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Part-IIIAdvances Dihydropyridines and …NO 2(H 3 C) 2 NC 2 H 5 OOPNHH 3 C CH 3OO CH 3NH 3 COONHNO 2OH 3 C CH 3OCH 3PAK-1 52Nifidipine 53NO 2N(CH 3 ) 2OOH 3 COCH 3H 3 CNHTeludipine 54OOOCF 3HC 2 H 5 NOOH 3 C CH 3ONHBZDC-DHP 55NO 2OONH 3 COH 3 C CH 3ONHNManidipine (CV-4093) 56Figure-8. Structures of new DHPsEarlier, N-alkylated 1,4-DHPs of general formula 57 & 58 were synthesized which werefound to possess a remarkable activity for overcoming resistance to anticancer agents.The DHPs were used in combination with anticancer agents. The DHPs were also foundvery potent in enhancing the therapeutic activity of anticancer agents. 103412
Part-IIIAdvances Dihydropyridines and …ROROH 3 COOOOH 3 C N CH 3R 1H 3 COOOR 3NHH 3 C N CH 3R 2R 25758Figure-9. Structures of 57 and 58 DHPs.In continuation to this, new N-alkylated 1,4- DHPs derivatives were synthesized and theirability to overcome MDR was examined in vincristine-resistant P388 cells (P388/VCRcells). DHPs that possessed an arylalkyl substituent on the DHPs ring nitrogen 59, 60, 61were more potent than verapamil in potentiating the cytotoxicity of vincristine againstP388/VCR cells. However, neither drug effectively enhanced the antitumor activity ofvincristine in tumor-bearing mice. Introduction of basic nitrogen-containing substituentson the side chain of 1,4- DHPs gave improved activity in vitro and in vivo. The piperazinederivative 62 and 63 were more than 10 times as potent as verapamil in vitro. Fourcompounds 64, 65, 66 and 67 selected for in vivo testing showed superior antitumoractivity in P388/VCR-bearing mice in combination with vincristine. The SARs of thecompounds are discussed. 89413
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Saurashtra UniversityRe - Accredite
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Statement Under O.Ph.D. 7 of Sauras
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ContentsAcknowledgementRegistration
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Contents1.2 Synthesis of condensed
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Contents1.5 MDR modulators 3981.6 D
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infrastructure and all the faciliti
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Above all I thank Lord Hanuman Ji a
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Abbreviations used1 H NMR Proton Nu
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UVVEGFRWCRWHOZ-EUltra VioletVascula
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22. 2-Substitutedthieno[3,2-d]/benz
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PrefacePrefaceHeterocyclic chemistr
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PrefaceThis entire cascade of react
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PrefaceOONHNHPOCl 3MWINVi-xviiClClC
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PrefaceOOHOOOONHNHDP-7 1NHMonastrol
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PART-I
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3.7 Results and discussion on biolo
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Part-1Review on Antiulcer Literatur
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Table 2: Distinguishing Features of
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1.2.2. Muscarinic AntagonistsPart-1
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1.5.5. Pharmacological PropertiesPa
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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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Page 427 and 428: M.P. : 280-282 o C; Yield: 90%Mol.
Page 429 and 430: 5.10 References:Part-IIExperimental
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Page 455 and 456: CH 3CH 3Part-IIIAdvances Dihydropyr
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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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