𝔖 Bobbio Scriptorium
✦   LIBER   ✦

The design of potent and stable benzisothiazolone inhibitors of human leukocyte elastase

✍ Scribed by Dennis J. Hlasta; Malcolm R. Bell; John J. Court; Kenneth C. Cundy; Ranjit C. Desai; Edward W. Ferguson; Robert J. Gordon; Virendra Kumar; Alan L. Maycock; Chakrapani Subramanyam; Richard P. Dunlap; Shari L. Eiff; Catherine A. Franke; Albert J. Mura; Anne G. Rowlands

Publisher
Elsevier Science
Year
1995
Tongue
English
Weight
332 KB
Volume
5
Category
Article
ISSN
0960-894X

No coin nor oath required. For personal study only.

πŸ“œ SIMILAR VOLUMES

[14C]-labelling of benzisothiazolone bas
[14C]-labelling of benzisothiazolone based inhibitors of human leukocyte elastase
✍ Alain Burgos; Gordon R. Duffin; George J. Ellames; Karen J. Wedge πŸ“‚ Article πŸ“… 1996 πŸ› John Wiley and Sons 🌐 French βš– 418 KB

The [ 4C] labelled synthesis of two benzisothiazolone based inhibitors of Human Leukocyte Elastase is described. These are The synthesis of the intermediate [3-14C]-2-(chloromethyl)-6-methoxy-4-( l-methylethyl)-l,2benzisothiazol-3(2H)-one 1 ,I-dioxide, 8, common to both these syntheses. was achieve

A comparative SAR and computer modeling
A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastase
✍ Dennis J. Hlasta; John J. Court; Ranjit C. Desai; Timothy G. Talomie; Jian Shen; πŸ“‚ Article πŸ“… 1996 πŸ› Elsevier Science 🌐 English βš– 332 KB

Distinct differences in the SAR for HLE and PPE inhibition in this class of compounds were observed. For example, larger lipophilic substituents at the benzisothiazolone 4-position afforded inhibitors that were potent against HLE, but inactive against PPE. These findings are consistent with computer