102568-35-4

Upstream product

• 84-89-9 1-aminonaphthalene-5-sulfonic acid 
• 108-24-7 acetic anhydride 

Downstream Products

• 52218-37-8 N-[5-(Chlorosulfonyl)-1-naphthalenyl]acetamide 
• 1025829-32-6 5-(Acetyl-methyl-amino)-naphthalene-1-sulfonic acid 
• 648899-33-6 N-[5-(3-nitro-phenylsulfamoyl)-naphthalen-1-yl]-acetamide 
• 648899-35-8 N-[5-(2,3-dimethyl-phenylsulfamoyl)-naphthalen-1-yl]-acetamide 
• 491580-08-6 N-[5-[[(2-phenylethyl)amino)sulfonyl]-1-naphthalenyl]acetamide 
• 648899-29-0 N-[5-(4-fluoro-phenylsulfamoyl)-naphthalen-1-yl]-acetamide 
• 648899-30-3 N-[5-(4-chloro-phenylsulfamoyl)-naphthalen-1-yl]-acetamide 
• 648899-31-4 N-[5-(4-bromo-phenylsulfamoyl)-naphthalen-1-yl]-acetamide 
• 648899-32-5 N-(5-p-tolylsulfamoyl-naphthalen-1-yl)-acetamide 
• 648899-34-7 N-(5-o-tolylsulfamoyl-naphthalen-1-yl)-acetamide 

Relevant academic research and scientific papers

Discovery and structure-activity relationships of sulfonamide ET(A)- selective antagonists

Random screening of compounds in an ETA receptor binding assay led to the discovery of a class of benzenesulfonamide ligands. Optimization led to the development of 5-amino-N-(3,4-dimethyl-5-isoxazolyl)-1- naphthalenesulfonamides which were functional ant

Design of Nitroso-Modified Naphthylene-Based Fluorophores as Photoactivatable Bioorthogonal Turn-On Probes

We reported a series of nitroso-modified naphthylene-based fluorophores as novel bioorthogonal fluorescence turn-on probes. The cycloadducts from nitroso-diene Diels-Alder reaction could be either photochemically or spontaneously transformed into highly f

Identification and validation of selective deubiquitinase inhibitors

Deubiquitinating enzymes (DUBs) are a class of isopeptidases that regulate ubiquitin dynamics through catalytic cleavage of ubiquitin from protein substrates and ubiquitin precursors. Despite growing interest in DUB biological function and potential as therapeutic targets, few selective small-molecule inhibitors and no approved drugs currently exist. To identify chemical scaffolds targeting specific DUBs and establish a broader framework for future inhibitor development across the gene family, we performed high-throughput screening of a chemically diverse small-molecule library against eight different DUBs, spanning three well-characterized DUB families. Promising hit compounds were validated in a series of counter-screens and orthogonal assays, as well as further assessed for selectivity across expanded panels of DUBs. Through these efforts, we have identified multiple highly selective DUB inhibitors and developed a roadmap for rapidly identifying and validating selective inhibitors of related enzymes.

USP30 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of USP30, and the treatment of USP30-mediated disorders.

USP30 INHIBITORS

The application relates to phenyl- or naphthylsulfonamide derivatives of the structural formula (I). The compounds are described as inhibitors of USP30 (ubiquitin specific peptidase 30) useful for the treatment of conditions involving mitochondrial defects including neurodegenerative diseases such as Alzheimer's and Parkinson's or a neoplastic disease such as leukemia.

Caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors

HIV-1 integrase (IN) is an essential enzyme for retroviral replication and a rational target for the design of anti-AIDS drugs. In the present study, we have designed, synthesized and tested a series of caffeoyl naphthalenesulfonamide derivatives as HIV integrase inhibitors. Among these compounds, we found that HIV integrase inhibitory activities of compounds III-3 and III-4 were more potent than L-chicoric acid (IC50=11.8 μg/mL) and others were comparable to L-chicoric acid. Furthermore, the structure-activity relationships of these compounds were studied. The information gathered from this paper will be useful in the development and design of HIV-1 integrase inhibitors in the future.

SULFONAMIDE ENDOTHELIN ANTAGONISTS

Compounds of the formula STR1 inhibit endothelin, wherein: one of X and Y is N and the other is O; R is naphthyl or naphthyl substituted with R. sup.1, R 2 and R 3 ;R 1, R 2 and R 3 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl, any of which may be substituted with Z 1, Z 2 and Z 3 ; halo; hydroxyl; cyano; nitro;--C(O)H;--C(O)R 6 ; CO 2 H;--CO 2 R 6 ;--SH;--S(O) n R 6 ;--S(O) m--OH;--S(O). sub.m--OR 6 ;--O--S(O) m--R 6 ;--O--S(O) m OH;--O--S(O) m--OR. sup.6 ;--Z 4--NR 7 R 8 ; or--Z 4--N(R. sup.11)--Z 5--NR 9 R 10 ;R 4 and R 5 are each independently hydrogen; alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, or aralkyl, any of which may be substituted with Z 1, Z 2 and Z 3 ; halo; hydroxyl; cyano; nitro;--C(O)H;--C(O)R 6 ;--CO 2 H;--CO 2 R 6 ;--SH,--S(O) n R. sup.6 ;--S(O) m--OH;--S(O) m--OR 6 ;--O--S(O) m--R. sup.6 ;--O--S(O) m OH;--O--S(O) m--OR. sup.6 ;--Z 4--NR. sup.7 R 8 ;--Z 4--N(R. sup.11)--Z 5--NR. sup.9 R 10 ; or R 4 and R 5 together are alkylene or alkenylene (either of which may be substituted with Z 1, Z 2 and Z 3), completing a 4-to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached.