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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