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Part-1Review on Antiulcer LiteratureNOSNHNLeminiprazole 25Figure 13: Structure of 2-[(2-aminobenzyl)sulfinyl]-1H-benzimidazoles as irreversiblegastric proton pump inhibitors.1.4.2. Reversible Gastric PPIs:- To overcome the drawbacks associated with the use ofirreversible PPIs, research has been directed towards discovery of reversible inhibitors.Examples include SCH28080 23, SK& F 97574 26, SCH 32651 27 & SKF 96067 28.CNNNHONONSCH 28080 23OCH 2 CH 2 OHSK & F 97574 26NH 2NHONNOSCH 32651 27ONSK & F 96067 28Figure 14: Structures of some reversible gastric proton pump inhibitors.18
Part-1Review on Antiulcer Literature1.5. Irreversible Proton Pump Inhibitors1.5.1. IntroductionIn early 1970’s, anti-secretory activity of the analogs of the pyridylthioacetamide (CMN)29 was studied. This led to the discovery of a class of extremely efficacious inhibitors ofgastric acid secretion, with a novel mode of action, of which the pyridylmethylbenzimidazole sulfoxide, timoprazole 16, is the archetypal structure. Meanwhile H + /K + -ATPase enzyme was also discovered by other research group that enabled thedemonstration that compounds related to timoprazole were non-competitive inhibitors ofthe enzyme. This led to the synthesis of picoprazole 17 and omeprazole 18, new drugs forthe treatment of peptic-ulcer and related diseases. This work also helped in generating andunderstanding the way in which the enzyme operates. 50SHNSON NH 2NCMN 29Timoprazole 16NHNOONSO Picoprazole 17NFigure 15: Structure of some initial PPIs1.5.2. Mechanism of ActionOn studying the mechanism of action of these inhibitors of the H + /K + -ATPase, severalsalient features of their action became apparent like; a) the weak basicity of thecompounds (pKa≈4), allowing them to accumulate in the acid space adjacent to their siteof action (i.e., secretory canaliculus of the parietal cells); b) the sulfoxides themselveshave no intrinsic activity, but under the influence of acid undergo a chemicalrearrangement to an active species; iii) the active species is thiophillic in nature andcovalently binds to thiol functions like cysteinyl residues generating disulfide bridges tothe enzymes, thereby causing its inactivation. 5019
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 and 20: 22. 2-Substitutedthieno[3,2-d]/benz
Page 21 and 22: PrefacePrefaceHeterocyclic chemistr
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 49: Part-1Review on Antiulcer Literatur
Page 55 and 56: 1.5.5. Pharmacological PropertiesPa
Page 89 and 90: 2. Aim of the Present WorkPart-IAim
Page 91 and 92: Part-IAim of Present WorkR 2 OR 3 R
Page 93 and 94: 2.2. Bacisity of Pyridine vs Pyrimi
Page 95 and 96: Part-IAim of Present WorkOANNHOSNHN
Page 97 and 98: Part-IAim of Present WorkS. No. A S
Page 99 and 100: 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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