716362-11-7

Upstream product

• 158840-78-9 3-(pyridin-2-yl)-5-hydroxymethylisoxazole 
• 873-69-8 2-pyridinealdoxime 
• 439126-55-3 3-(pyridin-2-yl)isoxazole-5-carboxylic acid ethyl ester 
• 39977-58-7 N-hydroxypyridine-2-carboximidoyl chloride hydrochloride 
• 330558-58-2 3-pyridin-2-ylisoxazole-5-carboxylic acid methyl ester 

Downstream Products

• 1198119-10-6 C₂₆H₂₃N₃O₄S 

Relevant academic research and scientific papers

5-Substituted pyridylisoxazoles as effective inhibitors of platelet aggregation

A series of 5-substituted 3-pyridylisoxazoles were synthesized using [3+2] cycloaddition of nitrile oxides to alkynes with variation of substituents at position 5 of the isoxazole ring without additional synthetic stages and with retention of 2-pyridyl-, 3-pyridyl, and 4-pyridyl substituents at position 3 of the isoxazole ring. Substituted pyridylisoxazoles are the potential antiaggregatory agents showing in vitro activity in the concentration range from 1?10-6 mol L-1 to 1?10-4 mol L-1 toward the human platelet rich blood plasma with arachidonic acid being used as the inductor of aggregation. These compounds do not act as cyclooxygenase or thromboxane synthase inhibitors, nor as thrombin inhibitors.

Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases

We describe here the identification of non-peptidic vinylsulfones that inhibit parasite cysteine proteases in vitro and inhibit the growth of Trypanosoma brucei brucei parasites in culture. A high resolution (1.75 A) co-crystal structure of 8a bound to cruzain reveals how the non-peptidic P2/P3 moiety in such analogs bind the S2 and S3 subsites of the protease, effectively recapitulating important binding interactions present in more traditional peptide-based protease inhibitors and natural substrates.

Concise synthesis and antimicrobial activities of new substituted 5-isoxazolpenicillins

The synthesis of a series of new 5-isoxazolpenicillins is described, which were obtained by coupling substituted isoxazoles with 6-APA. Concise large-scale synthesis of 3,5-disubstituted isoxazoles by 1,3-dipolar cycloaddition using copper(I) as catalyst was also investigated. Representative compounds were assayed for antimicrobial activities, showing satisfactory antimicrobial activities against Gram-negative bacteria.

Ramoplanin derivatives possessing antibacterial activity

Novel ramoplanin derivatives are disclosed. These ramoplanin derivatives exhibit antibacterial activity. As the compounds of the subject invention exhibit potent activities against gram positive bacteria, they are useful antimicrobial agents. Methods of synthesis and of use of the compounds are also disclosed.