DESIGN AND SYNTHESIS OF 2-SUBSTITUTED-1HBENZIMIDAZOLE- 4-CARBOXAMIDES AS INHIBITORS OF POLY (ADP-RIBOSE) POLYMERASE-1 (PARP-1)
Kalam Bhupathi Reddy, Kiran Kumar Murahari, Sunitha Kanakam, Kombu Subramanaian Rajan, Gangula Mohan Rao, Baru Vijaya Kumar*
ABSTRACT
Novel 2-subtituted-1H-benzimidazole-4-carboxamide poly (ADPribose)
polymerase-1 (PARP-1) inhibitors have been synthesized by
treating 2-(trichloromethyl)-1H-benzo[d]imidazole-4-carboxamide (4)
with various amines in acetonitrile medium using potassium carbonate
as base. The compound 4 was synthesised from 2-amino-3-
nitrobenzoicacid (1). All the synthesized compounds have been
characterized by 1H NMR and Mass spectral data together with
elemental analysis. The synthesised compounds (6a-6f) were screened
for PARP-1 inhibitory activity. Among these 5a (IC50= 31nM) and 5b
((IC50= 51nM)) were highly active PARP-1 inhibitors.
Keywords: 1H-benzimidazole-4-carboxamide, PARP inhibitors, IC50.
[Download Article]
[Download Certifiate]