98 Medicinal Chemistry, 2013, Vol. 9, No. 1
Kulkarni et al.
~2930 (ꢂ, -CH3, str), ~1760 cm-1 (ꢂ CO str), 1600 cm-1 (ꢂ NH
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bend). 1H NMR (DMSO d6) ꢁ (ppm): 11.8 (br. s, 1H, amide
ꢁ
NH), 10.0 (br. s, 1H, NH benzimidazole), 8.25 (d, 2H, C ,
3
ꢁ
ꢁ
ꢁ
C 5 aromatic), 8.17 (d, 2H, C 2, C 6, aromatic), 7.85 (s, 1H,
C4 benzimidazole), 7.7 (d, 2H, C6, C7 benzimidazole), 7.33
ꢀ
ꢀ
ꢀ
ꢀ
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(d, 2H, C 2, C 6, aromatic), 7.1 (d, 2H, C 3, C 5,aromatic), 3.75
(s, 3H, OCH3). ESI-MS (m/z): 389 [M+H] +.
[15]
[16]
CONCLUSION
In summary, we have identified 5-substituted benzoyl-
amino-2-substituted phenylbenzimidazoles as new p38
kinase inhibitors. The initial SAR reveals that compounds 7b
and 7c were found to be moderately active in both models.
Substitution at both R and R1 may not be effective however
compound 7j exhibited activity which contradicts our
explanation. New molecules with diverse substitution at R1
and methoxy group at R may help to understand incites of
SAR.
[17]
[18]
[19]
CONFLICT OF INTEREST
Author RG thank AICTE for granting fellowship for
carrying this project under quality improvement program.
ACKNOWLEDGEMENTS
The authors acknowledge Dr. G Narahari Sastry,
Scientist, Molecular Modelling Group, and P. Srivani, re-
search scholar, IICT, Molecular Modelling Group Hydera-
bad for their help in molecular docking studies. RGK express
thanks to Dr. V J Rao Scientist, Organic III, IICT, Hydera-
bad, for constructive ideas in solving the difficulties during
the synthesis of molecules.
cell
lines,
by
amine-substituted
2-arylbenzimidazole-4-
carboxamide PARP-1 inhibitors. Bioorg. Med. Chem. Lett., 2004,
14, 2433-37.
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Sondhi, S.; Singh, N.; Kumar, A.; Lozach, O.; Meijer, L. Synthesis,
anti-inflammatory, analgesic and kinase (CDK-1, CDK-5 and
GSK-3)
inhibition
activity
evaluation
of
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