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Part-IIIAdvances Dihydropyridines and …compiles the best-known MDR substrates used for functional diagnosis of the proteins. 8-11,40-433A: MDR-substrate anticancer agents. Abbreviations: VCR: vincristine, VP-16:etoposide, STER: steroids, TAM: tamoxiphen, TKI-INHIB: tyrosin kinase inhibitorse.g. STI-571, DOX: doxorubicine or adriamycin, DNR: daunorubicin, , EPIR:epirubicin, MX: mitoxantrone, TOPOT: topotecan, iridotecan, BISANT:bisanthrone, COLCH: colchicin, ACT-D: actinomycin D, MYTOM: mytomycin,TX: methotrexate, CPHAM: cyclophosphamide, CHLB: chlorambucil, CARM:carmustine, LCV: leucovorin, HUR: hydroxy urea, CISPL: cisplatin, TAXOL:paclitaxel. (Reproduced from reference-4)3B: MDR-Modulating agents. Abbreviations: CSA: cyclosporin A, VERAP: verapamilSTAURO: staurosporine, ECON: econazole, PRAZ: prazosine, FTC: fumitremorginC, PROB: probenecide, BBR: benzbromarone, SUPYR: sulfinpyrazone, INDOM:indomethacin, GENIS: genistein, PGA2: prostaglandin A2, CCCP: chlorocarbonylcyanide phenylhydrazine. (Reproduced from reference- 4)394
Part-IIIAdvances Dihydropyridines and …3C: Fluorescent Compounds for the functional detection of multi drug resistance.Abbreviations: CA-AM: calcein AM, FL-3-AM: fluo-3AM, Pot. Dyes:potentiomeric dyes, RH123: rhodamine123, HST: Hoechst dye No. 33342, GS-N-PM: N-Pyrenemaleimide glutathione conjugate, BOD-VER: BODIPY verapamil,BOD-PRAS: BODIPY prazosin, MX: mitoxantrone, LYS: LysoTracker dye.(Reproduced from reference-4)Figure-3. Venn-diagram for selected compounds interacting with the key MDR-relatedABC transporters.1.4.4 Cellular and Tissue Distribution of MDR-ABC TransporterThe tissue distribution of the MDR-ABC proteins is as varied as their substratespecificity. MRP1 is almost ubiquitously expressed, while the expression of Pgp is morerestricted to tissues involved in absorption and secretion. 8-11 High level MDR1 expressionhas also been shown in certain pharmacological barriers of the body, such as the bloodbrainbarrier (BBB) and the choroid plexus. 44,45 It has been reported that MXR is highlyexpressed in the placenta, liver, and most interestingly, in various stem cells. 34-46 Allmultidrug transporters are localized predominantly in the plasma membrane. In polarizedcells, Pgp-MDR1 is localized in the apical (luminal) membrane surface (e.g. in theepithelial cells of the intestine and the proximal tubules of kidney, or in the biliarycanalicular membrane of hepatocytes). 47-49 In contrast, MRP1 expression in polarizedcells is restricted to the basolateral membrane. The expression of MRP2, MDR3, and ofSister Pgp (BSEP) is predominant in the canalicular membrane of hepatocytes, whileMRP3 and MRP5 are expressed in the basolateral membranes of these cells (Figure 4).MRP2 is also highly expressed in the apical membranes of kidney proximal tubules. Inpolarized cells, the MXR expression was reported to be mostly apical. 50395
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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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Specimen IR spectra of some 2-chlor
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Part-IIResults and Discussion1 H NM
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Page 403 and 404: 4.6 References:Part-IIResults and D
Page 405 and 406: 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
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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Part-IIIAdvances Dihydropyridines a
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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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