Search Results - "Fryer, Andrew M"
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Discovery of (1S,2R,3R)-2,3-Dimethyl-2-phenyl-1-sulfamidocyclopropanecarboxylates: Novel and Highly Selective Aggrecanase Inhibitors
Published in Journal of medicinal chemistry (28-04-2011)“…Aggrecanases, particularly aggrecanase-1 (ADAMTS-4) and aggrecanase-2 (ADAMTS-5), are believed to be key enzymes involved in the articular cartilage breakdown…”
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2
A New Resin-Bound Universal Isonitrile for the Ugi 4CC Reaction: Preparation and Applications to the Synthesis of 2,5-Diketopiperazines and 1,4-Benzodiazepine-2,5-diones
Published in Organic letters (04-04-2002)“…The preparation and synthetic applications of a novel resin-bound isonitrile are described. The resin is an example of a novel convertible isonitrile that can…”
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3
Applications of Vinylogous Mannich Reactions. Total Syntheses of the Ergot Alkaloids Rugulovasines A and B and Setoclavine
Published in Journal of the American Chemical Society (27-06-2001)“…Concise syntheses of the Ergot alkaloids rugulovasine A (3a), rugulovasine B (3b), and setoclavine (2) have been completed by strategies that feature inter-…”
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4
Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors
Published in Bioorganic & medicinal chemistry letters (15-03-2009)“…A series of N-substituted sulfonylamino-alkanecarboxylate ADAMTS-5 (Aggrecanase-2) inhibitors has been synthesized and the in vitro enzyme SAR is discussed…”
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5
Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-11-2009)“…A series of 1-sulfonylaminocyclopropanecarboxylates was synthesized as ADAMTS-5 (Aggrecanase-2) inhibitors. After an intensive investigation of the central…”
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Parallel Synthesis of Novel Heteroaromatic Acromelic Acid Analogues from Kainic Acid
Published in Journal of organic chemistry (20-04-2001)“…A range of new C-4 heteroaromatic acromelic acid analogues has been synthesized in a parallel fashion from (−)-α-kainic acid 1. Protection of the amine and…”
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Towards a versatile synthesis of kainoids I: Introduction of the C-3 and C-4 substituents
Published in Tetrahedron (01-04-1997)“…The first stages in the synthesis of acromelic acid analogues from trans-4-hydroxy- L -proline are described. An enamine alkylation was used to…”
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8
1H NMR Study of Protected and Unprotected Kainoid Amino Acids: Facile Assignment of C-4 Stereochemistry
Published in Journal of organic chemistry (20-04-2001)“…The kainoid amino acids exhibit potent neuroexcitatory activity in the mammalian central nervous system. Around their pyrrolidine ring, a trans disposition…”
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A biomimetic approach to the pyridone rings of the acromelic acids: A concise synthesis of acromelic acid A and an approach to acromelic acid B
Published in Tetrahedron (25-06-1998)“…The syntheses of acromelic acid A 1, allo-acromelic acid A 19 and an approach towards acromelic acid B 2 are described. Palladium (0) catalysed cross-coupling…”
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Towards a versatile synthesis of kainoids II: Two methods for establishment of C-4 stereochemistry
Published in Tetrahedron (01-04-1997)“…Benzylic lactone hydrogenolysis and enamide reduction were used to generate protected C-4 aryl substituted kainoid analogues which were deprotected to their…”
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11
Concise syntheses of acromelic acid A and allo-acromelic acid A
Published in Tetrahedron letters (12-02-1998)“…Acromelic acid A 1 and allo-acromelic acid A 12 were synthesised in a biomimetic fashion. An oxidative cleavage - recyclisation strategy was used to construct…”
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Stereocontrol in the synthesis of kainoids
Published in Tetrahedron letters (16-09-1996)“…A stereoselective synthesis of acromelic acid analogues is described in which the C-3 C-4 cis-relative stereochemistry is established by a hydroxyl directed…”
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13
1 H NMR Study of Protected and Unprotected Kainoid Amino Acids: Facile Assignment of C-4 Stereochemistry
Published in Journal of organic chemistry (01-04-2001)Get full text
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14
Novel C-4 heteroaromatic kainoid analogues : A parallel synthesis approach
Published in Bioorganic & medicinal chemistry letters (07-02-2000)“…New C-4 thiazole 4, 5 and aminothiazole 6, 7 kainoid analogues were efficiently synthesised in five steps from commercially available (-)-alpha-kainic acid I…”
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Towards a versatile synthesis of kainoids III: Efficient methods for control of C-4 stereochemistry
Published in Tetrahedron (07-04-1997)“…Halo- and selenolactonisation methods were used to prepare benzylic lactones from enamide carboxylic acids. The lactones were subsequently cleaved with…”
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16
A Versatile Approach to Acromelic Acid Analogues
Published in Tetrahedron letters (03-07-1995)Get full text
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A versatile approach to acromelic acid analogues
Published in Tetrahedron letters (1995)“…A route to acromelic acid analogues and their corresponding C-4 epimers from trans-4-hydroxy- L -proline is described. The C-4 substituent was introduced by a…”
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