SYNTHESIS OF NOVEL IMIDAZOLE AND FUSED IMIDAZOLE DERIVATIVES AS CYTOTOXIC AND ANTIMICROBIAL AGENTS: MOLECULAR DOCKING AND BIOLOGICAL EVALUATION
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2015, Vol 7, Issue 11
Abstract
Objectives: The objective of this work is to synthesize novel imidazole and fused imidazole derivatives using 5-arylidene-2-hydrazino-3-phenyl imidazolin-4-ones (5a-c) as key intermediate. The structure of the newly synthesized compounds was characterized using IR, 1HNMR, Mass spectroscopy, elemental analysis and some representative 13CNMR.Methods: The target compounds were synthesized starting from 5-arylidene-2-hydrazino-3-phenyl imidazolin-4-ones (5a-c) which prepared from the appropriate 5-arylidene-2-(methylthio)-3-phenyl imidazolin-4-ones (3a-c). Several synthetic pathways were be used for the preparation of the targets. Some of the newly synthesized compounds were evaluated for their cytotoxic activity against breast carcinoma and colon carcinoma cell lines. On the other hand, the antimicrobial activity evaluation of some newly prepared compounds was performed using cup plate diffusion method.Results: Compound 5c was the most active one against breast carcinoma (IC50=3.3 ug/ml) and colon carcinoma cell lines (IC50=4.73 ug/ml) when compared with doxorubicin as standard. Molecular docking studies further supported the highest potency of 5c and further help understanding the various interactions between the ligand and enzyme active sites. On the other hand, the antimicrobial activity evaluation showed that most of the evaluated compounds exhibited broad spectrum activity.Conclusion: The present work led to the development of promising antitumor compounds containing substituted imidazolidin-5-one or imidazotriazol-6-one skeletons. Compounds 5c showed the highest potency at low µg/ml level against breast MCF-7 and colon HCT116 cell lines. On the other hand, most of the newly synthesized compounds showed broad spectrum antimicrobial activity when cup plate diffusion method was performed.Â
Authors and Affiliations
Eatedal H Abd El-aal, Hanan A Abdel Fattah, Nermine A Osman, Israa A Seliem
ANTIBACTERIAL ACTIVITY OF BIOLOGICALLY SYNTHESIS SILVER NANOPARTICLES FROM LEAF EXTRACT OF ALANGIUM SALVIFOLIUM (L.F) WANG
Biologically Synthesis process of silver nanoparticles using plant extract is simple, cost-effective, and ecofriendly. In the present study, silver nanoparticles (AgNPs) were rapidly synthesized using Alangium salvifoliu...
A FAST AND SENSITIVE SPECTROPHOTOMETRIC METHOD FOR THE DETERMINATION OF HYDRAZINE IN ATAZANAVIR SULFATE DRUG SUBSTANCE
Objective: To develop a fast and sensitive UV spectrophotometric method for the quantitative estimation of Hydrazine in Atazanavir Sulfate drug substances and validate as per ICH guidelines.Methods: The method was based...
PRELIMINARY INVESTIGATIONS INTO THE PHYSICOCHEMICAL AND COMPACTION CHARACTERISTICS OF MODIFIED STARCH OF DISCOREA ALATA USING DICLOFENAC SODIUM TABLET
Objective: This work focused on evaluating the micromeritic and compressional properties of pregelatinized African water yam (Discorea alata) starch and its modified forms with comparison to pregelatinized corn starch an...
PHYSIOCHEMICAL EVALUATION AND IN VITRO ANTIOXIDANT ACTIVITY OF FEW WONDER SEEDS
Objective: This study was an attempt to compare and investigate the physiochemical nature and antioxidant potential of few wonder seeds namely flaxseed, chia, sesame, pomegranate, dill, kalonji, pumpkin and watermelon se...
VITAMIN D DEFICIENCY AND DEPRESSIVE DISORDERS: REVIEW STUDY OF PROBABLE RELATIONSHIP
Vitamin D deficiency is evident in many parts of the world, even in the sunnier regions, for a variety of reasons. Recently, vitamin D has been reported in many scientific researchers as an important factor that may hav...