Watson, Christine published the artcileOptimization of a novel series of selective CNS penetrant CB2 agonists, Formula: C4H10OS, the publication is Bioorganic & Medicinal Chemistry Letters (2011), 21(14), 4284-4287, database is CAplus and MEDLINE.
A series of benzimidazole CB2 receptor agonists were prepared and their properties investigated. Optimization of the three benzimidazole substituents led to the identification of I [R = cyclopropylmethyl, II], a potent CB2 full agonist (EC50 2.7 nM) with excellent selectivity over the CB1 receptor (>3000-fold). II demonstrated good CNS penetration in rats. Further optimization led to the identification of I [R = (2R)-2-tetrahydrofuranylmethyl] with improved selectivity over hERG and excellent CNS penetration in rat.
Bioorganic & Medicinal Chemistry Letters published new progress about 73303-88-5. 73303-88-5 belongs to alcohols-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Alcohol, name is 2-Methyl-2-sulfanylpropan-1-ol, and the molecular formula is C9H20Cl2Si, Formula: C4H10OS.
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