Singh, Sarita published the artcileSynthesis and evaluation of substituted 8,8-dimethyl-8H-pyrano[2,3-f]chromen-2-one derivatives as vasorelaxing agents, SDS of cas: 4584-49-0, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(1), 126759, database is CAplus and MEDLINE.
A series of substituted 8,8-dimethyl-8H-pyrano[2,3-f]chromen-2-ones I [R = Me, (CH2)2NMe2, CH2C(O)N(Me)(n-Bu), etc.] was synthesized from scopoletin as vasorelaxing agents. The synthesized compounds were evaluated for vasorelaxation in endothelium intact rat main mesenteric artery (MMA). Scopoletin, and compounds I [R = Me, CH2C(O)N(Me)(n-Bu), (CH2)4C(O)N(Me)(n-Bu), CH2C(O)NH(n-pentyl), (CH2)3C(O)N(Me)(n-pentyl), (CH2)4C(O)NH(n-pentyl)] showed significant vasorelaxation in precontracted MMA within the range of EC50 value 1.58-5.02μM. These derivatives presented 29.40-70.89 fold increased sensitivity for exptl. tissue compared to scopoletin, the parent mol. Among others, compound I [R = Me] was found to be the most active compound which had EC50 1.58μM with 70.89 fold increased sensitivity. The mechanistic evaluation of compound I [R = Me] showed that it exerted vasorelaxation through Ca2+-activated K+ (BKca) channel and the effect was endothelium-independent.
Bioorganic & Medicinal Chemistry Letters published new progress about 4584-49-0. 4584-49-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Salt,Amine,Aliphatic hydrocarbon chain, name is 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, and the molecular formula is C15H23BO2, SDS of cas: 4584-49-0.
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