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Research focus:  

C3-Prof. f. Pharm. Chemie (Schirmeister)
Institut für Pharmazie und LM-Chemie Am Hubland, 97074 Würzburg
Mail: schirmei@pharmazie.uni-wuerzburg.de
Url: http://www.pharmazie.uni-wuerzburg.de/PharmChem/AKSchirmei/index.html

Scientific members:

   Professors:

   Scientific assistants:

Research foci (and basic equipment-based research projects):
Development of peptidic and peptidomimetic cysteine protease inhibitors containing aziridine-2,3-dicarboxylic acid as electrophilic building block (Vicik, Breuning)
Development of peptidic cysteine protease inhibitors containing thiiran-2-carboxylic acid (Bruno)
Development of peptidic cysteine protease inhibitors containing aziridine-2,2-dicarboxylic acid (Jenke)
Reactivity of aziridine-2,2-dicarboxylates against nucleophiles (Nahum)

Results:
Publications:

Aziridine-2,3-dicarboxylic acid derivatives as inhibitors of papain,
T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 1996, 329, 239-244.

Aziridine-2,2-dicarboxylates: synthesis, reactions, photochromism,
T. Schirmeister, Liebigs Ann./Recueil 1997, 1895-1899.

Cysteine proteases and their inhibitors,
H.-H. Otto, T. Schirmeister, Chem. Rev. 1997, 97, 133-171.

Synthesis of peptides with aziridine-2,3-dicarboxylic acid as an -amino acid equivalent building block,
T. Schirmeister, Peptide Science - Present and Future 1998, 654-656.

Metall-Ionen als Co-Inhibitoren von Serin-Proteasen: Ein neuer Ansatz bei der Suche nach hochaffinen und spezifischen Liganden,
T. Schirmeister, Angew. Chem. 1998, 110, 1930-1932.

New peptidic cysteine protease inhibitors derived from the electrophilic -amino acid aziridine-2,3-dicarboxylic acid,
T. Schirmeister, J. Med. Chem. 1999, 42, 560-572.

Inhibition of cysteine proteases by peptides containing aziridine-2,3-dicarboxylic acid building blocks,
T. Schirmeister, Biopolymers (Peptide Science) 1999, 51, 87-97.

Aziridinyl peptides as inhibitors of cysteine proteases: Effect of a free carboxylic acid function on inhibition,
T. Schirmeister, M. Peric, Bioorg. Med. Chem. 2000, 8, 1281-1291.

ß-Lactam derivatives as enzyme inhibitors: N-Substituted derivatives of (S)-4-oxoazetidine-2-carboxylate as inhibitors of elastase and papain,
K. Achilles, M. Schneider, T. Schirmeister, H.-H. Otto, Pharmazie 2000, 55, 798-802.

ß-Lactam derivatives as enzyme inhibitors: 1-Peptidyl derivatives of 4-phenylazetidin-2-one as inhibitors of elastase and papain,
K. Achilles, T. Schirmeister, H.-H. Otto, Arch. Pharm. Pharm. Med. Chem. 2000, 333, 243-253.

(S)-Thiirancarboxylic acid as a reactive building block for a new class of cysteine protease inhibitors,
T. Schirmeister, Bioorg. Med. Chem. Lett. 2000, 10, 2647-2651.

Non-peptidic inhibitors of cysteine proteases,
T. Schirmeister, U. Käppler, Mini Rev. Med. Chem. 2003, im Druck

Cysteine protease inhibitors containing small rings,
T. Schirmeister, A. Klockow, Mini Rev. Med. Chem. 2003, im Druck.

Thiirancarboxamides as a new class oc cysteine protease inhibitors,
G. Bruno, T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 2002, 335, Suppl. 1, 76.

Ex-chiral-pool synthesis of aziridine-2,3-dicarboxylates,
A. Breuning, T. Schirmeister, Arch. Pharm. Pharm. Med. Chem. 2002, 335, Suppl. 1, 76.

Non-peptidic inhibitors of cysteine proteases,
U. Käppler, T. Schirmeister, . Arch. Pharm. Pharm. Med. Chem. 2002, 335, Suppl. 1, 86.

Peptidomimetic inhibitors of cysteine proteases,
R. Vicik, T. Schirmeister. Arch. Pharm. Pharm. Med. Chem. 2002, 335, Suppl. 1, 102.

Improved stereoselective synthesis of aziridine-2,3-dicarboxylates,
A. Breuning, R. Vicik, T. Schirmeister, Synthesis, in Vorbereitung.

Thiirancarboxamides as inhibitors of papain,
G. Bruno, T. Schirmeister, Bioorg Med Chem, eingereicht.

Peptidomimetic cysteine protease inhibitors containing aziridine-2,3-dicarboxylic acid as electrophilic building block,
R. Vicik, T. Schirmeister, Bioorg. Med. Chem., in Vorbereitung.

Posters:

Irreversible peptidomimetic inhibitors of cysteine proteases,
R. Vicik, T. Schirmeister, Jahrestagung der GDCh, 2001, Würzburg.

A. Breuning, R. Vicik, T. Schirmeister; Inhibitors of cysteine proteases containing an aziridine unit. Abstract in: Drugs Fut. 2002, 27 (Suppl. A), 444, XVIIth International Symposium on Medicinal Chemistry of the EFMC European Federation of Medicinal Chemistry, Barcelona, 2002

G. Bruno, T. Schirmeister; Thiirancarboxylic acid as electrophilic building block for new cysteine protease inhibitors. Abstract in: Drugs Fut. 2002, 27 (Suppl. A), 443, XVIIth International Symposium on Medicinal Chemistry of the EFMC European Federation of Medicinal Chemistry Barcelona, 2002.

G. Bruno, T. Schirmeister, Thiirancarboxamides as a new class oc cysteine protease inhibitors. DPhG-Jahrestagung 2002, Berlin.

A. Breuning, T. Schirmeister, Ex-chiral-pool synthesis of aziridine-2,3-dicarboxylates. DPhG-Jahrestagung 2002, Berlin.

U. Käppler, T. Schirmeister, Non-peptidic inhibitors of cysteine proteases. DPhG-Jahrestagung 2002, Berlin.

R. Vicik, T. Schirmeister, Peptidomimetic inhibitors of cysteine proteases. DPhG-Jahrestagung 2002, Berlin.