Search Results - "CONNORS, Patrick J"
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Synthesis and Structure–activity relationships of 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils as antagonists of the human GnRH Receptor
Published in Bioorganic & medicinal chemistry letters (06-10-2003)“…A new class of small molecule GnRH antagonists, the 1-arylmethyl-3-(1-methyl-2-amino)ethyl-5-aryl-6-methyluracils, was designed and a novel stereoselective…”
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Initial Structure–Activity Relationship Studies of a Novel Series of Pyrrolo[1,2- a]pyrimid-7-ones as GnRH Receptor Antagonists
Published in Bioorganic & medicinal chemistry letters (11-02-2002)“…Initial SAR studies on 1-aminomethyl-2-aryl-3-cyano-pyrrolo[1,2- a]pyrimid-7-one-6-carboxylates as human GnRH receptor antagonists were discussed…”
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Synthesis and Structure−Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists
Published in Journal of medicinal chemistry (26-02-2004)“…Based on the SAR from bicyclic gonadotropin-releasing hormone (GnRH) antagonists such as 6-aminomethyl-7-aryl-pyrrolo[1,2-a]pyrimid-4-ones (5) and…”
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A Novel Synthesis of 2-Arylpyrrolo[1,2- a]pyrimid-7-ones and Their Structure–Activity Relationships as Potent GnRH Receptor Antagonists
Published in Bioorganic & medicinal chemistry letters (11-02-2002)“…In the process of developing GnRH receptor antagonists, a novel base-catalyzed cyclization of compounds 5a– b was discovered, which led to the formation of the…”
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Design and Structure−Activity Relationships of 2-Alkyl-3-aminomethyl-6-(3-methoxyphenyl)-7-methyl-8-(2-fluorobenzyl)imidazolo[1,2-a]pyrimid-5-ones as Potent GnRH Receptor Antagonists
Published in Journal of medicinal chemistry (24-04-2003)“…SAR studies of 7-phenylpyrrolo[1,2-a]pyrimid-4-ones 1 and 2, and 2-phenylimidazolo[1,2-a]pyrimidines 3 and 4, as nonpeptide human GnRH receptor antagonists,…”
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3-(2-Aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl- uracils as Orally Bioavailable Antagonists of the Human Gonadotropin Releasing Hormone Receptor
Published in Journal of medicinal chemistry (01-07-2004)“…Uracils possessing N-3 side chains derived from various amino alcohols were designed and synthesized as potent human gonadotropin releasing hormone receptor…”
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Identification of 1-Arylmethyl-3- (2-aminoethyl)-5-aryluracil as Novel Gonadotropin-Releasing Hormone Receptor Antagonists
Published in Journal of medicinal chemistry (22-05-2003)“…Based on SAR from bicyclic GnRH antagonists such as 6-aminomethyl-7-arylpyrrolo[1,2-a]pyrimid-4-ones (1) and 2-aryl-3-aminomethylimidazolo[1,2-a]pyrimid-5-ones…”
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A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2- a]pyrimid-4-ones as potent, stable GnRH receptor antagonists
Published in Bioorganic & medicinal chemistry letters (02-12-2002)“…A new class of small molecule GnRH antagonists, the 7-aryl-8-fluoro-pyrrolo[1,2- a]pyrimid-4-ones, was designed and a novel synthesis for these compounds was…”
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Synthesis and structure–activity relationships of uracil derived human GnRH receptor antagonists: ( R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5
Published in Bioorganic & medicinal chemistry letters (04-10-2004)“…The design and synthesis of a number of 5-thiazolyl and 5-thienyl substituted uracils is described and results from SAR studies are summarized. The best…”
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Design, synthesis and structure–Activity relationships of novel imidazolo[1,2- a]pyrimid-5-ones as potent GnRH receptor antagonists
Published in Bioorganic & medicinal chemistry letters (19-08-2002)“…SAR studies of lead GnRH receptor antagonists 2a and 2b reported earlier resulted in the discovery of compound 10b which showed much higher potency ( K i=4.6…”
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Coordination Compounds as Building Blocks: Single-Step Synthesis of Heteronuclear Multimetallic Complexes Containing RuII and OsII
Published in Inorganic chemistry (09-03-1998)Get full text
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Synthesis and initial structure–Activity relationships of a novel series of imidazolo[1,2- a]pyrimid-5-ones as potent GnRH receptor antagonists
Published in Bioorganic & medicinal chemistry letters (19-08-2002)“…SAR studies of 2-arylimidazolo[1,2- a]pyrimid-5-ones 10a– m, which were derived from initial lead 3a, resulted in the discovery of a series of potent…”
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Coordination Compounds as Building Blocks: Single-Step Synthesis of Heteronuclear Multimetallic Complexes Containing Ru II and Os II
Published in Inorganic chemistry (09-03-1998)Get full text
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