Hauptinhalt

Ausgewählte Publikationen

Wirkstoffe gegen Schistosomiasis

P. Mäder, G. A. Rennar, A. M. P. Ventura, C. G. Grevelding, M. Schlitzer, Chemotherapy for Fighting Schistosomiasis: Past, Present and Future, ChemMedChem, 2018, Accepted Article, DOI: 10.1002/cmdc.201800572.

P. Maeder, A. S. Blohm, T. Quack, K. Lange-Gruenweller, A. Gruenweller, R. K. Hartmann, C. G. Grevelding, M. Schlitzer, Biarylalkyl Carboxylic Acid Derivatives as Novel Antischistosomal Agents, ChemMedChem, 2016, 11(13), 1459-1468, DOI: 10.1002/cmdc.201600127.

A. S. Blohm, T. Quack, Z. Lu, S. Hahnel, C. G. Grevelding, P. Mader, M. Schlitzer, Derivatives of biarylalkyl carboxylic acid induce pleiotropic phenotypes in adult Schistosoma mansoni in vitro, Parasitology research, 2016, 115(10), 3831-3842, DOI: 10.1007/s00436-016-5146-7.

DOXP-Reduktoisomerase-Inhibitoren

J. Wiesner, C. Ziemann, M. Hintz, A. Reichenberg, R. Ortmann, M. Schlitzer, R. Fuhst, N. Timmesfeld, A. Vilcinskas, H. Jomaa, FR-900098, an antimalarial development candidate that inhibits the non-mevalonate isoprenoid biosynthesis pathway, shows no evidence of acute toxicity and genotoxicity, Virulence, 2016, 7(6), 718-728.

A.-S. Messiaen, T. Verbrugghen, C. Declerck, R. Ortmann, M. Schlitzer, H. Nelis, S. Van Calenbergh, T. Coenye, Resistance of the Burkholderia cepacia complex to fosmidomycin and fosmidomycin derivatives, International Journal of Antimicrobial Agents, 2011, 38(3), 261-264.

J. Perruchon, R. Ortmann, M. Altenkämper, K. Silber, J. Wiesner, H. Jomaa, G. Klebe, M. Schlitzer, Studies addressing the importance of charge in the binding of fosmidomycin-like molecules to deoxyxylulosephosphate reductoisomerase, ChemMedChem, 2008, 3, 1232-41.

T. Haemers, J. Wiesner, D. Giessmann, T. Verbrugghen, U. Hillaert, R. Ortmann, H. Jomaa, A. Link, M. Schlitzer, S. Van Calenbergh, Synthesis of beta- and gamma-oxa isosteres of fosmidomycin and FR900098 as antimalarial candidates, Bioorg Med Chem, 2008, 16, 3361-3371.

J. Wiesner, R. Ortmann, H. Jomaa, M. Schlitzer, Double ester prodrugs of FR900098 display enhanced in-vitro antimalarial activity, Arch Pharm (Weinheim), 2007, 340, 667-669.

R. Ortmann, J. Wiesner, K. Silber, G. Klebe, H. Jomaa, M. Schlitzer, Novel deoxyxylulosephosphate-reductoisomerase inhibitors: fosmidomycin derivatives with spacious acyl residues, Arch Pharm (Weinheim), 2007, 340, 483-490.

J. Perruchon, R. Ortmann, M. Schlitzer, A Novel Short and Efficient Synthetic Route to the Antimalarial Agent FR900098 and Derivatives, Synthesis, 2007, 22, 3553-3557.

R. Ortmann, J. Wiesner, A. Reichenberg, D. Henschker, E. Beck, H. Jomaa, M. Schlitzer, Alkoxycarbonyloxyethyl ester prodrugs of FR900098 with improved in vivo antimalarial activity, Arch Pharm (Weinheim), 2005, 338, 305.

R. Ortmann, J. Wiesner, A. Reichenberg, D. Henschker, E. Beck, H. Jomaa, M. Schlitzer, Acyloxyalkyl Ester Prodrugs of FR900098 with improved in vivo Antimalarial Activity, Bioorg. Med. Chem. Lett. 2003, 13, 2163-2166.

A. Reichenberg, J. Wiesner, C. Weidemeyer, E. Dreiseidler, S. Sanderbrand, B. Altincicek, E. Beck, M. Schlitzer, H. Jomaa, Diaryl Ester Prodrugs of FR900098 with Improved in-vivo Antimalarial Activity, Bioorg. Med. Chem. Lett. 2001, 11, 833-835.

Neuroprotektiva

S. Oppermann, F. C. Schrader, K. Elsaesser, A. M. Dolga, A. L. Kraus, N. Doti, C. Wegscheid-Gerlach, M. Schlitzer, C. Culmsee, Novel N-phenyl-substituted thiazolidinediones protect neural cells against glutamate- and tBid-induced toxicity, Journal of Pharmacology and Experimental Therapeutics, 2014, 350(2), 273-289.

M. T. Barho, S. Oppermann, F. C. Schrader, I. Degenhardt, K. Elsaesser, C. Wegscheid-Gerlach, C. Culmsee, M. Schlitzer, N-Acyl Derivatives of 4-Phenoxyaniline as Neuroprotective Agents, ChemMedChem, 2014, 9(10), 2260-2273.

Benzophenone als Antimalaria-Wirkstoffe

S. Heinrich, M. Altenkaemper, B. Bechem, J. Perruchon, R. Ortmann, H.-M. Dahse, Y. Wang, M. Lanzer, M. Schlitzer, 2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites, European Journal of Medicinal Chemistry, 2011, 46(4), 1331-1342.

M. Altenkaemper, B. Bechem, J. Perruchon, S. Heinrich, A. Maedel, R. Ortmann, H.-M. Dahse, E. Freunscht, Y. Wang, J. Rath, A. Stich, M. Hitzler, P. Chiba, M. Lanzer, M. Schlitzer, Antimalarial and antitrypanosomal activity of a series of amide and sulfonamide derivatives of a 2,5-diaminobenzophenone, Bioorganic & Medicinal Chemistry, 2009, 17(22), 7690-7697.

J. Wiesner, K. Kettler, J. Sakowski, R. Ortmann, H. Jomaa, M. Schlitzer, Structure-Activity Relationships of Novel Anti-Malarial Agents: 5. N-(4-Acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic Acid Amides, Bioorg. Med. Chem. Lett. 2003, 13, 361-363.

J. Wiesner, K. Fucik, K. Kettler, J. Sakowski, R. Ortmann, H. Jomaa, M. Schlitzer, Structure-Activity Relationships of Novel Anti-Malarial Agents: 6. N-(4-Arylpropionylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic Acid Amides, Bioorg. Med. Chem. Lett. 2003, 13, 1539-1541.

J. Wiesner, A. Mitsch, H. Jomaa, M. Schlitzer, Structure-Activity Relationships of Novel Anti-Malarial Agents: 7. N -(3-Benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic Acid Amides with Polar Moieties, Bioorg. Med. Chem. Lett. 2003, 13, 2159-2161.

J. Wiesner, A. Mitsch, M. Altenkämper, R. Ortmann, H. Jomaa, M. Schlitzer, Structure-Activity Relationships of Novel Anti-Malarial Agents: 8. Effect of Different Central Aryls in Biarylacryloylaminobenzophenones on Antimalarial Activity, Die Pharmazie 2003, 58, 854 – 856.

J. Wiesner, K. Kettler, H. Jomaa, M. Schlitzer, Structure-Activity Relationships of Novel Anti-Malarial Agents: 3. N-(4-Acylamino-3-benzoylphenyl)-4-propoxycinnamic Acid Amides, Bioorg. Med. Chem. Lett. 2002, 12, 543-545.

J. Wiesner, A. Mitsch, P. Wißner, O. Krämer, H. Jomaa, M. Schlitzer, Structure-Activity Relationships of Noval Anti-Malaria Agents. Part 4: N-(3-Benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic Acid Amides, Bioorg. Med. Chem. Lett. 2002, 12, 2681-2683.

J. Wiesner, P. Wißner, H.-M. Dahse, H. Jomaa, M. Schlitzer, Discovery of a Novel Lead Structure for Anti-Malarials, Bioorg. Med. Chem. 2001, 9, 785-792.

J. Wiesner, A. Mitsch, P. Wißner, H. Jomaa, M. Schlitzer, Structure-activity relationships of novel anti-malarial agents: 1. arylacyl and cyclohexylacyl derivatives of 5-amino-2-tolylacetylaminobenzophenone, Die Pharmazie 2001, 56, 443-444.

J. Wiesner, A. Mitsch, P. Wißner, H. Jomaa, M. Schlitzer, Structure-Activity Relationships of Novel Anti-Malarial Agents: 2. Cinnamic Acid Derivatives, Bioorg. Med. Chem. Lett., 2001, 11, 423-424.

Aldosereduktase-Inhibitoren

M. Eisenmann, H. Steuber, M. Zentgraf, M. Altenkaemper, R. Ortmann, J. Perruchon, G. Klebe, M. Schlitzer, Structure-based optimization of aldose reductase inhibitors originating from virtual screening, ChemMedChem, 2009, 4(5), 809-819.

M. Schlitzer, L. Rodriguez, P. F. Kador, Synthesis of Potential Aldose Reductase Inhibitors Based on Minimal Pharmacophore Requirements, Pharm. Pharmacol. 2001, 53, 831 - 839.

Farnesyltransferase-Inhibitoren

K. Kohring, J. Wiesner, M. Altenkämper, J. Sakowski, K. Silber, A. Hillebrecht, P. Haebel, H. M. Dahse, R. Ortmann, H. Jomaa, G. Klebe, M. Schlitzer, Development of benzophenone-based farnesyltransferase inhibitors as novel antimalarials, ChemMedChem, 2008, 3, 1217-1231.

K. Kettler, J. Wiesner, R. Ortmann, H. M. Dahse, H. Jomaa, M. Schlitzer, Antimalarial activity of methylpiperazinyl-substituted benzophenone-based farnesyltransferase inhibitors, Pharmazie, 2006, 61, 63-65.

M. I. Esteva, K. Kettler, C. Maidana, L. Fichera, A. M. Ruiz, E. J. Bontempi, B. Andersson, H. M. Dahse, P. Haebel, R. Ortmann, G. Klebe, M. Schlitzer, Benzophenone-based farnesyltransferase inhibitors with high activity against Trypanosoma cruzi, J Med Chem, 2005, 48, 7186-7191.

K. Kettler, J. Sakowski, J. Wiesner, R. Ortmann, H. Jomaa, M. Schlitzer, Novel lead structures for antimalarial farnesyltransferase inhibitors, Pharmazie, 2005, 60, 323-327.

K. Kettler, J. Wiesner, K. Fucik, J. Sakowski, R. Ortmann, H. M. Dahse, H. Jomaa, M. Schlitzer, 2-(aminoacylamino)-benzophenones: farnesyltransferase inhibition and antimalarial activity, Pharmazie, 2005, 60, 677-682.

K. Kettler, J. Wiesner, K. Silber, P. Haebel, R. Ortmann, I. Sattler, H. M. Dahse, H. Jomaa, G. Klebe, M. Schlitzer, Non-thiol farnesyltransferase inhibitors: N-(4-aminoacylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2 furyl]acrylic acid amides and their antimalarial activity, Eur J Med Chem, 2005, 40, 93-101.

A. Mitsch, M. Altenkämper, I. Sattler, M. Schlitzer, Non-thiol farnesyltransferase inhibitors: utilization of the far aryl binding site by arylthienylacryloylaminobenzophenones, Arch Pharm (Weinheim), 2005, 338, 9-17.

J. Wiesner, K. Kettler, J. Sakowski, R. Ortmann, A. M. Katzin, E. A. Kimura, K. Silber, G. Klebe, H. Jomaa, M. Schlitzer, Farnesyltransferase-Inhibitoren hemmen das Wachstum von Malaria-Erregern in vitro und in vivo, Angewandte Chemie 2004 , 116 , 254 - 257; Angewandte Chemie Int. Ed. 2004, 43, 251 - 254.

A. Mitsch, M. Böhm, I. Sattler, M. Schlitzer, Non-thiol farnesyltransferase inhibitors: utilization of the near aryl binding site by 5-arylacetylaminobenzophenones, Arch. Pharm. (Weinheim), 2004, 337, 213-218.

A. Mitsch, P. Wissner, M. Böhm, K. Silber, G. Klebe, I. Sattler, M. Schlitzer, Non-thiol farnesyltransferase inhibitors: utilization of the far aryl binding site by 5-cinnamoylaminobenzophenones, Arch Pharm (Weinheim), 2004, 337, 493-501.

A. Mitsch, P. Wissner, K. Silber, P. Haebel, I. Sattler, G. Klebe, M. Schlitzer, Non-thiol farnesyltransferase inhibitors: N-(4-tolylacetylamino-3-benzoylphenyl)-3-arylfurylacrylic acid amides, Bioorg Med Chem, 2004, 12, 4585-4600.

J. Wiesner, R. Ortmann, A. Mitsch, P. Wißner, I. Sattler, H. Jomaa, M. Schlitzer, Farnesyltransferase-Inhibitors: 5-Arylacryloylaminobenzophenones show Anti-Malarial Activity, Die Pharmazie 2003, 58, 289-290.

A. Mitsch, S. Bergmann, R. Gust, I. Sattler, M. Schlitzer, Non-Thiol Farnesyltransferase Inhibitors: FTase-Inhibition and Cellular Activity of Benzophenone-based Bisubstrate Analogue Farnesyltransferase Inhibitors, Arch. Pharm. Pharm. Med. Chem. 2003, 336, 242-250.

J. Sakowski, I. Sattler, M. Schlitzer, Non-Thiol Farnesyltransferase Inhibitors: N-(4-Acylamino-3-benzoylphenyl)-4-nitrocinnamic Acid Amides, Bioorg. Med. Chem. 2002, 10, 233-239.

J. Sakowski, M. Böhm, I. Sattler, M. Schlitzer, Non-Thiol Farnesyltransferase Inhibitors: Evaluatiuon of Different AA(X)-Peptidomimetic Substructures in Combination with Arylic Cysteine Replacements, Arch. Pharm. Pharm. Med. Chem. 2002, 335, 135-142.

M. Schlitzer, M. Böhm, I. Sattler, Non-Thiol Farnesyltransferase Inhibitors: Structure-Activity Relationships of Benzophenone-Based Bisubstrate Analog Farnesyltransferase Inhibitors, Bioorg. Med. Chem. 2002, 10, 615-620.

A. Mitsch, M. Böhm, P. Wißner, I. Sattler, M. Schlitzer, Non-Thiol Farnesyltransferase Inhibitors: Utilization of an Aryl Binding Site by 5-Arylacryloylaminobenzophenones, Bioorg. Med. Chem. 2002, 10, 2657-2662.

M. Schlitzer, Structure Based Design of Benzophenone-Based Non-Thiol Farnesyltransferase Inhibitors, Curr. Pharm. Design 2002, 8, 1713-1722.

M. Schlitzer, A. Winter-Vann, P. J. Casey, Non-Peptidic, Non-Prenylic Inhibitors of the Prenyl Protein-Specific Protease Rce1, Bioorg. Med. Chem. Lett. 2001, 11, 425-427.

A. Mitsch, P. Wißner, I. Sattler, M. Schlitzer, Non-Thiol Farnesyltransferase Inhibitors: Structure-Activity Relationships of Aralkylsubsituted Benzophenones, Arch. Pharm. Pharm. Med. Chem. 2001, 334, 40-44.

J. Sakowski, M. Böhm, I. Sattler, H.-M. Dahse, M. Schlitzer, Synthesis, Molecular Modeling and Structure Activity Relationship of Benzophenone-Based CAAX-Peptidomimetic Farnesyltransferase Inhibitors, J. Med. Chem. 2001, 44, 2886-2899.

M. Böhm, A. Mitsch, P. Wißner, I. Sattler, M. Schlitzer, Exploration of Novel Aryl Binding Sites of Farnesyltransferase Using Molecular Modeling and Benzophenone-Based Farnesyltransferase Inhibitors, J. Med. Chem. 2001, 44, 3117-3124.

M. Schlitzer, M. Böhm, I. Sattler, H.-M. Dahse, Design, Synthesis and Early Structure-Activity Relationship of Farnesyltransferase Inhibitors which Mimic Both the Peptidic and the Prenylic Substrate, Bioorg. Med. Chem. 2000, 8, 1991-2006.

M. Schlitzer, M. Böhm, I. Sattler, Non-Peptidic, Non-Prenylic Bisubstrate Farnesyltransferase Inhibitors 3. Structural Requirements of the Central Moiety for Farnesyltransferase Inhibitory Activity, Bioorg. Med. Chem. 2000, 8,
2399- 2406.

M. Schlitzer, I. Sattler, Non-Peptidic, Non-Prenylic Bisubstrate Farnesyltransferase Inhibitors 4. Effect on Farnesyltransferase Inhibitory Activity of Conformational Restrictions in the Central Group, Pharm. Pharmacol. Commun. 2000, 5, 117-124.

M. Schlitzer, I. Sattler, Non-Peptidic, Non-Prenylic Bisubstrate Farnesyltransferase Inhibitors 5. Effect on Farnesyltransferase Inhibitory Activity of a Carboxyl Group at the Central Group, Pharm. Pharmacol. Commun. 2000, 5, 507-512.

M. Schlitzer, I. Sattler, Non-Thiol Farnesyltransferase Inhibitors: the concept of benzophenone-based bisubstrate analog farnesyltransferase inhibitors, Eur. J. Med. Chem. 2000, 35, 721-726.

Verschiedenes

F. C. Schrader, S. Glinca, J. M. Sattler, H.-M. Dahse, G. A. Afanador, S. T. Prigge, M. Lanzer, A.-K. Mueller, G. Klebe, M. Schlitzer, Novel Type II Fatty Acid Biosynthesis (FAS II) Inhibitors as Multistage Antimalarial Agents, ChemMedChem, 2013, 8(3), 442-461.

R. Ortmann, M. Schlitzer, An inexpensive procedure for reductive aminations using dimethylamineborane on millimolar and molar scale, Synthesis, 2009, 10, 1757-1759.

D. Barthel, M. Schlitzer, G. Pradel, Telithromycin and quinupristin-dalfopristin induce delayed death in Plasmodium falciparum, Antimicrobial Agents and Chemotherapy, 2008, 52(2), 774-777.

P. Wißner, H.-M. Dahse, M. Schlitzer, Structure activity relationship of antiproliferative N-acyl-aspartic acid dimethyl ester. 2. Variation of the aspartyl moiety, Die Pharmazie 2001, 56, 33-35.

M. Schlitzer, I. Sattler, A. Friese, I. Zündorf, T. Dingermann, Synthesis of 4-(Acylaminomethyl)-benzamides and their Evaluation as Potential Anti-Cancer, Agents Anticancer Res. 2000, 20, 1723-1726.

M. Schlitzer, H.-M. Dahse, Structure Activity Relationship of Antiproliferative N-Acyl-ß-Alanine Amides, Anticancer Res. 2000, 20, 4431-4434.

Übersichtsartikel

F. C. Schrader, M. Barho, I. Steiner, R. Ortmann, M. Schlitzer, The antimalarial pipeline-an update, International journal of medical microbiology, 2012, 302(4-5), 165-71

D. Weeken, M. Schlitzer, Accidental discoveries, different mechanisms of action. Active agents against Mycobacterium tuberculosis in clinical application, Pharmazie in unserer Zeit, 2012, 41(1), 35-47

A. Stich, M. Schlitzer, African sleeping sickness and the drugs for its therapy, Chemotherapie Journal, 2011, 20(4), 115-125.

G. Klebe, M. Schlitzer, Agents against the flu: M2-inhibitors and neuraminidase inhibitors, Pharmazie in Unserer Zeit, 2011, 40(2), 144-150.

M. Schlitzer, New malaria drugs: screening against the entire parasite or target-based - which is the right path?, Pharmazie in unserer Zeit, 2011, 40(3), 190-191.

M. Schlitzer, R. Ortmann, Feeding the Antimalarial Pipeline, ChemMedChem, 2010, 5(11), 1837-1840.

M. Schlitzer, R. Ortmann, I. Form, Compounds used against worm- and protozoa-caused diseases and the virucide Ribavirin, Pharmazie in Unserer Zeit, 2010, 39(1), 18-26.

M. Schlitzer, R. Ortmann, M. Altenkaemper, CaaX-protein prenyltransferase inhibitors, in: Drug Design of Zinc-Enzyme Inhibitors, Edited By: C. T. Supuran, J.-Y. Winum, 2009, 813-857.

M. Schlitzer, Medicinal chemistry of antimalarial drugs, Pharmazie in Unserer Zeit, 2009, 38(6), 512-520.

M. Schlitzer, Antimalarials: what's in the pipeline?, Pharmazie in Unserer Zeit, 2009, 38(6), 522-526.

M. Schlitzer, Monkeys, humans and malaria. Monkey malaria - for people too dangerous!, Pharmazie in unserer Zeit, 2009, 38(6), 528-30.

M. Schlitzer, Drugs for the treatment of African sleeping sickness, Pharmazie in Unserer Zeit, 2009, 38(6), 552-558.

J. Wiesner, A. Reichenberg, S. Heinrich, M. Schlitzer, H. Jomaa, The plastid-like organelle of apicomplexan parasites as drug target, Curr Pharm Des, 2008, 14, 855-871.

M. Schlitzer, Antimalarial drugs - what is in use and what is in the pipeline, Arch Pharm (Weinheim), 2008, 341, 149.

J. Wiesner, A. Reichenberg, S. Heinrich, M. Schlitzer, H. Jomaa, The plastid-like organelle of apicomplexan parasites as drug target, Curr Pharm Des, 2008, 14, 855-871.

M. Altenkämper, M. Schlitzer, Repellentien und Insektizide - Erfolgreich gegen den Insekten-Angriff, Pharmazeutische Zeitung, 2008, 153, 18-25.

A. Stich, M. Altenkämper, M. Schlitzer, Malaria - Teil I: Medikamentöse Therapie, Deutsche Apotheker Zeitung, 2008, 148, 36-45.

A. Stich, M. Altenkämper, M. Schlitzer, Malaria - Teil II: Prophylaxe, Deutsche Apotheker Zeitung, 2008, 148, 53-58.

A. Stich, M. Schlitzer, Drugs for the treatment and prophylaxis of malaria, Arzneimitteltherapie, 2008, 26(5), 161-175.

A. Stich, M. Schlitzer, Drugs for treatment and prophylaxis of malaria, Chemotherapie Journal, 2008, 17(2), 37-56.

M. Schlitzer, Malaria chemotherapeutics part I: History of antimalarial drug development, currently used therapeutics, and drugs in clinical development, ChemMedChem, 2007, 2, 944-986.

M. Schlitzer, Selektiver Enzyminhibitor statt "Iron-triggered cluster bomb". Neue Erkenntnisse zum Wirkmechanismus von Artemisininderivaten, Pharm Unserer Zeit, 2006, 35, 8-9.

J. Wiesner, R. Ortmann, H. Jomaa, M. Schlitzer, Neue Antimalaria-Wirkstoffe, Angewandte Chemie 2003, 115, 5432-5451; und Angewandte Chemie Int. Ed. 2003, 42, 5274-5293.