Barbara A. Bricker
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View article: Enantiomeric Separation, Absolute Configuration by X-ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5-HT<sub>1A</sub> and 5-HT<sub>7A</sub> Receptors
Enantiomeric Separation, Absolute Configuration by X-ray Crystallographic Analysis, and Functional Evaluation of Enantiomers of the Dual Ligand, SYA0340 at 5-HT<sub>1A</sub> and 5-HT<sub>7A</sub> Receptors Open
We have previously identified 5-chloro-2-methyl-2-(3-(4-(pyridin-2-yl)piperazin-1-yl)propyl)-2,3-dihydro-1H-inden-1-one (SYA0340) as a dual 5-HT1A and 5-HT7 receptor ligand, and we posited such ligands might find utility in the treatment o…
View article: An Evaluation of the Anticancer Properties of SYA014, a Homopiperazine-Oxime Analog of Haloperidol in Triple Negative Breast Cancer Cells
An Evaluation of the Anticancer Properties of SYA014, a Homopiperazine-Oxime Analog of Haloperidol in Triple Negative Breast Cancer Cells Open
Triple negative breast cancer (TNBC) is a type of breast cancer associated with early metastasis, poor prognosis, high relapse rates, and mortality. Previously, we demonstrated that SYA013, a selective σ2RL, could inhibit cell proliferatio…
View article: Design and Discovery of a High Affinity, Selective and β-Arrestin Biased 5-HT7 Receptor Agonist
Design and Discovery of a High Affinity, Selective and β-Arrestin Biased 5-HT7 Receptor Agonist Open
Compound 1c, 2-(2-(3,4-Dihydroisoquinolin-2(1H)-yl)ethyl)-5-fluoro-2,3-dihydro-1H-inden-1-one was previously reported from our laboratory showing high affinity binding to the 5-HT7 receptor (Ki = 0.5 nM). However, compound 1c racemizes rea…
View article: Identification of a new selective dopamine D4 receptor ligand
Identification of a new selective dopamine D4 receptor ligand Open
The dopamine D4 receptor has been shown to play key roles in certain CNS pathologies including addiction to cigarette smoking. Thus, selective D4 ligands may be useful in treating some of these conditions. Previous studies in our laborator…
View article: Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-Chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one
Identification of a butyrophenone analog as a potential atypical antipsychotic agent: 4-[4-(4-Chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one Open
The synthesis and exploration of novel butyrophenones have led to the identification of a diazepane analog of haloperidol, 4-[4-(4-Chlorophenyl)-1,4-diazepan-1-yl]-1-(4-fluorophenyl)butan-1-one (Compound 13) with an interesting multirecept…
View article: Further evaluation of the tropane analogs of haloperidol
Further evaluation of the tropane analogs of haloperidol Open
Previous work from our labs has indicated that a tropane analog of haloperidol with potent D2 binding but designed to avoid the formation of MPP+-like metabolites, such as 4-(4-chlorophenyl)-1-(4-(4-fluorophenyl)-4-oxobutyl)pyridin-1-ium (…
View article: Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands
Design and synthesis of dual 5-HT1A and 5-HT7 receptor ligands Open
5-HT and 5-HT receptors have been at the center of discussions recently due in part to their major role in the etiology of major central nervous system diseases such as depression, sleep disorders, and schizophrenia. As part of our search …
View article: Enantioseparation of 5‐chloro‐2‐{2‐[3,4‐dihydroisoquinoline‐2(1<i>H</i>)‐yl]ethyl}‐2‐methyl‐2,3‐dihydro‐1<i>H</i>‐inden‐1‐one (SYA 40247), a high‐affinity 5‐HT<sub>7</sub> receptor ligand, by HPLC–PDA using amylose tris‐(3, 5‐ dimethylphenylcarbamate) as a chiral stationary phase
Enantioseparation of 5‐chloro‐2‐{2‐[3,4‐dihydroisoquinoline‐2(1<i>H</i>)‐yl]ethyl}‐2‐methyl‐2,3‐dihydro‐1<i>H</i>‐inden‐1‐one (SYA 40247), a high‐affinity 5‐HT<sub>7</sub> receptor ligand, by HPLC–PDA using amylose tris‐(3, 5‐ dimethylphenylcarbamate) as a chiral stationary phase Open
In previous structure–activity relationship studies to identify new and selective 5‐HT 7 receptor (5‐HT 7 R) ligands, we identified the chiral compound, 5‐chloro‐2‐{2‐[3,4‐dihydroisoquinoline‐2(1 H )‐yl]ethyl}‐2‐methyl‐2,3‐dihydro‐1 H ‐ind…
View article: The Mechanistic Targets of Antifungal Agents: An Overview
The Mechanistic Targets of Antifungal Agents: An Overview Open
Pathogenic fungi are a major causative group for opportunistic infections (OIs). AIDS patients and other immunocompromised individuals are at risk for OIs, which if not treated appropriately, contribute to the mortality associated with the…