287202-41-9

Upstream product

• 946857-56-3 4-(4-hydroxybenzenesulfonylmethyl)piperidine-1,4-dicarboxylic acid 1-tert-butyl ester 4-ethyl ester 
• 946857-73-4 4-(4-hydroxy-phenylsulfanylmethyl)-piperidine-1,4-dicarboxylic acid 1-tert-butyl ester 4-ethyl ester 
• 287201-95-0 4-but-2-ynyloxy-benzenethiol 
• 286459-94-7 4-but-2-ynyloxybenzenesulfonyl chloride 
• 142851-03-4 1-tert-butyl 4-ethyl piperidine-1,4-dicarboxylate 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1126-09-6 4-carbethoxypiperidine 
• 287202-23-7 1-(tert-butyl) 4-ethyl 4-({[4-(2-butynyloxy)phenyl]sulfanyl}methyl)-1,4-piperidinedicarboxylate 
• 287202-25-9 4-[[[4-(2-Butynyloxy)phenyl]sulfonyl]methyl]-1,4-piperidinedicarboxylic acid 1-tert-butyl 4-ethyl ester 
• 213013-98-0 4-(iodomethyl)piperidine-1,4-dicarboxylic acid 1-tert-butyl ester 4-ethyl ester 
• 287202-73-7 4-(4-but-2-ynyloxy-benzenesulfonylmethyl)-piperidine-1,4-dicarboxylic acid mono-tert-butyl ester 
• 37477-16-0 O-(tert-butyl)hydroxylamine 

Relevant academic research and scientific papers

Identification of potent and selective TACE inhibitors via the S1 pocket

By focusing on the P1 portion of the piperidine β-sulfone ligands we identified a motif that induces selectivity and resulted in a series of TACE inhibitors that demonstrated excellent in vitro potency against isolated TACE enzyme and excellent selectivity over MMPs 1, 2, 9, 13, and 14.

Design and synthesis of butynyloxyphenyl β-sulfone piperidine hydroxamates as TACE inhibitors

A series of butynyloxyphenyl β-sulfone piperidine hydroxamate TACE inhibitors was designed and synthesized. The resulting structure-activity relationship and MMP selectivity of the series were examined. Of the compounds investigated, 17s has excellent in

ALKYNYL CONTAINING HYDROXAMIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MATRIX METALLOPROTEINASE (MMP) INHIBITORS / TNF-ALPHA CONVERTING ENZYME (TACE) INHIBITORS

Compounds of the formula:useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.