What does this research mean for the field?

A novel series of 2,3-dioxindoles (isatins) function as selective, reversible, nonpeptidic inhibitors of human rhinovirus 3C protease, with their predicted binding mode confirmed by X-ray crystallography. Novelty: ClaimNovelty.NOVEL_FINDING. Consensus alignment: ConsensusAlignment.NEUTRAL.

January 1, 1996Journal of Medicinal ChemistryOpen Access

Design, Synthesis, and Evaluation of Nonpeptidic Inhibitors of Human Rhinovirus 3C Protease

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Population

Purified human rhinovirus-serotype 14 3C protease, HRV-14-infected HI-HeLa cells, and human…

Design

Preclinical

Authors

SWStephen E. WebberShinshu University JTJayashree TikheBristol-Myers Squibb (United States)SWStephen T. WorlandTherapeutics Clinical Research

Discussion

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Implication

These selective isatin derivatives merit preclinical optimization; extends HRV 3CP structural insights while leaving therapeutic potential open.

Structured PICO

Population

Purified human rhinovirus-serotype 14 (HRV-14) 3C protease (3CP), HRV-14-infected HI-HeLa cells, and human rhinovirus-serotype 2 (HRV-2) 3CP

Intervention

2,3-dioxindoles (isatins) derivatives (including compounds 8, 14, and 19)

Outcome

Inhibition of purified HRV-14 3CP and antiviral activity against HRV-14-infected HI-HeLa cellssurrogate

Novel isatin derivatives were designed and synthesized as reversible, nonpeptidic inhibitors of human rhinovirus 3C protease, demonstrating selective inhibition and structural validation.

Cite This Study

Webber et al. (1996) studied this question.

synapsesocial.com/papers/6a1c65cfecffbcc5fca14816 https://doi.org/10.1021/jm960603e

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Implication

These selective isatin derivatives merit preclinical optimization; extends HRV 3CP structural insights while leaving therapeutic potential open.

Design, Synthesis, and Evaluation of Nonpeptidic Inhibitors of Human Rhinovirus 3C Protease

Discussion

Member takes

Implication

Structured PICO

Cite This Study

Design, Synthesis, and Evaluation of Nonpeptidic Inhibitors of Human Rhinovirus 3C Protease

Discussion

Member takes

Implication

Structured PICO

Cite This Study

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