Among others, molecules with a nitrile moiety, which is a group that is susceptible to a nucleophilic attack by the enzyme, have been identified as good inhibitors.
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