Lawson, Edward C.; Santulli, Rosemary J.; Dyatkin, Alexey B.; Ballentine, Scott A.; Abraham, William M.; Rudman, Sandra; Page, Clive P.; de Garavilla, Lawrence; Damiano, Bruce P.; Kinney, William A.; Maryanoff, Bruce E. published an article in Bioorganic & Medicinal Chemistry. The title of the article was 《Selection of a 2-azabicyclo[2.2.2]octane-based α4β1 integrin antagonist as an inhaled anti-asthmatic agent》.Category: amides-buliding-blocks The author mentioned the following in the article:
The α4β1 integrin, expressed on eosinophils and neutrophils, induces inflammation in the lung by facilitating cellular infiltration and activation. From a number of potent α4β1 antagonists that the authors evaluated for safety and efficacy, compound (I) was selected as a lead candidate for antiasthma therapy by the inhalation route. The authors devised an optimized stereoselective synthesis to facilitate the preparation of a sufficiently large quantity of I for assessment in vivo. Administration of I to allergen-sensitive sheep by inhalation blocked the late-phase response of asthma and abolished airway hyper-responsiveness at 24 h following the antigen challenge. Addnl., the recruitment of inflammatory cells into the lungs was inhibited. Administration of I to ovalbumin-sensitized guinea pigs i.p. blocked airway resistance and inhibited the recruitment of inflammatory cells. The experimental part of the paper was very detailed, including the reaction process of 2,6-Dichloroisonicotinamide(cas: 89281-13-0Category: amides-buliding-blocks)
2,6-Dichloroisonicotinamide(cas: 89281-13-0) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Category: amides-buliding-blocks
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics