J. Holenz: search on Z-Library

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1

In vitro inhibition of liver forms of the rodent malaria parasitePlasmodium bergheiby naphthylisoquinoline alkaloids – structure-activity relationships of dioncophyllines A and C and ancistrocladine

Guido François, Georges Timperman, Tania Steenackers, Laurent Aké Assi, Jörg Holenz, Gerhard Bringmann

Journal:

Parasitology Research

Year:

1997

Language:

english

File:

PDF, 535 KB

english, 1997

2

Constituents of Picralima nitida display pronounced inhibitory activities against asexual erythrocytic forms of Plasmodium falciparum in vitro

G. François, L. AkéAssi, J. Holenz, G. Bringmann

Journal:

Journal of Ethnopharmacology

Year:

1996

Language:

english

File:

PDF, 362 KB

english, 1996

3

Vismione H and structurally related anthranoid compounds of natural and synthetic origin as promising drugs against the human malaria parasitePlasmodium falciparum: structure-activity relationships

Guido François, Tania Steenackers, Laurent Aké Assi, Wolfgang Steglich, Kai Lamottke, Jörg Holenz, Gerhard Bringmann

Journal:

Parasitology Research

Year:

1999

Language:

english

File:

PDF, 164 KB

english, 1999

4

Larvicidal activity of the naphthylisoquinoline alkaloid dioncophylline A against the malaria vector Anopheles stephensi

G. François, M. Van Looveren, G. Timperman, B. Chimanuka, L. AkéAssi, J. Holenz, G. Bringmann

Journal:

Journal of Ethnopharmacology

Year:

1996

Language:

english

File:

PDF, 421 KB

english, 1996

5

Differential sensitivity of erythrocytic stages of the rodent malaria parasitePlasmodium chabaudi chabaudito dioncophylline B, a highly active naphthylisoquinoline alkaloid

Guido François, Bantuzeko Chimanuka, Georges Timperman, Jörg Holenz, Jacqueline Plaizier-Vercammen, Laurent Aké Assi, Gerhard Bringmann

Journal:

Parasitology Research

Year:

1999

Language:

english

File:

PDF, 129 KB

english, 1999

6

Synthesis of σ receptor ligands with unsymmetrical spiro connection of the piperidine moiety

Annemarie Jasper, Dirk Schepmann, Kirstin Lehmkuhl, Jose Miguel Vela, Helmut Buschmann, Jörg Holenz, Bernhard Wünsch

Journal:

European Journal of Medicinal Chemistry

Year:

2009

Language:

english

File:

PDF, 294 KB

english, 2009

7

Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats

Angels Fisas, Xavier Codony, Gonzalo Romero, Alberto Dordal, Jesus Giraldo, Ramon Mercé, Jörg Holenz, David Heal, Helmut Buschmann, Petrus Johan Pauwels

Journal:

British Journal of Pharmacology

Year:

2006

Language:

english

File:

PDF, 334 KB

english, 2006

8

Microwave assisted synthesis of spirocyclic pyrrolidines – σ1 receptor ligands with modified benzene-N-distance

Annemarie Jasper, Dirk Schepmann, Kirstin Lehmkuhl, Jose Miguel Vela, Helmut Buschmann, Jörg Holenz, Bernhard Wünsch

Journal:

European Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 354 KB

english, 2012

9

Design and Synthesis of β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors with in Vivo Brain Reduction of β-Amyloid Peptides

Swahn, Britt-Marie, Kolmodin, Karin, Karlström, Sofia, von Berg, Stefan, Söderman, Peter, Holenz, Jörg, Berg, Stefan, Lindström, Johan, Sundström, Marie, Turek, Dominika, Kihlström, Jacob, Slivo, Can,

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 620 KB

english, 2012

10

[Methods and Principles in Medicinal Chemistry] Lead Generation || Selective Optimization of Side Activities: An Alternative and Promising Strategy for Lead Generation

Year:

2016

Language:

english

File:

PDF, 3.67 MB

english, 2016

11

‘Biomimetic’ oxidative dimerization of korupensamine A: Completion of the first total synthesis of michellamines A, B, and C

Gerhard Bringmann, Sven Harmsen, Jörg Holenz, Torsten Geuder, Roland Götz, Paul A. Keller, Rainer Walter, Yali F. Hallock, John H. Cardellina II, Michael R. Boyd

Journal:

Year:

1994

Language:

english

File:

PDF, 358 KB

english, 1994

12

Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of σ 1 Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1 H -pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)

Díaz, José Luis, Cuberes, Rosa, Berrocal, Joana, Contijoch, Montserrat, Christmann, Ute, Fernández, Ariadna, Port, Adriana, Holenz, Jörg, Buschmann, Helmut, Laggner, Christian, Serafini, Maria Teresa,

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 1.47 MB

english, 2012

13

[Methods and Principles in Medicinal Chemistry] Lead Generation || A Fragmentation Enumeration Approach to Generating Novel Drug Leads

Year:

2016

Language:

english

File:

PDF, 5.62 MB

english, 2016

14

[Methods and Principles in Medicinal Chemistry] Lead Generation || A Medicinal Chemistry Perspective on the Hit-to-Lead Phase in the Current Era of Drug Discovery

Year:

2016

Language:

english

File:

PDF, 4.54 MB

english, 2016

15

Chronic 5-HT6 receptor modulation by E-6837 induces hypophagia and sustained weight loss in diet-induced obese rats

A Fisas, X Codony, G Romero, A Dordal, J Giraldo, R Mercé, J Holenz, N Vrang, R V Sørensen, D Heal, H Buschmann, P J Pauwels

Journal:

British Journal of Pharmacology

Year:

2007

Language:

english

File:

PDF, 36 KB

english, 2007

16

[Methods and Principles in Medicinal Chemistry] Lead Generation || Molecular Recognition and Its Importance for Fragment-Based Lead Generation and Hit-to-Lead

Year:

2016

Language:

english

File:

PDF, 12.68 MB

english, 2016

17

[Methods and Principles in Medicinal Chemistry] Lead Generation || Predictive Methods in Lead Generation

Year:

2016

Language:

english

File:

PDF, 4.34 MB

english, 2016

18

Growth Inhibition of Asexual Erythrocytic Forms of Plasmodium falciparum and P. berghei in vitro by Naphthylisoquinoline Alkaloid-Containing Extracts of Ancistrocladus and Triphyophyllum Species

François, G, Timperman, G, Haller, R D, Bär, S, Isahakia, M A, Robertson, S A, Zhao, C, De Souza, N J, Aké Assi, L, Holenz, J, Bringmann, G

Journal:

Pharmaceutical Biology

Year:

1997

Language:

english

File:

PDF, 98 KB

english, 1997

19

Antiplasmodial Activity of Mono- and Dimeric Carbazoles

Bringmann, Gerhard, Ledermann, Alfons, Holenz, Jörg, Kao, Muh-Tsuen, Busse, Ulrich, Wu, Howard, François, Guido

Journal:

Year:

1998

Language:

english

File:

PDF, 258 KB

english, 1998

20

[Methods and Principles in Medicinal Chemistry] Lead Generation || Vorapaxar: From Lead Identification to FDA Approval

Year:

2016

Language:

english

File:

PDF, 3.41 MB

english, 2016

21

Novel KV7 ion channel openers for the treatment of epilepsy and implications for detrusor tissue contraction

Seefeld, Mark A., Lin, Hong, Holenz, Joerg, Downie, Dave, Donovan, Brian, Fu, Tingting, Pasikanti, Kishore, Zhen, Wei, Cato, Matthew, Chaudhary, Khuram W., Brady, Pat, Bakshi, Tania, Morrow, Dwight, R

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2018

Language:

english

File:

PDF, 532 KB

english, 2018

22

Acetogenic Isoquinoline Alkaloids, LXXXII. Biomimetic Total Synthesis of Michellamines A–C

Gerhard Bringmann, Roland Götz, Sven Harmsen, Jörg Holenz, Rainer Walter

Journal:

European Journal of Organic Chemistry

Year:

1996

Language:

english

File:

PDF, 1.60 MB

english, 1996

23

[Methods and Principles in Medicinal Chemistry] Lead Generation || Lead Structure Discovery for Neglected Diseases: Product Development Partnerships Driving Drug Discovery

Year:

2016

Language:

english

File:

PDF, 4.84 MB

english, 2016

24

Advances in Lead Generation

Holenz, Joerg, Stoy, Patrick

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2018

Language:

english

File:

PDF, 935 KB

english, 2018

25

Novel derivatives of 3-alkyl-1,5-diaryl-1H-1,2,4-triazoles and their pharmacological evaluation as CB1cannabinoid ligands

Laura Hernandez-Folgado, Pilar Goya, Jordi Frigola, María Rosa Cuberes, Alberto Dordal, Jörg Holenz, Nadine Jagerovic

Journal:

Monatshefte für Chemie - Chemical Monthly

Year:

2008

Language:

english

File:

PDF, 212 KB

english, 2008

26

Medicinal chemistry strategies to 5-HT6 receptor ligands as potential cognitive enhancers and antiobesity agents

Jörg Holenz, Petrus J. Pauwels, José Luis Díaz, Ramon Mercè, Xavier Codony, Helmut Buschmann

Journal:

Drug Discovery Today

Year:

2006

Language:

english

File:

PDF, 1.15 MB

english, 2006

27

Antidepressants, Antipsychotics, Anxiolytics || Chemistry

Buschmann, Helmut, Daz, Jos Luis, Holenz, Jrg, Prraga, Antonio, Torrens, Antoni, Vela, Jos Miguel

Year:

2007

Language:

english

File:

PDF, 800 KB

english, 2007

28

Thiophene Bioisosteres of Spirocyclic σ Receptor Ligands: Relationships between Substitution Pattern and σ Receptor Affinity

Oberdorf, Christoph, Schepmann, Dirk, Vela, Jose Miguel, Buschmann, Helmut, Holenz, Jörg, Wünsch, Bernhard

Journal:

Journal of Medicinal Chemistry

Year:

2012

Language:

english

File:

PDF, 1.65 MB

english, 2012

29

Sulfonimidamides as Sulfonamides Bioisosteres: Rational Evaluation through Synthetic, in Vitro, and in Vivo Studies with γ-Secretase Inhibitors

Dr. Fernando Sehgelmeble, Dr. Juliette Janson, Dr. Colin Ray, Susanne Rosqvist, Dr. Susanne Gustavsson, Linda I. Nilsson, Dr. Alexander Minidis, Dr. Jörg Holenz, Dr. Didier Rotticci, Dr. Johan Lundkvi

Journal:

Year:

2012

Language:

english

File:

PDF, 292 KB

english, 2012

30

A comparison of the stage-specific efficacy of chloroquine, artemether and dioncophylline B against the rodent malaria parasitePlasmodium chabaudi chabaudiin vivo

B. Chimanuka, G. François, G. Timperman, Vander Y. Heyden, J. Holenz, J. Plaizier-Vercammen, G. Bringmann

Journal:

Parasitology Research

Year:

2001

Language:

english

File:

PDF, 254 KB

english, 2001

31

[Methods and Principles in Medicinal Chemistry] Lead Generation || Introduction: Learnings from the Past - Characteristics of Successful Leads

Year:

2016

Language:

english

File:

PDF, 3.00 MB

english, 2016

32

Biotransformation of Two -Secretase Inhibitors Including Ring Opening and Contraction of a Pyrimidine Ring

Lindgren, A., Eklund, G., Turek, D., Malmquist, J., Swahn, B.-M., Holenz, J., von Berg, S., Karlstrom, S., Bueters, T.

Journal:

Drug Metabolism and Disposition

Year:

2013

Language:

english

File:

PDF, 2.68 MB

english, 2013

33

[Methods and Principles in Medicinal Chemistry] Lead Generation || Development of Influenza Virus Sialidase Inhibitors

Year:

2016

Language:

english

File:

PDF, 5.93 MB

english, 2016

34

Medicinal Chemistry Driven Approaches Toward Novel and Selective Serotonin 5-HT6 Receptor Ligands

Holenz, Jörg, Mercè, Ramon, Díaz, José Luis, Guitart, Xavier, Codony, Xavier, Dordal, Alberto, Romero, Gonzalo, Torrens, Antoni, Mas, Josep, Andaluz, Blas

Journal:

Journal of Medicinal Chemistry

Year:

2005

Language:

english

File:

PDF, 349 KB

english, 2005

35

Synthesis and Pharmacological Evaluation of a Potent and Selective σ1 Receptor Antagonist with High Antiallodynic Activity

Tina Utech, Jens Köhler, Helmut Buschmann, Jörg Holenz, Jose Miguel Vela, Bernhard Wünsch

Journal:

Archiv der Pharmazie

Year:

2011

Language:

english

File:

PDF, 207 KB

english, 2011

36

[Methods and Principles in Medicinal Chemistry] Lead Generation || Competitive Intelligence-based Lead Generation and Fast Follower Approaches

Year:

2016

Language:

english

File:

PDF, 7.28 MB

english, 2016

37

[Methods and Principles in Medicinal Chemistry] Lead Generation || Front Matter

Year:

2016

Language:

english

File:

PDF, 2.79 MB

english, 2016

38

[Methods and Principles in Medicinal Chemistry] Lead Generation || Lead Generation for Challenging Targets

Year:

2016

Language:

english

File:

PDF, 6.73 MB

english, 2016

39

[Methods and Principles in Medicinal Chemistry] Lead Generation || Index

Year:

2016

Language:

english

File:

PDF, 3.84 MB

english, 2016

40

Thiophene Bioisosteres of Spirocyclic σ Receptor Ligands. 1. N-Substituted Spiro[piperidine-4,4′-thieno[3,2- c ]pyrans]

Oberdorf, Christoph, Schepmann, Dirk, Vela, Jose Miguel, Diaz, Jose Luis, Holenz, Jörg, Wünsch, Bernhard

Journal:

Journal of Medicinal Chemistry

Year:

2008

Language:

english

File:

PDF, 309 KB

english, 2008

41

[Methods and Principles in Medicinal Chemistry] Lead Generation || The Strategies and Politics of Successful Design, Make, Test, and Analyze (DMTA) Cycles in Lead Generation

Year:

2016

Language:

english

File:

PDF, 6.69 MB

english, 2016

42

Combination of Two Pharmacophoric Systems: Synthesis and Pharmacological Evaluation of Spirocyclic Pyranopyrazoles with High σ 1 Receptor Affinity

Schläger, Torsten, Schepmann, Dirk, Lehmkuhl, Kirstin, Holenz, Jörg, Vela, Jose Miguel, Buschmann, Helmut, Wünsch, Bernhard

Journal:

Journal of Medicinal Chemistry

Year:

2011

Language:

english

File:

PDF, 1.55 MB

english, 2011

43

[Methods and Principles in Medicinal Chemistry] Lead Generation || GPR81 HTS Case Study

Year:

2016

Language:

english

File:

PDF, 10.69 MB

english, 2016

44

Aminoimidazoles as BACE-1 inhibitors: The challenge to achieve in vivo brain efficacy

Britt-Marie Swahn, Jörg Holenz, Jacob Kihlström, Karin Kolmodin, Johan Lindström, Niklas Plobeck, Didier Rotticci, Fernando Sehgelmeble, Marie Sundström, Stefan von Berg, Johanna Fälting, Biljana Geor

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 767 KB

english, 2012

45

Synthesis of 3-(2-N,N-diethylaminoethoxy)indoles as potential 5-HT6 receptor ligands

Alex, Karolin, Schwarz, Nicolle, Khedkar, Vivek, Sayyed, Iliyas Ali, Tillack, Annegret, Michalik, Dirk, Holenz, Jörg, Díaz, José Luis, Beller, Matthias

Journal:

Organic & Biomolecular Chemistry

Year:

2008

Language:

english

File:

PDF, 173 KB

english, 2008

46

[Methods and Principles in Medicinal Chemistry] Lead Generation || The Discovery of Cathepsin A Inhibitors: A Project-Adapted Fragment Approach Based on HTS Results

Year:

2016

Language:

english

File:

PDF, 10.02 MB

english, 2016

47

[Methods and Principles in Medicinal Chemistry] Lead Generation || “Ligandability” of Drug Targets: Assessment of Chemical Tractability via Experimental and In Silico Approaches

Year:

2016

Language:

english

File:

PDF, 4.12 MB

english, 2016

48

Structural–activity relationship study on C-4 carbon atom of the CB1 antagonist SR141716: synthesis and pharmacological evaluation of 1,2,4-triazole-3-carboxamides

Nadine Jagerovic, Laura Hernandez-Folgado, Ibon Alkorta, Pilar Goya, María Isabel Martín, María Teresa Dannert, Ángela Alsasua, Jordi Frigola, María Rosa Cuberes, Alberto Dordal, Jörg Holenz

Journal:

European Journal of Medicinal Chemistry

Year:

2006

Language:

english

File:

PDF, 334 KB

english, 2006

49

[Methods and Principles in Medicinal Chemistry] Lead Generation || Rational Hit Generation

Year:

2016

Language:

english

File:

PDF, 4.00 MB

english, 2016

50

Molluscicidal Activity (Biomphalaria glabrata) of Dioncophylline A: Structure-Activity Investigations#

G. Bringmann, J. Holenz, L. Assi, K. Hostettmann

Year:

1998

Language:

english

File:

PDF, 122 KB

english, 1998

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