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  1. Article: Enantioselective total synthesis of (+)-obtusenyne.

    Crimmins, Michael T / Powell, Mark T

    Journal of the American Chemical Society

    2003  Volume 125, Issue 25, Page(s) 7592–7595

    Abstract: A total synthesis of the laurencia metabolite (+)-obtusenyne has been completed. The key steps include a Sharpless kinetic resolution and an asymmetric glycolate alkylation to establish the stereogenic centers adjacent to the ether linkage and a ring- ... ...

    Abstract A total synthesis of the laurencia metabolite (+)-obtusenyne has been completed. The key steps include a Sharpless kinetic resolution and an asymmetric glycolate alkylation to establish the stereogenic centers adjacent to the ether linkage and a ring-closing metathesis reaction to construct the nine-membered ether without the aid of a cyclic conformational constraint. The synthesis was completed in 20 linear steps from commercially available 1,5-hexadiene-3-ol.
    MeSH term(s) Alkynes/chemical synthesis ; Ethers, Cyclic/chemical synthesis ; Rhodophyta/chemistry
    Chemical Substances Alkynes ; Ethers, Cyclic ; obtusenyne
    Language English
    Publishing date 2003-06-25
    Publishing country United States
    Document type Journal Article ; Research Support, U.S. Gov't, P.H.S.
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/ja029956v
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Optically active iridium imidazol-2-ylidene-oxazoline complexes: preparation and use in asymmetric hydrogenation of arylalkenes.

    Perry, Marc C / Cui, Xiuhua / Powell, Mark T / Hou, Duen-Ren / Reibenspies, Joseph H / Burgess, Kevin

    Journal of the American Chemical Society

    2003  Volume 125, Issue 1, Page(s) 113–123

    Abstract: This work explores the potential of iridium complexes of the N-heterocyclic carbene oxazoline ligands 1 in asymmetric hydrogenations of arylalkenes. The accessible carbene precursors, imidazolium salts 2, and robust iridium complexes 5 facilitated a ... ...

    Abstract This work explores the potential of iridium complexes of the N-heterocyclic carbene oxazoline ligands 1 in asymmetric hydrogenations of arylalkenes. The accessible carbene precursors, imidazolium salts 2, and robust iridium complexes 5 facilitated a discovery/optimization approach that featured preparation of a small library of iridium complexes, parallel hydrogenation reactions, and automated analysis. Three of the complexes (5ab, 5ad, and 5dp) and a similar rhodium complex (6ap) were studied by single-crystal X-ray diffraction techniques. This revealed molecular features of 6ap, and presumably the corresponding iridium complex 5ap, that the others do not have. In enantioselective hydrogenations of arylalkenes complex 5ap was the best for many, but not all, substrates. The enantioselectivities and conversions observed were sensitive to minor changes to the catalyst and substrate structure. Ligands with aliphatic N-heterocyclic carbene substituents gave complexes that are inactive, and do not lose the 1,5-cyclooctadiene ligands under the hydrogenation conditions. Experiments to investigate this unexpected observation imply that it is of a steric, rather than an electronic, origin. Temperature and pressure effects on the conversions and enantioselectivities of these reactions had minimal effects for some alkenes, but profound effects for others. In one case, the enantioselectivities obtained at high-pressure/low-temperature conditions were opposite to those obtained under high-temperature/low-pressure conditions (-64% enantiomeric excess versus +89% enantiomeric excess); a transformation from one prevalent mechanism to another is inferred from this. The studies of pressure dependence revealed that many reactions proceeded with high conversions, and optimal enantioselectivities in approximately 2 h when only 1 bar of hydrogen was used. Deuterium-labeling experiments provide evidence for other types of competing mechanisms that lead to D-incorporation at positions that do not correspond to direct addition to the double bond.
    Language English
    Publishing date 2003-01-08
    Publishing country United States
    Document type Journal Article
    ZDB-ID 3155-0
    ISSN 1520-5126 ; 0002-7863
    ISSN (online) 1520-5126
    ISSN 0002-7863
    DOI 10.1021/ja028142b
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  3. Article ; Online: Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists.

    Shook, Brian C / Chakravarty, Devraj / Barbay, J Kent / Wang, Aihua / Leonard, Kristi / Alford, Vernon / Powell, Mark T / Rassnick, Stefanie / Scannevin, Robert H / Carroll, Karen / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Lampron, Lisa / Westover, Lori / Rhodes, Kenneth / Jackson, Paul F

    Bioorganic & medicinal chemistry letters

    2013  Volume 23, Issue 9, Page(s) 2688–2691

    Abstract: A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A2A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse ... ...

    Abstract A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A2A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.
    MeSH term(s) Adenosine A2 Receptor Antagonists/chemistry ; Adenosine A2 Receptor Antagonists/pharmacokinetics ; Adenosine A2 Receptor Antagonists/therapeutic use ; Animals ; Brain/metabolism ; Catalepsy/drug therapy ; Half-Life ; Humans ; Kinetics ; Mice ; Protein Binding ; Pyrimidines/chemistry ; Pyrimidines/pharmacokinetics ; Pyrimidines/therapeutic use ; Rats ; Receptor, Adenosine A2A/chemistry ; Receptor, Adenosine A2A/metabolism
    Chemical Substances Adenosine A2 Receptor Antagonists ; Pyrimidines ; Receptor, Adenosine A2A
    Language English
    Publishing date 2013-05-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2013.02.078
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  4. Article: Substituted thieno[2,3-d]pyrimidines as adenosine A₂A receptor antagonists

    Shook, Brian C / Chakravarty, Devraj / Barbay, J. Kent / Wang, Aihua / Leonard, Kristi / Alford, Vernon / Powell, Mark T / Rassnick, Stefanie / Scannevin, Robert H / Carroll, Karen / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Lampron, Lisa / Westover, Lori / Rhodes, Kenneth / Jackson, Paul F

    Bioorganic & medicinal chemistry letters. 2013 May 1, v. 23, no. 9

    2013  

    Abstract: A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A₂A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse ... ...

    Abstract A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A₂A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.
    Keywords adenosine ; antagonists ; chemistry ; mice ; pyrimidines
    Language English
    Dates of publication 2013-0501
    Size p. 2688-2691.
    Publishing place Elsevier Ltd
    Document type Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2013.02.078
    Database NAL-Catalogue (AGRICOLA)

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  5. Article ; Online: Design and characterization of optimized adenosine A₂A/A₁ receptor antagonists for the treatment of Parkinson's disease.

    Shook, Brian C / Rassnick, Stefanie / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Chakravarty, Devraj / Barbay, J Kent / Wang, Aihua / Powell, Mark T / Leonard, Kristi / Alford, Vernon / Scannevin, Robert H / Carroll, Karen / Lampron, Lisa / Westover, Lori / Lim, Heng-Keang / Russell, Ronald / Branum, Shawn / Wells, Kenneth M /
    Damon, Sandra / Youells, Scott / Li, Xun / Beauchamp, Derek A / Rhodes, Kenneth / Jackson, Paul F

    Journal of medicinal chemistry

    2012  Volume 55, Issue 3, Page(s) 1402–1417

    Abstract: The design and characterization of two, dual adenosine A(2A)/A(1) receptor antagonists in several animal models of Parkinson's disease is described. Compound 1 was previously reported as a potential treatment for Parkinson's disease. Further ... ...

    Abstract The design and characterization of two, dual adenosine A(2A)/A(1) receptor antagonists in several animal models of Parkinson's disease is described. Compound 1 was previously reported as a potential treatment for Parkinson's disease. Further characterization of 1 revealed that it was metabolized to reactive intermediates that caused the genotoxicity of 1 in the Ames and mouse lymphoma L51784 assays. The identification of the metabolites enabled the preparation of two optimized compounds 13 and 14 that were devoid of the metabolic liabilities associated with 1. Compounds 13 and 14 are potent dual A(2A)/A(1) receptor antagonists that have excellent activity, after oral administration, across a number of animal models of Parkinson's disease including mouse and rat models of haloperidol-induced catalepsy, mouse and rat models of reserpine-induced akinesia, and the rat 6-hydroxydopamine (6-OHDA) lesion model of drug-induced rotation.
    MeSH term(s) Adenosine A1 Receptor Antagonists/chemical synthesis ; Adenosine A1 Receptor Antagonists/pharmacokinetics ; Adenosine A1 Receptor Antagonists/pharmacology ; Adenosine A2 Receptor Antagonists/chemical synthesis ; Adenosine A2 Receptor Antagonists/pharmacokinetics ; Adenosine A2 Receptor Antagonists/pharmacology ; Administration, Oral ; Animals ; Drug Design ; Female ; Indenes/chemical synthesis ; Indenes/pharmacokinetics ; Indenes/pharmacology ; Macaca fascicularis ; Male ; Mice ; Mice, Inbred BALB C ; Parkinsonian Disorders/chemically induced ; Parkinsonian Disorders/drug therapy ; Pyrimidines/chemical synthesis ; Pyrimidines/pharmacokinetics ; Pyrimidines/pharmacology ; Rats ; Rats, Sprague-Dawley ; Receptor, Adenosine A2A/metabolism ; Structure-Activity Relationship
    Chemical Substances 2-amino-8-(2-morpholinoethoxy)-4-phenyl-5H-indeno(1,2-d)pyrimidin-5-one ; 2-amino-8-(4-methylpiperazine-1-carbonyl)-4-phenyl-5H-indeno(1,2-d)pyrimidin-5-one ; Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Indenes ; Pyrimidines ; Receptor, Adenosine A2A
    Language English
    Publishing date 2012-02-09
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/jm201640m
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.B 151: Show issues Location:
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  6. Article ; Online: Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.

    Shook, Brian C / Rassnick, Stefanie / Chakravarty, Devraj / Wallace, Nathaniel / Ault, Mark / Crooke, Jeffrey / Barbay, J Kent / Wang, Aihua / Leonard, Kristi / Powell, Mark T / Alford, Vernon / Hall, Daniel / Rupert, Kenneth C / Heintzelman, Geoffrey R / Hansen, Kristen / Bullington, James L / Scannevin, Robert H / Carroll, Karen / Lampron, Lisa /
    Westover, Lori / Russell, Ronald / Branum, Shawn / Wells, Kenneth / Damon, Sandra / Youells, Scott / Beauchamp, Derek / Li, Xun / Rhodes, Kenneth / Jackson, Paul F

    Bioorganic & medicinal chemistry letters

    2010  Volume 20, Issue 9, Page(s) 2868–2871

    Abstract: Two reactive metabolites were identified in vivo for the dual A(2A)/A(1) receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a ... ...

    Abstract Two reactive metabolites were identified in vivo for the dual A(2A)/A(1) receptor antagonist 1. Two strategies were implemented to successfully mitigate the metabolic liabilities associated with 1. Optimization of the arylindenopyrimidines led to a number of amide, ether, and amino analogs having comparable in vitro and in vivo activity.
    MeSH term(s) Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Animals ; Catalepsy/drug therapy ; Disease Models, Animal ; Mice ; Neurotransmitter Agents/chemical synthesis ; Neurotransmitter Agents/chemistry ; Neurotransmitter Agents/therapeutic use ; Pyrimidines/chemical synthesis ; Pyrimidines/chemistry ; Pyrimidines/therapeutic use ; Receptor, Adenosine A1/metabolism ; Receptor, Adenosine A2A/metabolism ; Structure-Activity Relationship
    Chemical Substances Adenosine A1 Receptor Antagonists ; Adenosine A2 Receptor Antagonists ; Neurotransmitter Agents ; Pyrimidines ; Receptor, Adenosine A1 ; Receptor, Adenosine A2A
    Language English
    Publishing date 2010-05-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2010.03.024
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  7. Article: Substituted thieno[2,3-d]pyrimidines as adenosine A₂A receptor antagonists

    Shook, Brian C. / Chakravarty, Devraj / Barbay, J. Kent / Wang, Aihua / Leonard, Kristi / Alford, Vernon / Powell, Mark T. / Rassnick, Stefanie / Scannevin, Robert H. / Carroll, Karen / Wallace, Nathaniel / Crooke, Jeffrey / Ault, Mark / Lampron, Lisa / Westover, Lori / Rhodes, Kenneth / Jackson, Paul F.

    Bioorganic & medicinal chemistry letters

    Volume v. 23,, Issue no. 9

    Abstract: A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A₂A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse ... ...

    Abstract A novel series of benzyl substituted thieno[2,3-d]pyrimidines were identified as potent A₂A receptor antagonists. Several five- and six-membered heterocyclic replacements for the optimized methylfuran were explored. Select compounds effectively reverse catalepsy in mice when dosed orally.
    Keywords mice ; adenosine ; chemistry ; pyrimidines ; antagonists
    Language English
    Document type Article
    ISSN 0960-894X
    Database AGRIS - International Information System for the Agricultural Sciences and Technology

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