Search Results - "Lewicki, Sarah A"
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1
Functionalized Congeners of 2H-Chromene P2Y6 Receptor Antagonists
Published in Cells (Basel, Switzerland) (16-08-2024)“…The P2Y6 receptor (P2Y6R), a Gq-coupled receptor, is a potential drug discovery target for various inflammatory and degenerative conditions. Antagonists have…”
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2
Synthesis and pharmacological characterization of multiply substituted 2H-chromene derivatives as P2Y6 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-11-2022)“…P2Y6 receptor (P2Y6R) antagonists represent potential drugs for treating cancer, pain, neurodegeneration, asthma, diabetes, colitis and other disorders…”
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3
Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2 H -naphtho[1,2- b ][1,4]diazepine-2,4(3 H )-diones as P2X4 Receptor Antagonists
Published in Journal of medicinal chemistry (27-10-2022)“…We analyzed the P2X4 receptor structure-activity relationship of a known antagonist , a 1,5-dihydro-2 -naphtho[1,2- ][1,4]diazepine-2,4(3 )-dione. Following…”
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4
Machine learning-aided search for ligands of P2Y6 and other P2Y receptors
Published in Purinergic signalling (01-12-2024)“…The P2Y 6 receptor, activated by uridine diphosphate (UDP), is a target for antagonists in inflammatory, neurodegenerative, and metabolic disorders, yet few…”
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5
Stereocontrolled access to thioisosteres of nucleoside di- and triphosphates
Published in Nature chemistry (01-02-2024)“…Nucleoside diphosphates and triphosphates impact nearly every aspect of biochemistry; however, the use of such compounds as tools or medicinal leads for…”
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6
Alicyclic Ring Size Variation of 4-Phenyl-2-naphthoic Acid Derivatives as P2Y 14 Receptor Antagonists
Published in Journal of medicinal chemistry (13-07-2023)“…P2Y receptor (P2Y R) is activated by extracellular UDP-glucose, a damage-associated molecular pattern that promotes inflammation in the kidney, lung, fat…”
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7
Alicyclic Ring Size Variation of 4‑Phenyl-2-naphthoic Acid Derivatives as P2Y14 Receptor Antagonists
Published in Journal of medicinal chemistry (13-07-2023)“…P2Y14 receptor (P2Y14R) is activated by extracellular UDP-glucose, a damage-associated molecular pattern that promotes inflammation in the kidney, lung, fat…”
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8
Structure activity relationships of 5-HT2B and 5-HT2C serotonin receptor antagonists: N6, C2 and 5′-Modified (N)-methanocarba-adenosine derivatives
Published in European journal of medicinal chemistry (05-11-2023)“…(N)-Methanocarba adenosine derivatives were structurally modified to target 5-HT2B serotonin receptors as antagonists, predominantly containing branched…”
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9
In vivo phenotypic validation of adenosine receptor-dependent activity of non-adenosine drugs
Published in Purinergic signalling (01-09-2023)“…Some non-adenosinergic drugs are reported to also act through adenosine receptors (ARs). We used mouse hypothermia, which can be induced by agonism at any of…”
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10
Chimeras Derived from a P2Y 14 Receptor Antagonist and UDP-Sugar Agonists for Potential Treatment of Inflammation
Published in ACS pharmacology & translational science (11-10-2024)“…Tethered glycoconjugates of a naphthalene- and piperidine-containing antagonist of the P2Y receptor (PPTN) were synthesized, and their nM receptor binding…”
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11
Chimeras Derived from a P2Y14 Receptor Antagonist and UDP-Sugar Agonists for Potential Treatment of Inflammation
Published in ACS pharmacology & translational science (11-10-2024)“…Tethered glycoconjugates of a naphthalene- and piperidine-containing antagonist of the P2Y14 receptor (PPTN) were synthesized, and their nM receptor binding…”
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12
2‑Substituted (N)-Methanocarba A3 Adenosine Receptor Agonists: In Silico, In Vitro, and In Vivo Characterization
Published in ACS pharmacology & translational science (12-07-2024)“…2-Arylethynyl (N)-methanocarba adenosine 5′-methylamides are selective A3 adenosine receptor (AR) agonists containing a preestablished receptor-preferred…”
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13
2-Substituted (N)-Methanocarba A 3 Adenosine Receptor Agonists: In Silico, In Vitro, and In Vivo Characterization
Published in ACS pharmacology & translational science (12-07-2024)“…2-Arylethynyl (N)-methanocarba adenosine 5'-methylamides are selective A adenosine receptor (AR) agonists containing a preestablished receptor-preferred…”
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14
Structure–Activity Relationship and Neuroprotective Activity of 1,5-Dihydro‑2H‑naphtho[1,2‑b][1,4]diazepine-2,4(3H)‑diones as P2X4 Receptor Antagonists
Published in Journal of medicinal chemistry (27-10-2022)“…We analyzed the P2X4 receptor structure–activity relationship of a known antagonist 5, a 1,5-dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-dione…”
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Journal Article -
15
Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2H-naphtho1,2-b1,4diazepine-2,4(3H)-diones as P2X4 Receptor Antagonists
Published in Journal of medicinal chemistry (27-10-2022)“…We analyzed the P2X4 receptor structure-activity relationship of a known antagonist 5, a 1,5-dihydro-2H-naphtho[1,2-b][1,4]diazepine-2,4(3H)-dione. Following…”
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16
Potent and Selective Human 5-HT 2B Serotonin Receptor Antagonists: 4′-Cyano-(N)-methanocarba-adenosines by Synthetic Serendipity
Published in Journal of medicinal chemistry (26-11-2024)Get full text
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17
Functionalized Congeners of 2H-Chromene P2Y[sub.6] Receptor Antagonists
Published in Cells (Basel, Switzerland) (01-08-2024)“…The P2Y[sub.6] receptor (P2Y[sub.6]R), a G[sub.q]-coupled receptor, is a potential drug discovery target for various inflammatory and degenerative conditions…”
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18
Functionalized Congeners of 2 H -Chromene P2Y 6 Receptor Antagonists
Published in Cells (Basel, Switzerland) (16-08-2024)“…The P2Y receptor (P2Y R), a G -coupled receptor, is a potential drug discovery target for various inflammatory and degenerative conditions. Antagonists have…”
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Journal Article -
19
Machine learning-aided search for ligands of P2Y 6 and other P2Y receptors
Published in Purinergic signalling (25-03-2024)“…The P2Y receptor, activated by uridine diphosphate (UDP), is a target for antagonists in inflammatory, neurodegenerative, and metabolic disorders, yet few…”
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Journal Article -
20
Structure activity relationships of 5-HT 2B and 5-HT 2C serotonin receptor antagonists: N 6 , C2 and 5'-Modified (N)-methanocarba-adenosine derivatives
Published in European journal of medicinal chemistry (05-11-2023)“…(N)-Methanocarba adenosine derivatives were structurally modified to target 5-HT serotonin receptors as antagonists, predominantly containing branched N -alkyl…”
Get full text
Journal Article