IN SILICO DRUG DESIGN,MOLECULAR MODELLING,SYNTHESIS AND CHARACTERIZATION OF NOVEL BENZIMIDAZOLES

摘要

Benzimidazole and its scaffolds are considered as an important heterocyclic motif containing two annular nitrogen atoms of bicyclic compound fused with benzene to imidazole ring established and obtained in many synthetic and natural compounds.In recent years,a few marketed drugs containing 1,2,5-trisubstituted benzimidazoles have shown extensive interest with anticancer(Bendamustine),antifungal(Benomyl),analgesic(Etonitazine),antihypertensive(Telmisartan)and antihistaminic(Norastemizole)activities etc,as shown in Figure 1.It also exhibits varied pharmaceutical applications resembling antibacterial,1 antifungal,2 anti-inflammatory,3 antitumor,4 anthelmintic,5 antihypertensive,6 anti-HIVs,7 antiulcer,8 anti-convulsant,9 and anti-diabetic10 activities.In addition,most of the drugs have substitution at 2nd and 5th position at the benzimidazole core.Moreover;at these two positions,substitutions of the benzimidazole moiety were recognized as fundamental for potency of receptor binding and receptor activation.