Výsledky vyhledávání - "Kirkup, Michael P"

(−)-SCH 57939: synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor

Autor: Kirkup Michael P, Bandarpalle B. Shankar, John W. Clader, Keith Huie, Sue-Ing Lin, Harry R. Davis, Douglas S Compton, Stuart W. McCombie, Andrew T. McPhail, Margaret van Heek, Yumibe Nathan P, Razia Rizvi, Sundeep Dugar

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 6:2069-2072

Previous SAR studies of C-3 side chain modified analogs of (−)-SCH 48461, 1,3,4 as well as information concerning the metabolic stability this series, enabled us to design a cholesterol absorption inhibitor (i.e., (−) 2a, SCH 57939) with tenfold

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e1110e2e0b2531fce1b60f72f94d4e12
https://doi.org/10.1016/0960-894x(96)00365-4

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Synthesis of an optically pure 3-unsubstituted β-lactam using an asymmetric Reformatsky reaction and its conversion to cholesterol absorption inhibitors

Autor: Ashit K. Ganguly, Stuart W. McCombie, Kirkup Michael P, John W. Clader, Bandarpalle B. Shankar

Publikováno v: Tetrahedron Letters. 37:4095-4098

Asymmetric induction by several chiral alcohols in the reaction of their bromoaceates with imines in the presence of activated Zn (Reformatsky reaction) was studied. Trans -2-phenylcyclohexanol and phenyl menthol gave β-lactam 9 , obtained by cycliz

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ed96a0211903eb9cba015891fedc0674
https://doi.org/10.1016/0040-4039(96)00764-2

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Gamma-lactams and related compounds as cholesterol absorption inhibitors: homologs of the beta-lactam cholesterol absorption inhibitor SCH 484611

Autor: Mark E. Snow, Sue-Ing Lin, Stuart W. McCombie, Harry R. Davis, Sundeep Dugar, Kirkup Michael P, John W. Clader, Razia Rizvi

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 5:2947-2952

Our search for potent cholesterol absorption inhibitors led to the discovery of the β-lactam SCH 48461. Structure activity relationship studies prompted us to this study of γ-lactams, ring homologs of β-lactam SCH 48461, to determine their potenti

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b99ff499e3f36aa5927d24f3b12e1363
https://doi.org/10.1016/0960-894x(95)00516-6

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Indolocarbazoles.3. Synthesis of novel aza analogs of staurosporine and K 252a as PKC inhibitors

Autor: Razia Rizvi, A. Q. Viet, Stuart W. McCombie, B. B. Shankar, Kirkup Michael P, Ashit K. Ganguly

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 4:495-498

Indolocarbazole 4 and arcyriaflavin A 19 reacted under basic conditions with 1-benzyl-2,6-bis (benzotriazolyl)-piperidine to give 5 and 20 . As an extension of this methodology other related bis benzotriazole derivatives were synthesized and coupled

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::81984a70eb01996750b0d08be026b58f
https://doi.org/10.1016/0960-894x(94)80024-3

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A novel application of 'benzotriazole' methodology : Reactions of polyhydroxylated bis-(benzotriazolyl) piperidines with mono- and bidentate nucleophiles

Autor: Ashit K. Ganguly, Stuart W. McCombie, Kirkup Michael P, Bandarpalle B. Shankar

Publikováno v: Tetrahedron Letters. 34:7171-7174

A variety of 2,6 substituted trihydroxy piperidines 4 was synthesized with stereocontrol from the corresponding 2,6 bis-(Benzotriazolyl) trihydroxy piperidine 9 , which in turn was prepared from 1,2-O-isopropylidene-D-glucofuranose 5 employing a simp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::34ee82bd9d306bd2679f04d82e10a06b
https://doi.org/10.1016/s0040-4039(00)79279-3

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Indolocarbazoles. 2. Synthetic studies towards staurosporine. An unexpected 1,2 migration of indolocarbazole nitrogen results in a novel and potent Protein kinase C inhibitor

Autor: Stuart W. McCombie, B. B. Shankar, Ashit K. Ganguly, M. S. Puar, Kirkup Michael P, A. Q. Viet

Publikováno v: Tetrahedron Letters. 34:5685-5688

Attempted transformation of the readily accessible cyclofuransylated indolocarbazole (4) to a cyclopyranosylated compound related to 1 was explored. An unexpected rearranged product (10) was obtained from (9). Compound (10) was converted to (14), a p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3e1010c126284defee78fc58ceabde34
https://doi.org/10.1016/s0040-4039(00)73833-0

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Indolocarbazoles. 1. Total synthesis and protein kinase inhibiting characteristics of compounds related to K-252c

Autor: Stuart W. McCombie, Oswald Wilson, Kirkup Michael P, Karen Rosinski, Sue-Ing Lin, Robert Bishop, Bandarpalle B. Shankar, Paul Kirschmeier, Emily Dobek, Joanne M. Petrin, Donna Carr

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 3:1537-1542

The condensation of indolo[2,3-a]-carbazole (12) with 2,5-dimethoxytetrahydrofuran derivatives gave cyclofuranosylated compounds (e.g. 13), which were converted via dibromocompounds to the dinitriles (e.g. 25). Hydrolysis, hydrolysis-reduction and th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::939084d47bf3f57a87b0aac1ea2e9285
https://doi.org/10.1016/s0960-894x(00)80013-x

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