Abstract
The present research work was aimed to synthesize some Mannich bases of benzo1,3-diazole dervivatives and was investigated for their biological activities. The newly synthesized compounds have been characterized by their analytical and spectral (IR, 1HNMR, Mass spectra) properties. All the compounds have been screened for their antitubercular activities by standard methods. Antitubercular study revealed that Both BZ2 and BZ5 have promising activity.
 Keywords: Benzo1,3-diazole, o-phenylenediamine, urea, benzamide, Hydroxylamine, Antitubercular activity.
Highlights
N anti tubercular and anti fungal activity were evaluated
2.2.1 Synthesis of benzo1,3-diazole derivatives The different 2-(2 or 5 – substituted) phenyl benzo1,3-diazole derivatives were prepared as reported in the literature. ( Linga S et al 2011). 2.2.2 Synthesis of 1-{[2-4-methoxyphenyl)- 1-H benzimidazol-1-y1]methyl} urea (BZ1) Formaldehyde (0.05 mol) was added slowly to 0,05 mol of 2-( 4-methoxy phenyl ) 1-H Benzimidazole and 0.05 mol of urea in 15 ml of ethanol, with continuous stirring for 1 hour and refrigerated
The mannich bases of benzimidazole derivatives were designed using CADD, of which eight derivatives satisfying the required criteria were synthesized as depicted in scheme
Summary
Benzo1,3-diazole is a bicyclic heterocyclic system consisting of two nitrogen atoms and fused phenyl ring. Benzo1,3-diazole derivatives dervatives take part in a vital role in biological fields such as antitubercular, antineoplastic, antiviral, antioxidant, anticonvulsant, antiinflammatory, antibacterial and antifungal activities. The synthesis of newer benzimidazole derivatives remains a main center of attention of medicinal research (Hubschwerlen.C et al 1992). Latest observations imply that substituted benzo1,3-diazole and heterocycles, which are the structural isoster’s of nucleotides owing fused heterocyclic nuclei in their structures that allow them to interact with the biopolymers, posses potential activity with lower toxicities in the chemotherapeutic approach in man. As an outgrowth of our investigation to discover novel antitubercular and antifungal agents a new series of 1, 2 disubstituted benzimidazole analogs were synthesized and both
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