Abstract
Our goal in this research, some new nucleoside analogues was synthesized. Starting from ?-D glucose which was converted to per acetylated ?-D gluco pyronoside then converted to active from(1-Bromo Sugar (2) as a sugar moiety.The base moiety 2-substituted benzimidazole was prepared from condensation of phenylene diamine with different aromatic aldehydes, which were subjected to amino alkylation via Mannich reaction forming new nucleobase derivatives. Condensation of nucleobase with bromo sugar through nucleophilic substitution of anomeric carbon with nitrogen forming new protected nucleoside analogues then hydrolyzed with sodium methoxide in methanol to obtain our target, the free nucleoside analogues. All prepared compound were identified by FT-IR Spectroscopy and some of them with H1 –NMR and C13-NMR Spectroscopy. The synthesized nucleoside analogues were screened for their antibacterial activity in vitro against four types of bacteria including, Bacillus Staphylococcus, aureus (Gram Positive), E.Coli and Pseudoman as (Gram Negative).Also were screened against four types of Fungi (Aspergines flurs, Aspergillus fumgntnts, Aspergillus niger and pencillum).
Highlights
Nucleoside analogues have proven to be a highly successful class of anti-viral[1], anti-cancer,anti-tumerand chemotherpeutic agent[2]
Nucleosides have sixmembered carbohydrate moiety have been evaluated for their potential antiviral[3], and antibiotic properties, as building block in nucleic acid Synthesis[4]
Benzimidazole ring is an important pharmaccophore in modern drug discover [5], compounds that exhibit functionality of benzimidazole and Its derivatives have been used in the area of pharmaceutical[6], these good and high profile applications of compound with benzimidazoles structures have prompted extensive studies for their method of synthesis
Summary
Nucleoside analogues have proven to be a highly successful class of anti-viral[1], anti-cancer,anti-tumerand chemotherpeutic agent[2]. Nucleosides are large class of agents that include drugs for several diseases. The Synthesis and development of glycosidase inhibitors have been the focus of attention, because of their vital role played by carbohydrates invairety of biological processes. Benzimidazole ring is an important pharmaccophore in modern drug discover [5], compounds that exhibit. Modifications of the benzimidazole ring System that have made the studies of anthelmintic activity have provided [7]. The most active drugs for anti-cancer, anticoagulant [8], anti-viral [9], anti-inflammatory, antihypertensive and anti-tumor [10]. Based on the above significances, our research focus on synthesis of new nucleoside analogues containing 2-. Substituted benzimidazole as anucleobase through Mannich base [11]
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