Ochiai, Hiroshi published the artcileOrally active PDE4 inhibitor with therapeutic potential, Application of 3,3,3-Trifluoropropan-1-ol, the publication is European Journal of Medicinal Chemistry (2004), 39(7), 555-571, database is CAplus and MEDLINE.
Based on the promising results obtained by the clin. trial of Ariflo (I), further optimization of the spatial arrangement of the three pharmacophores (the carboxylic acid moiety, nitrile moiety and 3-cyclopentyloxy-4-methoxyphenyl moiety) in the structure of I was attempted using a bicyclo[3 3 0]octane template with more stereochem. diversity than the cyclohexane template of I. Biol. evaluation of the decyanated analogs and further optimization of the cyclopentyloxy moiety of II (R = cyclopentyl; X = OH, NHOH) were also performed. Among the compounds tested, II [R = cyclopentyl; X = OH (III)], IV and II (X = OH, R = 2,3-dihydro-1H-indene-2-yl) were found to be orally active and were estimated to have therapeutic potential based on cross-species and same-species comparisons. The structure-activity relationships (SARs) of these compounds were investigated and pharmacokinetic data for III and IV (X = NHOH) were also obtained by single-dose studies in rats.
European Journal of Medicinal Chemistry published new progress about 2240-88-2. 2240-88-2 belongs to alcohols-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Aliphatic hydrocarbon chain,Alcohol, name is 3,3,3-Trifluoropropan-1-ol, and the molecular formula is C3H5F3O, Application of 3,3,3-Trifluoropropan-1-ol.
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