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45. Antiproliferative activity results of newly synthesized DHPM derivatives(VIIi-xxx).467xi
PrefacePrefaceHeterocyclic chemistry is vastly expending because of the enormous amount of researchwork being done in this area. The majority of known molecules are heterocycles andheterocycles dominate the field of biochemistry, medicinal chemistry, dyestuff,photographic sciences and are of increasing importance in many other areas includingpolymers, adhesives and molecular engineering.Among the heterocyclic compounds, pyrimidines have a long and distinguished historyextending from the days of their discovery as important constituents of nucleic acid totheir current use in the chemotherapy of AIDS. During the last four decades, severalpyrimidines have been developed as chemotherapeutic agents and have found wideclinical applications as anticancer, antiviral and anti-AIDS, antitubercular,sedative/hypnotic/antiepileptic, cardiac agents, as well as analgetics, diuretics, antibioticsand metabolic electrolytes etc. 1Thus, the focus of the present work is to synthesize some novel pyrimidine, condensedpyrimidine and dihydropyrimidine derivatives and to evaluate them for their antiulcer andmultidrug reverting activities.This thesis has been divided into following three parts.Part-I of this work deals with the “Synthesis, Pharmacological Evaluation and QSAR ofsome Pyrimidylmethylsulfinylbenzimidazoles as potential reversible Proton PumpInhibitors (PPI’s)”.In 19 th Century, light diet consisting of food not stimulating gastric acid secretion wasrecommended for treating peptic ulcer related disorders. Since then a number of strategieshave been designed to control these disorders related to the hypersecretion of acid. 2,3These therapeutic strategies extend from simple conventional antacids to the use of morecomplex and effective proton pump inhibitors (PPI’s). 4 Associated effects of conventionalantacids like constipation or diarrhea limit their patient compliance and are today mainlyused for fast symptomatic relief. Muscarinic antagonists like pirenzepine inhibit gastricacid secretion as well as decrease gastric motility, but clinical use of these drugs is nowlimited because of the availability of more effective anti-secretory medications. A newxii
Page 1 and 2: Saurashtra UniversityRe - Accredite
Page 3 and 4: Statement Under O.Ph.D. 7 of Sauras
Page 5 and 6: ContentsAcknowledgementRegistration
Page 7 and 8: Contents1.2 Synthesis of condensed
Page 9 and 10: Contents1.5 MDR modulators 3981.6 D
Page 11 and 12: infrastructure and all the faciliti
Page 13 and 14: Above all I thank Lord Hanuman Ji a
Page 15 and 16: Abbreviations used1 H NMR Proton Nu
Page 17 and 18: UVVEGFRWCRWHOZ-EUltra VioletVascula
Page 19: 22. 2-Substitutedthieno[3,2-d]/benz
Page 23 and 24: PrefaceThis entire cascade of react
Page 25 and 26: PrefaceOONHNHPOCl 3MWINVi-xviiClClC
Page 27 and 28: PrefaceOOHOOOONHNHDP-7 1NHMonastrol
Page 29 and 30: PART-I
Page 31 and 32: 3.7 Results and discussion on biolo
Page 33 and 34: Part-1Review on Antiulcer Literatur
Page 37 and 38: Table 2: Distinguishing Features of
Page 41 and 42: 1.2.2. Muscarinic AntagonistsPart-1
Page 55 and 56: 1.5.5. Pharmacological PropertiesPa
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Part-1Review on Antiulcer Literatur
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2. Aim of the Present WorkPart-IAim
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Part-IAim of Present WorkR 2 OR 3 R
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2.2. Bacisity of Pyridine vs Pyrimi
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Part-IAim of Present WorkOANNHOSNHN
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Part-IAim of Present WorkS. No. A S
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3. Results and Discussion
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Part-IResults and Discussion3.1.1d
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Part-IResults and DiscussionOR 1XR
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Part-IResults and Discussionformed
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Part-IResults and DiscussionOOON 2
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c. Synthesis of 2-carbethoxy-3-amin
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Part-IResults and DiscussionTable 7
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Part-IResults and DiscussionOOEtNHO
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Part-IResults and DiscussionTable-8
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Part-IResults and DiscussionCompd.N
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Part-IResults and DiscussionStep-IY
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S. No. Y Mol. Formula(Sol. ofrecrys
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Part-IResults and DiscussionS. No.
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Part-IResults and DiscussionONNHIII
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Part-IResults and DiscussionS. No.A
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Part-IResults and Discussion3.5. Sp
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Specimen 1 H NMR spectra of 2-chlor
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Part-IResults and Discussioninvolve
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Part-IResults and DiscussionSpecime
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The Infrared (IR) spectra:Part-IRes
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Part-IResults and DiscussionR 1ON+
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Part-IResults and DiscussionOSNHOSN
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3.6 Biological Evaluation of PPI’
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Part-IResults and DiscussionExperim
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Part-IResults and DiscussionDrug Pr
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Table 11. Effect of newly synthesiz
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Part-IResults and DiscussionS.No.AR
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Part-IResults and DiscussionS.No.AR
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Figure-1. Effect of newly synthesiz
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Figure-3. Effect of newly synthesiz
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Part-IResults and DiscussionFigure
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Part-IResults and DiscussionFigure
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Part-IResults and Discussion2. Effe
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Part-IResults and Discussionby kine
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Part-IResults and DiscussionNNNNNHN
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3.8. QSAR StudiesPart-IResults and
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Part-IResults and DiscussionFigure-
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Part-IResults and DiscussionPhysico
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Part-IResults and DiscussionThe MDS
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2. Volume of gastric secretion:Desc
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Part-IResults and DiscussionFor the
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3. Ulcer scoreDescription of the de
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Part-IResults and Discussion24. Ros
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4. Experimental
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Part-IExperimental119 o C was 128-1
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5. Synthesis of ethyl 2-amino-4-phe
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Part-IExperimentalthe procedure des
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Part-IExperimentalRecrystallization
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Part-IExperimentalM.P. : 132-134 o
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Part-IExperimentalA solution of thi
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Part-IExperimentalNMR (CDCl 3 )δpp
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Part-IExperimental6. Reaction of et
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Part-IExperimentalNMR (CDCl 3 )δpp
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Part-IExperimentalM.P. : 240-245 o
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Part-IExperimentalrecrystallization
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Part-IExperimental(1H, d, CH at imi
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Part-IExperimentalNMR (DMSO-d 6 )δ
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M.P. : 140-142 o C; Yield: 73%.Mol.
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M.P. : 135-141 o C; Yield: 67%.Mol.
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Part-IExperimentalml), over a perio
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Part-IExperimentalchloride was adde
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Part-IExperimental29. Synthesis of
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Part-IExperimentalIR (KBr) cm -1 :
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Part-IExperimentaladded while stirr
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Part-IExperimentald]pyrimidin-4(3H)
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Part-IExperimentalMol. formula : C
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Part-IExperimentalthis clear soluti
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Part-IExperimentalwhile maintaining
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Part-IExperimentalMol. Formula : C
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PART-II
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Part-IIContents2.3.2.1 Mononuclear
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Part-IISynthesis of Pyrimidines1. S
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Part-IISynthesis of PyrimidinesYZR
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Part-IISynthesis of Pyrimidineselec
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Part-IISynthesis of PyrimidinesR 1R
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Part-IISynthesis of Pyrimidinespyri
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R 1 R 2 R Yield(%)Part-IISynthesis
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Part-IISynthesis of Pyrimidinesyiel
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Table 27: 2-Amino-3-substitutedaryl
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Part-IISynthesis of PyrimidinesWhil
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Part-IISynthesis of PyrimidinesSimi
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Part-IISynthesis of PyrimidinesTabl
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R 1 R 2 R X Yield(%)Part-IISynthesi
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Part-IISynthesis of Pyrimidines+RCN
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Part-IISynthesis of PyrimidinesNN+
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Part-IISynthesis of PyrimidinesR 1+
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Part-IISynthesis of Pyrimidinesthe
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Part-IISynthesis of Pyrimidinesacet
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Part-IISynthesis of Pyrimidinesexpe
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Part-IISynthesis of PyrimidinesNOOC
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Part-IISynthesis of PyrimidinesThe
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Part-IISynthesis of PyrimidinesTabl
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Part-IISynthesis of PyrimidinesOH 3
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1.10 ReferencesPart-IISynthesis of
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Part-IISynthesis of Pyrimidines42.
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2. Impact of Microwave Assisted Hea
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Part-IIImpact of Microwave…Microw
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Part-IIImpact of Microwave…Figure
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Part-IIImpact of Microwave…R 1ArR
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Part-IIImpact of Microwave…as an
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Part-IIImpact of Microwave…al. 21
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Part-IIImpact of Microwave…XOHR 1
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Part-IIImpact of Microwave…N+N21B
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Part-IIImpact of Microwave…OO+ NO
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Part-IIImpact of Microwave…NO 2NO
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Part-IIImpact of Microwave…RNHNNH
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Part-IIImpact of Microwave…assist
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Part-IIImpact of Microwave…CNRNH
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Part-IIImpact of Microwave…Multig
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Part-IIImpact of Microwave…Nie et
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Part-IIImpact of Microwave…synthe
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Part-IIImpact of Microwave…An eff
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Part-IIImpact of Microwave…OO+S 8
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2.6. ReferencesPart-IIImpact of Mic
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49. Baxendale, I. R.; Ley, S. V. J.
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Part-IIAim of the Present Work3. Ai
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Part-IIAim of the Present WorkONHR
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Part-IIAim of the Present WorkYZXNN
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Part-IIAim of the Present WorkThe c
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3.5 References:Part-IIAim of the Pr
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Part-IIAim of the Present Work37. S
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Part-IIResults and Discussion4.1 Sy
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4.2 Synthesis of condensed 2-substi
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Table 38: Physical data of condense
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S. No. X Time ofMWIHeating(Min)VxiV
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S. No. X Time ofMWIHeating(Min)Yiel
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4.3 Synthesis of condensed 4-chloro
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Part-IIResults and DiscussionHerein
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Part-IIResults and DiscussionS. No.
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Part-IIResults and DiscussionS. No.
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The Mass spectraPart-IIResults and
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Specimen IR spectra of some 2-chlor
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Part-IIResults and Discussion1 H NM
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Part-IIResults and Discussionion (c
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Specimen 1 H NMR spectra of 4-chlor
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Part-IIResults and Discussion4.5 MD
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Part-IIResults and DiscussionH 3CO1
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Part-IIResults and DiscussionCl14.
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Part-IIResults and DiscussionO14. V
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4.6 References:Part-IIResults and D
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5. ExperimentalPart-IIExperimentalA
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3. Synthesis of 2-chloromethyl-5-ph
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Part-IIExperimentalIR (KBr) cm -1 :
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Part-IIExperimentalM.P. : 247-249 o
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Part-IIExperimental5.4 Synthesis of
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Part-IIExperimentalwere reacted und
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27. Synthesis of 2-methyl-5-phenylt
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Part-IIExperimental80 o C) that yie
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Part-IIExperimental36. Synthesis of
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Part-IIExperimentalunder microwave
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Part-IIExperimentalM.P. : >300 o C
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M.P. : 280-282 o C; Yield: 90%Mol.
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5.10 References:Part-IIExperimental
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Synthesis, Characterization and Ant
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Part-IIIAdvances Dihydropyridines a
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CH 3CH 3Part-IIIAdvances Dihydropyr
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2. Aim of the Present Work
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Part-IIIAim of the Present Workshor
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3. Results and Discussion
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Part-IIIResults and DiscussionOOOHR
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Part-IIIResults and DiscussionUsing
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Part-IIIResults and DiscussionS. No
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S. No R X MolFormula(Sol. of Recrys
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Part-IIIResults and Discussionpheny
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Specimen 13 C NMR spectra of some D
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Part-IIIResults and DiscussionTable
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Part-IIIResults and DiscussionTable
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3.5 DiscussionPart-IIIResults and D
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4. Experimental
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Part-IIIExperimentalglacial acetic
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Part-IIIExperimental5. Synthesis of
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Part-IIIExperimentalIR(KBr) cm -1 :
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Part-IIIExperimentalM.P. : 184-186
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Part-IIIExperimental1 H NMR(DMSO-d
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Part-IIIExperimentalM.P. : 188-190
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Part-IIIExperimental4.2 MDR reversa
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Summary and Conclusion
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Summary and Conclusionactivity in P
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Summary and Conclusionreverting act
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Publications and Presentations
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Publications and PresentationsOther
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Publications and Presentations8. K.
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