172738-60-2

Upstream product

• 78-81-9 isobutylamine 
• 98-68-0 4-methoxy-phenyl-sulphonyl chloride 
• 696-63-9 4-Methoxybenzenethiol 

Downstream Products

• 177702-12-4 ethyl 2-[[4-methoxybenzenesulfonyl](isobutyl)-amino]acetate 
• 1613304-80-5 N-(4-chlorobenzyl)-N-isobutyl-4-methoxybenzenesulfonamide 
• 1613304-81-6 N-(4-chlorobenzyl)-4-hydroxy-N-isobutylbenzenesulfonamide 
• 1027870-37-6 [(4-Cyclohexylmethoxy-benzenesulfonyl)-isobutyl-amino]-acetic acid ethyl ester 
• 161315-33-9 ethyl 2-[[4-hexyloxybenzenesulfonyl](isobutyl)amino]acetate 
• 1027905-16-3 {[4-(2-Ethoxy-ethoxy)-benzenesulfonyl]-isobutyl-amino}-acetic acid ethyl ester 
• 1026649-42-2 {Isobutyl-[4-(3-methyl-butoxy)-benzenesulfonyl]-amino}-acetic acid ethyl ester 
• 1027323-89-2 [Isobutyl-(4-isopropoxy-benzenesulfonyl)-amino]-acetic acid ethyl ester 
• 161314-17-6 N-hydroxy-2-[isobutyl-(4-methoxybenzenesulfonyl)amino]acetamide 
• 161315-34-0 ethyl 2-[[4-hydroxybenzenesulfonyl](isobutyl)amino]acetate 

Relevant academic research and scientific papers

BENZENE SULFONAMIDE DERIVATIVES AND THEIR USE AS RORC MODULATORS

Compounds of the formula la or lb: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, D, E, G, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

BENZYL SULFONAMIDE DERIVATIVES AS RORC MODULATORS

Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.

Hydroxamates: Relationships between structure and plasma stability

Hydroxamates are valuable tools for chemical biology as well as interesting leads for medicinal chemistry. Although many hydroxamates display nanomolar activities against metalloproteases, only three hydroxamates have reached the market, among which is the HDAC inhibitor vorinostat. Failures in development are generally attributed to lack of selectivity, toxicity, or poor stability. To help medicinal chemists with respect to plasma stability, we have performed the first and preliminary study on structure-plasma stability for hydroxamates. We define some structural rules to predict or improve the plasma stability in the preclinical stage.

Convenient one-pot synthesis of sulfonamides from thiols using trichloroisocyanuric acid

A convenient synthesis of sulfonamides from thiols is described. In situ preparation of sulfonyl chlorides from thiols is accomplished by oxidation with trichloroisocyanuric acid (TCCA), benzyltrimethylammonium chloride and water (2.5 equiv). The sulfonyl chlorides are then further allowed to react with excess amine in the same reaction vessel. Triethylamine can be optionally added as acid scavenger. Copyright Taylor & Francis Group, LLC.

SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE

This invention provides a novel class of sulfonamide compounds of formula I which are aspartyl protease inhibitors: STR1 This invention also provides pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also provides methods for inhibition aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.

Discovery of CGS 27023A, a non, peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits

Structure-activity relationships of a lead hydroxamic acid inhibitor of recombinant human stromelysin were systematically defined by taking advantage of a concise synthesis that allowed diverse functionality to be explored at each position in a template. An ex vivo rat model and an in vivo rabbit model of stromelysin-induced cartilage degradation were used to further optimize these analogs for oral activity and duration of action. The culmination of these modifications resulted in CGS 27023A, a potent, orally active stromelysin inhibitor that blocks the erosion of cartilage matrix.