Search Results - "Looker, Brian E"
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Synthesis and Structure−Activity Relationships of Long-acting β2 Adrenergic Receptor Agonists Incorporating Metabolic Inactivation: An Antedrug Approach
Published in Journal of medicinal chemistry (10-06-2010)“…A series of saligenin β2 adrenoceptor agonist antedrugs having high clearance were prepared by reacting a protected saligenin oxazolidinone with protected…”
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The discovery of quinoline based single-ligand human H 1 and H 3 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-12-2016)“…A novel series of potent quinoline-based human H and H bivalent histamine receptor antagonists, suitable for intranasal administration for the potential…”
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Discovery of a rapidly metabolized, long-acting β(2) adrenergic receptor agonist with a short onset time incorporating a sulfone group suitable for once-daily dosing
Published in Journal of medicinal chemistry (09-01-2014)“…A series of novel, potent, and selective human β2 adrenoceptor agonists incorporating a sulfone moiety on the terminal right-hand-side phenyl ring of…”
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Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis
Published in Bioorganic & medicinal chemistry letters (01-11-2017)“…Selective human H1 histamine receptor antagonist pA2=9.3 with 24h duration of action. [Display omitted] A series of potent, selective and long-acting…”
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Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H 1 receptor antagonists for use in allergic rhinitis
Published in Bioorganic & medicinal chemistry letters (01-11-2017)“…A series of potent, selective and long-acting quinoline-based sulfonamide human H histamine receptor antagonists, designed for once-daily intranasal…”
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The discovery of quinoline based single-ligand human H1 and H3 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (15-12-2016)“…3-(8-(4-(4-(3-(Azepan-1-yl)propoxy)phenethyl)piperazin-1-yl)-6-butylquinolin-2-yl)propanoic acid; pA2=8.8 for H1 receptor; pKi=9.1 for H3 receptor. [Display…”
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Discovery of a Rapidly Metabolized, Long-Acting β2 Adrenergic Receptor Agonist with a Short Onset Time Incorporating a Sulfone Group Suitable for Once-Daily Dosing
Published in Journal of medicinal chemistry (09-01-2014)“…A series of novel, potent, and selective human β2 adrenoceptor agonists incorporating a sulfone moiety on the terminal right-hand-side phenyl ring of…”
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Design of Phthalazinone Amide Histamine H 1 Receptor Antagonists for Use in Rhinitis
Published in ACS medicinal chemistry letters (11-05-2017)“…The synthesis of potent amide-containing phthalazinone H histamine receptor antagonists is described. Three analogues , , and were equipotent with azelastine…”
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Design of Phthalazinone Amide Histamine H1 Receptor Antagonists for Use in Rhinitis
Published in ACS medicinal chemistry letters (11-05-2017)“…The synthesis of potent amide-containing phthalazinone H1 histamine receptor antagonists is described. Three analogues 3e, 3g, and 9g were equipotent with…”
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The Discovery of Phthalazinone-Based Human H1 and H3 Single-Ligand Antagonists Suitable for Intranasal Administration for the Treatment of Allergic Rhinitis
Published in Journal of medicinal chemistry (14-04-2011)“…A series of potent phthalazinone-based human H1 and H3 bivalent histamine receptor antagonists, suitable for intranasal administration for the potential…”
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Synthesis and Structure−Activity Relationships of Long-acting β2 Adrenergic Receptor Agonists Incorporating Arylsulfonamide Groups
Published in Journal of medicinal chemistry (23-04-2009)“…A series of saligenin alkoxyalkylphenylsulfonamide β2 adrenoceptor agonists were prepared by reacting a protected saligenin oxazolidinone with alkynyloxyalkyl…”
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12
discovery of long-acting saligenin β₂ adrenergic receptor agonists incorporating a urea group
Published in Bioorganic & medicinal chemistry (15-10-2011)“…A series of novel, potent and selective human β₂ adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of…”
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The discovery of long-acting saligenin β2 adrenergic receptor agonists incorporating hydantoin or uracil rings
Published in Bioorganic & medicinal chemistry (15-07-2011)“…A series of novel, potent and selective human β2 adrenoceptor agonists incorporating a hydantoin or a uracil ring on the right-hand side phenyl ring of…”
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14
4-Acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a Novel Class of Non-Brain-Penetrant Histamine H3 Receptor Antagonists
Published in Journal of medicinal chemistry (27-12-2007)“…A series of ketopiperazines were prepared and evaluated for their activity as histamine H3 antagonists. From investigation of the tertiary basic center in the…”
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The discovery of long-acting saligenin β 2 adrenergic receptor agonists incorporating a urea group
Published in Bioorganic & medicinal chemistry (15-10-2011)“…A series of novel, potent and selective human β 2 adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of (…”
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The discovery of long-acting saligenin [beta] sub(2 adrenergic receptor agonists incorporating a urea group)
Published in Bioorganic & medicinal chemistry (15-10-2011)“…A series of novel, potent and selective human [beta] sub(2 adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of…”
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4-Acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a Novel Class of Non-Brain-Penetrant Histamine H 3 Receptor Antagonists
Published in Journal of medicinal chemistry (27-12-2007)Get full text
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The discovery of long-acting saligenin beta sub(2 adrenergic receptor agonists incorporating hydantoin or uracil rings)
Published in Bioorganic & medicinal chemistry (15-07-2011)“…A series of novel, potent and selective human beta sub(2 adrenoceptor agonists incorporating a hydantoin or a uracil ring on the right-hand side phenyl ring of…”
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