63285-84-7

Upstream product

• 872-31-1 3-Bromothiophene 
• 108-95-2 phenol 

Downstream Products

• 81028-68-4 3-phenoxythiophene-2-carboxylic acid 
• 81028-69-5 4-phenoxythiophene-2-carboxylic acid 
• 81028-70-8 3-phenoxythiophene-2,5-dicarboxylic acid 
• 166964-13-2 3-phenoxythiophene-2-sulfonyl chloride 
• 132706-25-3 3-phenoxythiophene-2-carboxaldehyde 
• 132706-26-4 4-phenoxy-5-trimethylsilylthiophene-2-carboxaldehyde 
• 1260170-07-7 3-phenoxy-4-phenylthiophene 

Relevant academic research and scientific papers

Biphenylsulfonamides and derivatives thereof that modulate the activity of endothelin

Biphenylsulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, bicyclic or tricyclic carbon or heterocyclic ring biphenylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin

Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

THIENYL-, FURYL- AND PYRROLYL SULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN

Thienyl-, furyl-and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl) furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

SULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN

Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula I: STR1 in which Ar 1 is a 3-or 5-isoxazolyl and Ar. sup.2 is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar 2 is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar. sup.1 is a 4-halo-substituted isoxazole are more active than the corresponding alkyl-substituted compound and compounds in which Ar 1 is substituted at this position with a higher alkyl tend to exhibit greater affinity for ET B receptors than the corresponding lower alkyl-substituted compound.

Thiophenesulfonamides as endothelin receptor antagonists

The synthesis and in vitro binding affinities of a series of thiophenesulfonamides as ET(A) selective endothelin receptor antagonists is described. The most potent inhibitor displayed an IC50 of 43 nM and 3 μM to ET(A) and ET(B) receptors, respectively.

UREA BASED LIPOXYGENASE INHIBITING COMPOUNDS

Substituted phenyl, naphthyl, and thienyl N-hydroxy urea compounds form a class of potent inhibitors of 5-and 12-lipoxygenase and are thus useful compounds in the treatment of inflammatory disease states where leukotrienes and other products of lipoxygenase enzyme activity are implicated.

Application of Regioselective Thiophene Lithiation to the Synthesis of Thiophene Analogues of Xanthones and Thioxanthones

Treatment of 3-(p-tolyloxy)thiophene (3) with phenyllithium followed by carbonation with CO2 was found to be a convenient procedure for the preparation of the thiophene-2-carboxylic acid 4, which was cyclized to 5 with PPE.Treatment of 3 with butyllithium followed by carbonation gave the thiophene-2,5-dicarboxylic acid 8 which was cyclized to 9.Alkaline permanganate oxidation of 4 gave the diacid 10, which was cyclized to the tricyclic acid 11.Similar lithiation reactions were observed with additional 3-(aryloxy)thiophenes and with 3-(arylthio)thiophenes, and xanthone analogues were prepared from the resulting intermediates.