Pero, Joseph E. published the artcileDesign and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model, Product Details of C7H3Cl2NO2S, the publication is Journal of Medicinal Chemistry (2018), 61(24), 11209-11220, database is CAplus and MEDLINE.
Pulmonary edema is a common ailment of heart failure patients and has remained an unmet medical need due to dose-limiting side effects associated with current treatments. Preclin. studies in rodents have suggested that inhibition of transient receptor potential vanilloid-4 (TRPV4) cation channels may offer an alternative-and potentially superior-therapy. Efforts directed toward small-mol. antagonists of the TRPV4 receptor have led to the discovery of a novel sulfone pyrrolidine sulfonamide chemotype exemplified by lead compound 6. Design elements toward the optimization of TRPV4 activity, selectivity, and pharmacokinetic properties are described. Activity of leading exemplars 19 and 27 in an in vivo model suggestive of therapeutic potential is highlighted herein.
Journal of Medicinal Chemistry published new progress about 254749-11-6. 254749-11-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Benzene, name is 2-Chloro-4-cyanobenzene-1-sulfonyl chloride, and the molecular formula is C7H3Cl2NO2S, Product Details of C7H3Cl2NO2S.
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