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In the structure of five-members heteroaromatic the introduction of heteroatoms with larger electronegativity or benzene ring leads to a deceasing hydrophobility or big steric hindrance, weakening or blocking the hydrophobic interaction between TTDs and the binding pocket of reversetranscriptase, and thereby reduces and loses corresponding activity of TTDs. Hence, the structural modification of five-members heteroaromatic moiety of TTDs plays a key role in the generation of TTDs-type NNRTIs with high activity.
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In the structure of five-members heteroaromatic the introduction of heteroatoms with larger electronegativity or benzene ring leads to a deceasing hydrophobility or big steric hindrance, weakening or blocking the hydrophobic interaction between TTDs and the binding pocket of reversetranscriptase, and thereby reduces and loses corresponding activity.
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