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Inside Cover: Esterase‐Sensitive Prodrugs with Tunable Release Rates and Direct Generation of Hydrogen Sulfide (Angew. Chem. Int. Ed. 14/2016)
Author(s) -
Zheng Yueqin,
Yu Bingchen,
Ji Kaili,
Pan Zhixiang,
Chittavong Vayou,
Wang Binghe
Publication year - 2016
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201602011
Subject(s) - prodrug , nucleophile , hydrogen sulfide , chemistry , sulfide , esterase , cover (algebra) , int , hydrogen , combinatorial chemistry , medicinal chemistry , stereochemistry , organic chemistry , catalysis , enzyme , biochemistry , sulfur , computer science , mechanical engineering , operating system , engineering
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 H 2 S with tunable release rates by modifying the ester group.