176960-47-7

Usage

Uses

Used in Pharmaceutical Industry:
[1,1'-Biphenyl]-2-sulfonamide, N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)is used as a potential active pharmaceutical ingredient for its possible antibacterial and antifungal properties due to the presence of the sulfonamide group. [1,1'-Biphenyl]-2-sulfonamide,
N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)-'s specific side chains may also provide novel biological activities, making it a candidate for the development of new drugs.
Used in Research and Development:
In the field of chemical and biological research, [1,1'-Biphenyl]-2-sulfonamide, N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)can be used as a subject for studying the effects of its unique side chains on biological activity. This may lead to a better understanding of its potential applications in medicine and the creation of new therapeutic agents.

Upstream product

• 176961-14-1 N-(3,4-dimethyl-5-isoxazolyl)-N-[(methoxyethoxy)methyl]-4'-(2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-50-5 2-(4-bromophenyl)oxazole 
• 586-75-4 4-chlorobenzoyl chloride 
• 698-67-9 p-bromobenzamide 

Downstream Products

• 176961-18-5 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(5-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-19-6 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(4-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-34-5 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(2-oxazolylmethyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-20-9 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(2-methyl-4-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-21-0 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(4-methyl-2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-22-1 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(5-methyl-2-oxazolyl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-23-2 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(1H-pyrazol-1-yl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-26-5 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(1-methyl-1H-imidazole-2-yl)[1,1'-biphenyl]-2-sulfonamide 
• 176961-44-7 N-(3,4-Dimethyl-5-isoxazolyl)-2'-formyl-N-[(2-methoxyethoxy)methyl]-4'-(2-oxazolyl)-[1,1'-biphenyl]-2-sulfonamide 
• 176961-15-2 N-(3,4-Dimethyl-5-isoxazolyl)-N-[(2-methoxyethoxy)methyl]-4'-(2-thiazolyl)[1,1'-biphenyl]-2-sulfonamide 

Relevant academic research and scientific papers

Methods for the preparation of biphenyl isoxazole sulfonamides

Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates therof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endot

Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists

The synthesis and structure-activity relationship (SAR) studies of a series of 4'-oxazolyl-N-(3,4-dimethyl-5-isoxazolyl)[1, 1'-biphenyl]-2-sulfonamide derivatives as endothelin-A (ET(A)) receptor antagonists are described. The data reveal a remarkable improvement in potency and metabolic stability when the 4'-position of the biphenylsulfonamide is substituted with an oxazole ring. Additional 2'-substitution of an acylaminomethyl group further increased the binding activity and provided one of the first subnanomolar ET(A)-selective antagonists in the biphenylsulfonamide series (17, ET(A) K(i) = 0.2 nM). Among the compounds described, 3 (N-(3,4-dimethyl-5-isoxazolyl)-4'-(2-oxazolyl)[1,1'-biphenyl]-2-s ulfonamide; BMS-193884) had the optimum pharmacological profile and was therefore selected as a clinical candidate for studies in congestive heart failure.

Methods for the preparation of biphenyl isoxazole sulfonamides

Methods for the preparation of biphenyl isoxazole sulfonamides and intermediates thereof. The present invention also relates to the novel intermediates prepared by these methods. The biphenyl isoxazole sulfonamides prepared by the present methods are endothelin antagonists useful, inter alia, for the treatment of hypertension.

Substituted biphenyl isoxazole sulfonamides

Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R1, R2, R3 and R4 are each directly bonded to a ring carbon and are each independently (a) hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3 ; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) --C(O)H or --C(O)R5 ; (h) --CO2 H or --CO2 R5 ; (i) --Z4 --NR6 R7 ; (j) --Z4 --N(R10)--Z5 --NR8 R9 ; or (k) R3 and R4 together may also be alkylene or alkenylene, either of which may be substituted with Z1, Z2 and Z3, completing a 4- to 8-membered saturated, unsaturated or aromatic ring together with the carbon atoms to which they are attached; and the remaining symbols are as defined in the specification.

SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES

Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2, R 3 and R 4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy,

SUBSTITUTED BIPHENYL ISOXAZOLE SULFONAMIDES

Compounds of the formula STR1 inhibit the activity of endothelin. The symbols are defined as follows: R 1, R 2, R 3 and R 4 are each directly bonded to a ring carbon and are each independently(a) hydrogen;(b) alkyl, alkenyl, alkynyl, alkoxy,