Inside Cover: Esterase-Sensitive Prodrugs with Tunable Release Rates and Direct Generation of Hydrogen Sulfide (Angew. Chem. Int. Ed. 14/2016)

A series of thioacids is described as hydrogen sulfide prodrugs by B. Wang et al. in their Communication on page 4514 ff. The release takes advantage of a “trimethyl lock”‐facilitated lactonization controlled by an esterase trigger that unmasks a hydroxy group as the attacking nucleophile. These hyd...

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Bibliographic Details
Published in:Angewandte Chemie International Edition 2016-03, Vol.55 (14), p.4370-4370
Main Authors: Zheng, Yueqin, Yu, Bingchen, Ji, Kaili, Pan, Zhixiang, Chittavong, Vayou, Wang, Binghe
Format: Article
Language:English
Subjects:
anti-inflammatory drugs
enzyme trigger
H2S-NSAIDs
Hydrogen sulfide
hydrogen sulfide prodrugs
lactonization
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Summary:A series of thioacids is described as hydrogen sulfide prodrugs by B. Wang et al. in their Communication on page 4514 ff. The release takes advantage of a “trimethyl lock”‐facilitated lactonization controlled by an esterase trigger that unmasks a hydroxy group as the attacking nucleophile. These hydrogen sulfide prodrugs are stable under physiological conditions and release H2S with tunable release rates by modifying the ester group.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.201602011