synthesis and in vitro pharmacology of a series of histamine h2 ...

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List of publications J.A.M. Christiaans, A.D. Windhorst, P.M. Groenenberg, H. van der Goot, H. Timmerman Synthesis and in vitro pharmacology of new 1,4-dihydropyridines. 1. 2-(co-Aminoalkylthiomethyl)-1,4-dihydropyridines as potent calcium channel blockers EurJ.Med.Chem., 28, 859-867 (1993) J.A.M. Christiaans, H. van der Goot, H. Timmerman Synthesis and in vitro pharmacology of a series of new 1,4-dihydropyridines. 2. Diethyl 4-[2-(co-aminoalkoxy)phenyl]-2,6-dimethyl-l,4-dihydropyridine-3,5dicarboxylates and their corresponding isothioureas as tools for determining structure-acticity relationships EurJ.Med.Chem., 28, 935-941 (1993) J.A.M. Christiaans, A.D. Windhorst, H. van der Goot, H. Timmerman Synthesis and in vitro pharmacology of a series of hybrid molecules possessing 1,4dihydropyridine calcium channel blocking activity and histamine H2-agonistic properties submitted J.A.M. Christiaans, H. Timmerman Hybrid molecules: combination of more than one pharmacological property in one single molecule in preparation J.A.M. Christiaans, W.M.P.B. Menge, H. van der Goot, H. Timmerman Synthesis and in vitro pharmacology of a series of dimaprit analogues with histamine H2-agonistic and histamine Hi-antagonistic activities] in preparation 213
Curriculum Vitae Johannes Antonius Maria Christiaans was born in 1963 on August 17* at Boxmeer, The Netherlands. He graduated from secondary school (HAVO) in 1981 and from high school (VWO) in 1983 at the Hertog-Jan College at Valkenswaard. In the same year he entered the Faculty of Chemistry of the Rijksuniversiteit at Utrecht. After studying Chemistry with Bio-organic Chemistry as principal subject (under the supervision of Prof. Dr. J.F.G. Vliegenthart and Prof. Dr. J.P. Kamerling; Synthesis of polysaccharides) and Biochemistry and Bio-organic Chemistry as subsidiary subject, he acquired his M.Sc. in Chemistry in 1988. Form March 15* 1989 he worked as a scientific research assistant at the Department of Pharmacochemistry of the Leiden/Amsterdam Center for Drug Research at the Vrije Universiteit at Amsterdam. The project was financially supported by Byk-Cedona Nederland B.V. 215
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SYNTHESIS AND IN VITRO PHARMACOLOGY
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Promotor : prof.dr H. Timmerman Cop
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The investigations described in thi
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Chapter 1 Chapter 1 Pharmacotherape
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Chapter 1 2.2 Role of calcium Calci
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Chapter 1 The excitation-contractio
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Chapter 1 Antiarrhythmic drugs modi
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Chapter 1 Until now, no selective c
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Chapter 1 pyridines are expected to
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Chapter 1 Like the p-adrenoceptor s
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Chapter 1 3.3.3 Phosphodiesterase I
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arteries brain Central Nervous Syst
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Chapter 1 The development of renin
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^-ADRENOCEPTOR ANTAGONISTS Chapter
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51 Cromakalim 52 Nicorandil 53 Pina
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Chapter 1 The CCBs are a heterogene
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Chapter 1 4.2 Combination of cardio
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Chapter 1 22 Claremon DA, Baldwin J
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Chapter 1 56 Carini DJ, Chiu AT, Du
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Chapter 2 Chapter 2 Hybrid molecule
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identical twin drug (A-A) - 2A non-
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Chapter 2 Dimeric 1,4-dihydropyridi
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Chapter 2 plasma-protein binding si
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Chapter 2 PAF antagonist, showing o
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Corsano et al. 18 Chapter 2 have sy
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Chapter 2 Görlitzer et al. 21 synt
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Chapter 2 enzyme cyclooxygenase is
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Chapter 2 Table 4: TxA 2/PGH 2 bind
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Chapter 2 the compound had poor ora
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Chapter 2 presented to explain why
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Chapter! When two antihypertensive
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Chapter 2 Table 9: p-Receptor affin
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Chapter 2 dual vasodilating mechani
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Figure 33: Hybrid molecule DG20 (R
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5.4 Antihypertensive hybrid molecul
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Chapter 2 However, due to the terat
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Figure 43: Hybrid molecule possessi
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Chapter 2 5.4.e Hybrid molecules co
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Chapter 2 The two pairs of enantiom
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I H CH 3 Figure 50: Urapidil, an 04
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Chapter 2 15 Pilar Ortega M, Del Ca
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Chapter 2 AI Morgan TK Jr, Lis R, L
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Chapter 2 68 Baldwin JJ, Lurama WC
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Chapter 3 '2 Chapter 3 Organic nitr
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Chapter 3 phosphorylation of contra
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Chapter 3 In table 1, the in vitro
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Figure 8: Ligands for the histamine
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Chapter 3 Nitrate esters can be obt
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Chapter 3 resulting in the loss of
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Chapter 3 14 Yeates RA, Possible me
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Chapter 4 Chapter 4 2 + L-type volt
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Chapter 4 homologous domains surrou
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Chapter 4 channel, which is suggest
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Chapter 4 channel blocking activity
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Chapter 4 Structural modifications
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Chapter 4 Table 6: Calcium channel
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RiOOC COORo compound R\ R 2 nicardi
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Chapter 4 enantiomer.(-)-S11568 inh
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Chapter 4 The cardiovascular activi
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Chapter 4 rat tail artery 73 . Also
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Chapter 4 The compound HOE 166 18 (
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Figure 11: Molecular structure of a
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Chapter 4 SM-6586 was a more potent
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Chapter 4 inactivated (resting) sta
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Chapter 4 20 van Amsterdam F.T.M, Z
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Chapter 4 45 Muto K, Kuroda T, Kawa
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Chapter 4 67 Gaviraghi G, Lacidipin
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Chapter 4 95 Goldmann S, Stoltefuß
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Chapter 5 Synthesis and in vitro ph
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Chapters
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Chapters from the 1,4-DHPs 17. In t
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3 Pharmacology Chapter 5 3.1 In vit
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Chapter 5 Table II. Calcium blockin
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Chapter 5 Radioligand binding affin
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Chapters 13.1 Hz, 2H, pyridine-CHb-
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2-(2-aminoethylthio)methyl-3,5-dica
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Chapters 5 Katz AM, In: Calcium ant
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Chapter 6 Synthesis and in vitro ph
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Chapter 6 by nifedipine analogues i
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Chapter 6 4 Results and discussion
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lipid compartment protein compartme
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Chapter 6 phthalimide-H), 7.77-7.80
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Chapter 6 ^-NMR (CDCI3): 1.18 ppm (
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Page 173 and 174: Chapter 7 generation calcium channe
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Page 203 and 204: 4 Pharmacology Chapter 8 4.1 Histam
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Page 207 and 208: Chapter 8 Based on the observations
Page 209 and 210: Chapter 8 iH-NMR (CDCI3): 1.28-1.50
Page 211 and 212: Chapter 8 13 Vitali T, Impicciatore
Page 213 and 214: Summary The investigations describe
Page 215 and 216: Samenvatting Het in dit proefschrif
Page 217: substituenten, zoals een difenylalk
Page 221: voor de prettige sociale contacten
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