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Part-A Studies on 2-methyl indoline derivatives…..
128
Zhao et. al. optimized the lead compound 2-[-4-(4chlorobenzyl)piperazin-1-yl]-1-(2,
3-dihydroindol-1-yl) ethanone by systematic
structure-activity relation (SAR) studies and synthesized numbers of Nsubstituted
(substituted-piperazinyl) 2-methyl indoline derivatives which led to
the two potent compounds, 2 - [4 - (4 - chlorobenzyl) piperazine – 1 - yl] – 1 -
(2 – methyl - 2, 3-dihydroindol – 1 - yl) ethanone and 2 - [4 - (4 -
chlorobenzyl)piperazine – 1 - yl] – 1 - (2 – methyl - 2, 3 – dihydroindol – 1 -
yl)ethanone as mixed D2/D4 receptor antagonists.
Tyunova et. al. 129 developed a convenient and efficient protocol for the
synthesis of combinatorial library of 3-(2-thieno-sulfonyl) propionylamides.
The synthetic route involved initial sulfochlorination of thiophene (or 2bromothiophene),
conversion of the resulting sulfochlorides into sulphinates
followed by their reaction with acrylic acid. The resulting
thienosulfonylpropionic acids were converted into the corresponding acid
chlorides, which were used for acylation of primary and secondary aliphatic,
aromatic and heteroaromatic amines. Several physico-chemical molecular
parameters were calculated for the synthesized compounds, related to their
potential pharmacokinetic profile.
Bordon et. al. 130 synthesized new 2-methyl indoline derivatives (1) [Y =
N, O, S, CHR 3 , CR 3 ; the dotted lines = single or double bond; R, R 1 = H, halo,
OH, alkyl, alkoxy, CN, NO2, NR 4 R 5 , CF3, CF3O, aryl, heteroaryl, S(O)nNR 4 R 5 ;
n = 0 - 2; R 3 = H, halo, alkyl, CN, NO2, NR 4 R 5 , CF3, aryl; R 2 = R 4 , OR 4 , SR 4 or
NR 4 R 5 ; R 4 = H, alkyl, cycloalkyl, aryl; either R 4 and R 5 is selected among the
values of R 4 or heterocyclic containing N, O and S, all optionally substituted],
these products being in all the isomer forms - racemates, enantiomers or
diastereomers - and pharmaceutically acceptable salts, for use as drugs.
Thus, trans-N-[6-(5, 6-dichloro-1H-benzimidazol-1-yl) 9H-purin-2-yl]-1, 4cyclohexanediamine
(2-HCl) was prepared, from 2, 6-dichloropurine via
amination with 5, 6-dichloro-1H-benzimidazole in butanol followed by fusion
with trans-1, 4-diaminocyclohexane. The protein kinase inhibitory activity of
(2) as hydrochloride was detected [IC50 = 1.3 µM vs CIV-CDK; 98% inhibition
SRC kinase at the rate 20 µM; 93% inhibition CDK1 at the rate 20 µM; 98%
Department of Chemistry, Saurashtra University, Rajkot – 360 005 24