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Part-A Studies on 2-methyl indoline derivatives….. inhibition ZAP kinase at the rate 20 µM; 93% inhibition casein kinase (2) at the rate 20 µM; 100% inhibition AKT kinase at the rate 20 µM; IC50 = 2 µM vs FAK kinase; IC50 = 0.84 µM vs JNK3 kinase]. (Fig. A.12) Fig. A.12 Gonzales et. al. 131 synthesized different N-(4-sulfamoylphenyl) amide derivatives of 2-methyl indoline as voltage-gated sodium channels inhibitors. Dehmlow et. al. 132 reported preparation of indolyl hexafluoropropanols as Live-X-Receptor (LXR) modulators for the treatment of diabetes and related diseases. The invention relates to compounds (1) [wherein R 1 - R 6 = H, alkyl, etc.; A = (un)substituted aryl or heterocyclyl; m, p = 0-3; n = 0 or 1; R 3 and R 4 are absent when a is a double bond, with limitations, and pharmaceutically acceptable salts and esters thereof], their pharmaceutical compositions, processes for their preparations, and their use in the treatment and prophylaxis of diseases modulated by LXRα and/or LXRβ agonists, such as diabetes. For instance, (2), which showed IC50 values of 0.02 µM and 0.006 µM against LXRα and LXRβ, respectively, in the binding assay, was synthesized in multiple steps from 2-methyl-2,3-dihydro-1H-indole, hexafluoroacetone sesquihydrate and methyl-3-(chloromethyl) benzoate. (Fig. A.13) Fig. A.13 Department of Chemistry, Saurashtra University, Rajkot – 360 005 25
Part-A Studies on 2-methyl indoline derivatives….. Literature also revealed different synthetic methodologies 133-143 for the synthesis of N-substituted-2-methyl indoline derivatives. A.2.4 MANNICH REACTION ON 2-METHYL INDOLINE Abonia et. al. 144 in their effort to synthesize pyrroloquinolines, synthesized 1-(benzotriazol-1(2)-ylmethyl)indolines for which they carried out Mannich reaction on 2-methyl indoline using benzotriazole as a secondary amine, formaldehyde and diethylether as a solvent and stirred for 30 minutes at room temperature. This Mannich base was reacted with unactivated and electron-rich alkenes in the presence of p-toluenesulfonic acid catalyst to give pyrroloquinolines but the pharmacological importance of the synthesized molecules was not reported. Department of Chemistry, Saurashtra University, Rajkot – 360 005 26
Page 1 and 2: Saurashtra University Re - Accredit
Page 3 and 4: Statement under O. Ph. D. 7 of Saur
Page 6 and 7: ACKNOWLEDGEMENT It is a moment of g
Page 8 and 9: Jignesh Lunagariya, Hitesh Sarvaiya
Page 10 and 11: CONTENT Content General Remarks 6 A
Page 12 and 13: Content 3.2 Reaction scheme 149 3.3
Page 14 and 15: 5.14 Conclusion 313 5.15 Spectral r
Page 16 and 17: MF Molecular Formula MW Molecular W
Page 18 and 19: GABA Gamma Amino Butyric Acid MES M
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Page 22 and 23: Part-A Studies on 2-methyl indoline
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Chapter - 2 Microwave assisted simp
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Part - B Studies on isatin derivati
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CHAPTER - 3 PREPARATION OF SMALL LI
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Chapter - 3 Preparation of small li
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CHAPTER - 4 STUDIES ON DIFFERENT TY
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Chapter - 4 Studies on different ty
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Chapter - 5 Synthesis and Character
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Chapter - 6 Biological evaluation o
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Summary Synthesis and biological pr
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Summary Synthesis and biological pr
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Conferences / Seminar / Workshop At
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