Olaf Kinzel
United States Military Academy
11 Papers
113 Citations
Olaf Kinzel is an academic researcher from United States Military Academy. The author has contributed to research in topics: Cancer & Isomerization. The author has an hindex of 6, co-authored 11 publications.
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Papers
Discovery of Raltegravir, a Potent, Selective Orally Bioavailable HIV-Integrase Inhibitor for the Treatment of HIV-AIDS Infection
Vincenzo Summa,Alessia Petrocchi,Fabio Bonelli,Benedetta Crescenzi,Monica Donghi,Marco Ferrara,Fabrizio Fiore,Cristina Gardelli,Odalys Gonzalez Paz,Daria J. Hazuda,Philip Jones,Olaf Kinzel,Ralph Laufer,Edith Monteagudo,Ester Muraglia,Emanuela Nizi,Federica Orvieto,Paola Pace,Giovanna Pescatore,Rita Scarpelli,Kara A. Stillmock,Marc V. Witmer,Michael Rowley +22 more
TL;DR: The discovery of Raltegravir is reported, the first HIV-integrase inhibitor approved by FDA for the treatment of HIV infection, which derives from the evolution of 5,6-dihydroxypyrimidine-4-carboxamides and N-methyl- 4-hydroxypyridinone-car boxamides, which exhibited potent inhibition of the HIV-Integrase catalyzed strand transfer process.
669
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Ester Muraglia,Olaf Kinzel,Cristina Gardelli,Benedetta Crescenzi,Monica Donghi,Marco Ferrara,Emanuela Nizi,Federica Orvieto,Giovanna Pescatore,Ralph Laufer,Odalys Gonzalez-Paz,Annalise Di Marco,Fabrizio Fiore,Edith Monteagudo,Massimiliano Fonsi,Peter J. Felock,Michael Rowley,Vincenzo Summa +17 more
TL;DR: The evolution from the N-methylpyridinone structure to bicyclic pyrimidinones is shown and introduction of a suitably substituted amino moiety modulated the physical-chemical properties of the molecules and conferred nanomolar activity in the inhibition of spread of HIV-1 infection in cell culture.
54
Patent
Pyrrolo[1,2-a]pyrazin-1(2h)-one and pyrrolo[1,2-d][1,2,4]triazin-1(2h)-one derivatives as inhibitors of poly(adp-ribose)polymerase(parp)
Philip Jones,Olaf Kinzel,Bufi Laura Llauger,Ester Muraglia,Giovanna Pescatore,Caterina Torrisi +5 more
- 29 May 2007
TL;DR: The present paper relates to compounds of formula I: and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP- ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischaemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular disease, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage as mentioned in this paper.
20
A novel base-mediated intramolecular hydroamination to build fused heteroaryl pyrazinones
Laura Llauger,Costanza Bergami,Olaf Kinzel,Samuele Lillini,Giovanna Pescatore,Caterina Torrisi,Philip Jones +6 more
TL;DR: In this paper, a functionalized fused heteroaryl pyrazinones were built up through a novel DBU-catalyzed intramolecular hydroamination reaction of aryl(prop-2-yn-1-yl)-1 H -heteroaryl-2 carboxamides.
15
3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates—fast access to a heterocyclic scaffold for HIV-1 integrase inhibitors
Olaf Kinzel,Richard G. Ball,Monica Donghi,Courtney K. Maguire,Ester Muraglia,Silvia Pesci,Michael Rowley,Vincenzo Summa +7 more
TL;DR: An efficient and reliable synthesis of the heterocyclic scaffold methyl-3-hydroxy-4-oxo-4 H -pyrido[1,2- a ]pyrimidine-2-carboxylate is described.
14