Chatzopoulou, Maria published the artcileDecreasing acidity in a series of aldose reductase inhibitors: 2-Fluoro-4-(1H-pyrrol-1-yl)phenol as a scaffold for improved membrane permeation, COA of Formula: C10H9NO, the publication is Bioorganic & Medicinal Chemistry (2014), 22(7), 2194-2207, database is CAplus and MEDLINE.
Targeting long-term diabetic complications, as well as inflammatory pathologies, aldose reductase inhibitors (ARIs) have been gaining attention over the years. In the present work, in order to address the poor membrane permeation of previously reported ARIs, derivatives of N-phenylpyrrole, bearing groups with putative pKa ≥ 7.4, were synthesized and evaluated for aldose reductase inhibitory activity. The 2-fluorophenol group proved the most promising moiety, and further modifications were explored. The most active compound was identified as a submicromolar inhibitor (IC50 = 0.443 μM), was also selective against the homologous enzyme aldehyde reductase. Cross-docking revealed that the above mentioned compound displays a peculiar interaction network that may be responsible for high affinity. Physicochem. profiling of it showed a pKa of 7.64, rendering it less than 50% ionized in the physiol. pH range, with potentially favorable membrane permeation. The latter was supported from the successful inhibition of sorbitol formation in rat lenses and the ability to permeate rat jejunum.
Bioorganic & Medicinal Chemistry published new progress about 23351-09-9. 23351-09-9 belongs to alcohols-buliding-blocks, auxiliary class Pyrrole,Benzene,Alcohol, name is 4-(1H-Pyrrol-1-yl)phenol, and the molecular formula is C10H9NO, COA of Formula: C10H9NO.
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https://en.wikipedia.org/wiki/Alcohol,
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