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Part-IIIAdvances Dihydropyridines and …OOHOSNEt 2CO 2 HOHHOORClNMK-571 30SR = H Kaempferol 27R = OH Quercetin 28OHOOCH 3NHNOCH 3OCH 3ONHGF-120918 (GG-918) 20H 3 CH 3 COH 3 COCH 3OH OHOCH 3 CH 2OHOOCH 3CH 3OAcCH 3CH 3OHOCH 3Tacrolimus (FK506) 34OOMegestrol acetate 36HOCH 3CH 3OHFigure-6. Structures of various classes of drugs used as MDR reversal agents (contd.)404
Part-IIIAdvances Dihydropyridines and …OCH 3H 3 COOH 3 COOCH 3CH 3CH 3OAcONOONOCH 333NMedroxyprogesterone acetate 37Biricodar (VX-710) 35AcOOAcAcOOAcH 3 CH 3 CCH 3CH 3CH 3CH 3OOCH 3HOAcTaxuspine C 38CH 2OCinnCinn = CinnamoylHCH 3H O39OAcOCinnFigure-6. Structures of various classes of drugs used as MDR reversal agents1.6 DHPs as Potential MDR Reversal AgentsHistorical Background:Some members of calcium channel blockers, such as nicardipine 40 and nimodipine 41,were identified as potent MDR antagonists. This early work stressed the lack ofcorrelation between the calcium channel blocking and anti-MDR potencies. 75 It has beenreported that DHPs bind to a site which is allosterically coupled to the receptor site whichbinds anticancer agents and other MDR reversal agents. 76,77 DHPs are well recognized as“privileged structure” for their multi receptor affinity. 78,79In the derivatives bearing a stereogenic center at C-4, such as nicardipine, nimodipine,nitrendipine 42, felodipine 43, isradipine 44 and niguldipine 45, both stereoisomers differmarkedly in their potencies as calcium channel blockers but they are about equally405
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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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Page 401 and 402: Part-IIResults and DiscussionO14. V
Page 403 and 404: 4.6 References:Part-IIResults and D
Page 405 and 406: 5. ExperimentalPart-IIExperimentalA
Page 407 and 408: 3. Synthesis of 2-chloromethyl-5-ph
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Page 425 and 426: Part-IIExperimentalM.P. : >300 o C
Page 427 and 428: M.P. : 280-282 o C; Yield: 90%Mol.
Page 429 and 430: 5.10 References:Part-IIExperimental
Page 431 and 432: Synthesis, Characterization and Ant
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Page 455 and 456: CH 3CH 3Part-IIIAdvances Dihydropyr
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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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