Search Results - "Geiss, William"
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Design, Synthesis, and Structure−Activity Relationships of Novel 2-Substituted Pyrazinoylguanidine Epithelial Sodium Channel Blockers: Drugs for Cystic Fibrosis and Chronic Bronchitis
Published in Journal of medicinal chemistry (13-07-2006)“…Amiloride (1), the prototypical epithelial sodium channel (ENaC) blocker, has been administered with limited success as aerosol therapy for improving pulmonary…”
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Synthesis and Pharmacological Evaluation of Novel γ-Aminobutyric Acid Type B (GABAB) Receptor Agonists as Gastroesophageal Reflux Inhibitors
Published in Journal of medicinal chemistry (24-07-2008)“…We have previously demonstrated that the prototypical GABAB receptor agonist baclofen inhibits transient lower esophageal sphincter relaxations (TLESRs), the…”
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Synthesis and SAR development of novel P2X₇ receptor antagonists for the treatment of pain: Part 2
Published in Bioorganic & medicinal chemistry letters (15-12-2011)“…Novel P2X₇ antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X₇ receptor in human and rodent as well as…”
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Effects of (2R)‐(3‐amino‐2‐fluoropropyl)sulphinic acid (AFPSiA) on transient lower oesophageal sphincter relaxation in dogs and mechanism of hypothermic effects in mice
Published in British journal of pharmacology (01-09-2005)“…The effects of the novel GABA analogue (2R)‐(3‐amino‐2‐fluoropropyl)sulphinic acid (AFPSiA) on transient lower oesophageal sphincter relaxations (TLOSRs) were…”
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A Stereospecific Synthesis of 24(S)-Hydroxyvitamin D2, a Prodrug for 1α,24(S)-Dihydroxyvitamin D2
Published in Organic process research & development (17-05-2002)“…This contribution describes the first stereospecific synthesis of 24(S)-hydroxyvitamin D2 (1), a metabolite of vitamin D2. This metabolite acts as a prodrug…”
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Synthesis and SAR development of novel P2X 7 receptor antagonists for the treatment of pain: Part 1
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Structure–activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X 7 receptor antagonists with improved…”
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Synthesis and SAR development of novel P2X sub(7 receptor antagonists for the treatment of pain: Part 1)
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X sub(7 receptor antagonists with…”
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Synthesis and SAR development of novel P2X₇ receptor antagonists for the treatment of pain: Part 1
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Structure–activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X₇ receptor antagonists with improved…”
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Synthesis and SAR development of novel P2X 7 receptor antagonists for the treatment of pain: Part 2
Published in Bioorganic & medicinal chemistry letters (2011)“…Novel P2X 7 antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X 7 receptor in human and rodent as well as…”
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A Stereospecific Synthesis of 24( S )-Hydroxyvitamin D 2 , a Prodrug for 1α,24( S )-Dihydroxyvitamin D 2
Published in Organic process research & development (01-05-2002)Get full text
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Effect of triplet-state sensitization on inter- and intramolecular 2+2 photocycloadditions of 2,5-cyclohexadien-1-ones
Published in Journal of the American Chemical Society (01-04-1991)Get full text
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