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After careful study of Structure Activity Relationship, a fresh libraries of N1substituted 2-aminoimidazoles and N1-unsubstituted 2-aminoimidazoles have been synthesized and tested for anti biofilm activity. In Chapter-4 microwave assisted one pot protocol for synthesis of 2-aminoimidazole-triazoel framework has been described and all newly synthesized compounds were tested for antibiofilm activity. However activities of these calls of compounds are under pipeline. Chapter-5 entitled “Crystal and molecular structure analysis of DP-7: A new Multi Drug Resistance Reverter Lead Molecule” deal with crystal and molecular structure analysis. 3,5-Dibenzoyl-4-(3-methoxyphenyl)-1,4-dihydro-2,6-dimethyl pyridine (DP-7) has been shown to be a powerful P-gp inhibitor, almost devoid of cardiovascular effects, but capable of inhibiting liver CYP3A, thus it can be conclude that DP-7 is a good lead compound for the synthesis of new dihydropyridines. As DP- 7 demonstrated promising MDR activity, several scientific publications on this molecule appeared. However study of X-ray crystallography was done first time and presented in the current work. All newly synthesized compounds have been characterized by 1 H NMR, 13 C NMR and HRMS. Some representative copy of 1 H and 13 C NMR spectra also presented.
CONFERENCES/SEMINARS/WORKSHOPS ATTENDED “International Conference On The Interface of Chemistry-Biology In Biomedical Research” jointly organized by ISCBC and Birla Institute of Technology & Science, Pilani. February, 22-24, 2008 “National Workshop On Management And Use Of Chemistry Database And Patent Literature” organized by GUJCOST & Dept. of Chemistry of Saurashtra University, Rajkot, (Gujarat), February, 27-29, 2008. “A National Workshop On Updates In Process And Medicinal Chemistry” jointly organized by National Facility for Drug Discovery through New Chemicals Entities Development & Instrumentation support to Small Manufacturing Pharma Enterprises and DST FIST, UGC-SAP & DST-DPRP Funded Department of Chemistry, Saurashtra University, Rajkot March, 3-4, 2009. “National Conference On Selected Topics In Spectroscopy And Stereochemistry” organized by the Department of Chemistry, Saurashtra University, Rajkot, March, 18-20, 2009. “12th Belgian Organic Synthesis Symposium” (BOSS XII) Namur, Belgium July 11-16, 2010.
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Saurashtra University Re - Accredit
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JANUARY-2011 Statement under O. Ph.
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Acknowledgment This thesis arose in
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since I was a child. My Mother Hans
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CHAPTER - 2 Microwave Assisted Synt
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5.5 Results and discussion 156 5.6
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Ms Mesyl MW Microwave NBS N-bromosu
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1. Microwave Assisted Organic Synth
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1.4 Heating Mechanism In microwave
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1.5. Effects of solvents Every solv
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1.7 Application of microwave in org
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aromatic amines, Lancini’s group
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1.9 2-Aminoimidazole Alkaloids The
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Recently group of Erik 83 described
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1.10 Methods for the preparation of
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R 1 O X R 2 NH 2 H 2N NAc R 1 HN R
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this manifold, was reported in 1925
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Another route to 4(5)-acyl-2-amino-
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this series of compounds against th
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documented. Extra care is needed be
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Very recently the research group of
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OH a,b O N H2N N Boc N 3 H N R N N
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1.12.2 Biofilm Growth Cycle 1) Plan
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can survive both the onslaught of a
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[26] Leadbeater, N. E. (2004) Chemi
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[86] Kreutzberger, A. (1962) J. Org
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Microwave Assisted Synthesis & Stru
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2.1 Introduction As described in ch
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2.3 Proposed Mechanism: Regarding t
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No. 12 60 120 traces 84 a All react
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the development of biofilm related
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In first instance, a series of 2-hy
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Br N N N R 1 OH Br N N N R 1 OH Fig
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do have a very strong effect agains
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2.6 Conclusion In the present study
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2.8 Biological assays 2.8.1 Static
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2.9 Experimental protocol: 2.9.1 Ge
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temperature of 80 °C and a maximum
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29.5,29.4, 29.2, 27.0, 22.6, 14.1.
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Yield: 78 %. 1 H NMR (300 MHz, CDCl
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N Br N N C 14H 29 OH Yield: 72 %. 1
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(75.5 MHz, CDCl3): δ = 167.7, 154.
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N Br N N C 14H 29 OH Cl Yield: 90 %
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2-(3,4-Dichlorophenyl)-2-hydroxy-1-
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N Br N N C 8H 17 OH NO 2 Yield: 49
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C3H7 HN N N H Cl Cl Yield : 70 %. 1
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(s, 1H), 3.16 (s, 3H), 1.80 (m, 2H)
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5-(4’-Nitrobiphenyl-4-yl)-N-octyl
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2.11 Representative NMR spectra 2.1
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2.11.3 10.4329 0.7429 151.5720 10.0
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[21] Matz C, McDougald D, Moreno A.
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Chapter-3 Structure Activity Relati
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imidazoles, where the addition of a
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3.4 Result and Discussion It was fo
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No. H 2N Compound Code N N C8H17 R1
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medium used in the set-up to monito
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H 2N N N N H2N N R R Figure-1 Effec
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3.5.3 Cyclo-alkyl 2-aminoimidazoles
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3.6. Conclusion In the present stud
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3.8. Experimental protocols 3.8.1 G
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122.6, 54.6, 33.3(×2), 27.3 (×2),
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Yield: 52 %. 1 H NMR (300 MHz, CDCl
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5-(4-Chlorophenyl)-1-cyclooctyl-1H-
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Yield: 50 %. Mp: 76-78 ° C. 1 H NM
Page 131 and 132: 5-(4-Chlorophenyl)-1-cyclobutyl-1H-
Page 133 and 134: Yield: 66%. 1 H NMR (300 MHz, CDCl3
Page 135 and 136: 3.10 Representative NMR spectra 3.1
Page 137 and 138: 3.11 References [1] (a) Alvi K. A,
Page 139 and 140: Copper Catalyzed Microwave Assisted
Page 141 and 142: 4.1 Introduction There are only a f
Page 143 and 144: (Table-1, No- 6). Next reaction tem
Page 145 and 146: No. Product, Yield b (%) No. Produc
Page 147 and 148: 4.4 Possible Mechanism Regarding th
Page 149 and 150: 4.7 Experimental protocols 4.7.1 Ge
Page 151 and 152: Yield: 69 %. 1 H NMR (300 MHz, CDCl
Page 153 and 154: 1-(3-Azidopropyl)-2-(3,4-dichloroph
Page 155 and 156: Yield: 84 %. 1 H NMR (300 MHz, DMSO
Page 161 and 162: 1H), 1.66 (m, 6H), 1.70 (m, 2H). 13
Page 163 and 164: 5.48 Hz, 2H), 3.59 (m, 2H), 3.16 (d
Page 165 and 166: 4.10 References [1] For a general r
Page 167 and 168: Crystal and Molecular Structure Ana
Page 169 and 170: 5.1 Introduction The membrane efflu
Page 171 and 172: oscillation range of 5˚ and proces
Page 173 and 174: C12-C13 1.372(4) C32-C37 1.390(3) C
Page 175 and 176: Fig.-3: Packing of the molecules wh
Page 177 and 178: 1 H NMR (400 MHz CDCl3): δ = 7.57-
Page 179 and 180: 5.9.2 13 C spectra of bs-DP-7
Page 181: SUMMARY The work represented in the
Page 185: PUBLICATIONS [1] One-Pot Microwave-
Page 200 and 201: Scheme 2 Competitive formation of 1
Page 202 and 203: Table 2 continued 9 10 11 12 N hydr
Page 204: 8. Colson G, Raboult L, Lavelle F,
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