1.
Bioorg Med Chem Lett
; 10(15): 1637-40, 2000 Aug 07.
Article
in English
| MEDLINE
| ID: mdl-10937713
ABSTRACT
Synthesis of an arylsulfone hydroxamate lead optimization library is presented. Biological activity of representative examples is given to demonstrate the value of this approach for lead optimization.
Subject(s)
Hydroxamic Acids/chemical synthesis , Sulfones/chemistry , 3',5'-Cyclic-AMP Phosphodiesterases/antagonists & inhibitors , Cyclic Nucleotide Phosphodiesterases, Type 4 , Enzyme Inhibitors/chemical synthesis , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/pharmacology , Hydroxamic Acids/chemistry , Hydroxamic Acids/pharmacology , Matrix Metalloproteinase Inhibitors , Structure-Activity Relationship
2.
J Comb Chem
; 2(6): 691-7, 2000.
Article
in English
| MEDLINE
| ID: mdl-11126297
ABSTRACT
A new tetrafluorophenol activated resin that facilitates the use of 19F NMR to quantitate loading is presented. This new resin provides a useful tool for acylation, and a novel activated polymeric sulfonate ester to generate sulfonamides. This activated resin reacts with a wide scope of N-nucleophiles including primary and secondary amines, and anilines. This new activated resin methodology provides a powerful tool for pure single-compound library synthesis.
