1609477-94-2

Upstream product

• 51446-30-1 2-fluoro-5-hydroxybenzoic acid 
• 110-52-1 1,4-dibromo-butane 
• 1084801-91-1 methyl 2-fluoro-5-hydroxybenzoate 

Downstream Products

• 1609477-70-4 C₂₁H₂₃FO₆ 
• 1609477-16-8 5-(4-(4-acetyl-3-hydroxy-2-methylphenoxy)butoxy)-2-fluorobenzoic acid 
• 1609477-75-9 C₂₂H₂₅FO₆ 
• 1609477-21-5 2-fluoro-5-(4-(3-hydroxy-2-methyl-4-propionylphenoxy)butoxy)benzoic acid 
• 1609477-80-6 C₂₃H₂₇FO₆ 
• 1609477-26-0 2-fluoro-5-(4-(3-hydroxy-4-isobutyryl-2-methylphenoxy)butoxy)benzoic acid 
• 1609477-85-1 C₂₃H₂₇FO₆ 
• 1609477-31-7 5-(4-(4-butyryl-3-hydroxy-2-methylphenoxy)butoxy)-2-fluorobenzoic acid 
• 1609477-90-8 C₂₅H₃₁FO₆ 
• 1609477-36-2 5-(4-(4-(3,3-dimethylbutanoyl)-3-hydroxy-2-methylphenoxy)butoxy)-2-fluorobenzoic acid 
• 1609476-95-0 5-(4-(2,3-dimethyl-4-(3-methylbutanoyl)phenoxy)butoxy)-2-fluorobenzoic acid 
• 1609477-49-7 C₂₅H₃₁FO₅ 
• 1609476-96-1 5-(4-(4-(2-cyclopentylacetyl)-2,3-dimethylphenoxy)butoxy)-2-fluorobenzoic acid 
• 1609477-50-0 C₂₇H₃₃FO₅ 

Relevant academic research and scientific papers

Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics

In the present study, a series of benzamides, endowed with potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties, was synthesized and evaluated as potential antipsychotics. Among them, 3-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl)-piperidin-1-yl)butoxy)-N-methylbenzamide (21) and its fluoro-substituted analogue (22) held the best pharmacological binding profiles. They not only presented potent activities for D2, 5-HT1A, and 5-HT2A receptors, but were also endowed with low activities for 5-HT2C, H1 receptors and hERG channels, suggesting a low propensity of inducing weight gain and QT prolongation. In animal models, compounds 21 and 22 reduced phencyclidine-induced hyperactivity with a high threshold for catalepsy induction. It thus provides potential candidates for further preclinical studies.

Design and synthesis of systemically active metabotropic glutamate subtype-2 and -3 (mGlu2/3) receptor positive allosteric modulators (PAMs): Pharmacological characterization and assessment in a rat model of cocaine dependence

As part of our ongoing small-molecule metabotropic glutamate (mGlu) receptor positive allosteric modulator (PAM) research, we performed structure-activity relationship (SAR) studies around a series of group II mGlu PAMs. Initial analogues exhibited weak activity as mGlu2 receptor PAMs and no activity at mGlu3. Compound optimization led to the identification of potent mGlu2/3 selective PAMs with no in vitro activity at mGlu1,4-8 or 45 other CNS receptors. In vitro pharmacological characterization of representative compound 44 indicated agonist-PAM activity toward mGlu2 and PAM activity at mGlu 3. The most potent mGlu2/3 PAMs were characterized in assays predictive of ADME/T and pharmacokinetic (PK) properties, allowing the discovery of systemically active mGlu2/3 PAMs. On the basis of its overall profile, compound 74 was selected for behavioral studies and was shown to dose-dependently decrease cocaine self-administration in rats after intraperitoneal administration. These mGlu2/3 receptor PAMs have significant potential as small molecule tools for investigating group II mGlu pharmacology.