Strong activity against hbv replication and low cytotoxicity were generally observed in these benzimidazoles. Pdf synthesis and antimicrobial activity evaluation of. Mothukuri bg, settypalli t, begari n, dalavai vk, chunduri vr 2019 synthesis and antibacterial activity of novel benzimidazole linked 1,3,4oxadiazole derivatives. Structures of the synthesized compounds were elucidated by 1hnmr, ir and esms spectral data and elemental analysis. Antimicrobial potential of 1 h benzo d imidazole scaffold. The synthesized compounds were screened for their antimicrobial activity against b. Synthesis and antibacterial activity of novel benzimidazole. Antioxidant and antifungal properties of benzimidazole. Synthesis, characterization and antibacterial evaluation. Among them, compounds i, ii, iii and iv exhibited good antimicrobial activity. Synthesis of benzimidazole derivatives containing schiff base exhibiting antimicrobial activities. Benzimidazole derivatives have shown hopeful activity in the treatment of several diseases, for this reason, the synthesis of novel benzimidazole remains a main focus for researchers. It was further converted as substituted benzimidazole derivatives with yield between 7080%. Finally, it could be pointed out that generally high and wide spectrum of antibacterial activity was exhibited by compound 21a of the.
Department of chemistry, bundelkhand university, jhansi u. Synthesis and antimicrobial activities of some bridged bis. The melting points of all synthesized compounds were found in open capillary tubes and readings were given in table. Synthesis and evaluation of 2aryl substituted benzimidazole derivatives bearing 1,3,4oxadiazole nucleus for antimicrobial activity archana kapoor and naiya dhiman drug discovery and research laboratory, department of pharmaceutical sciences, guru jambeshwar university of science and technology, hisar haryana, india. A structureactivity relationship sar study including some electronic parameters was carried out and a connection between antibacterial activity and electronic properties of the target compounds was determined.
Antimicrobial activity and a sar study of some novel. Synthesis and evaluation of selected benzimidazole. The present work deals with the identification of potent benzimidazole derivative using antimicrobial studies. Synthesis and antimicrobial studies of substituted 2. Antimicrobial and antibacterial activity a series of 1, 2disubstituted1hbenzimidazole n alkylated 5carboxamidine derivatives are very potent antibacterial activities against s. Synthesis, characterization and antimicrobial properties. In this paper, we report on the synthesis of a series of benzimidazole derivatives and their antimicrobial activity. Synthesis and antimicrobial activity of benzimidazole derivatives 1519 benzimidazoles 12a,b improved the potency against escherichia coli superior to that of the standard gentamycin. In some previous papers,, we reported the synthesis and antimicrobial activity of some benzimidazole 56carboxamido and 41hbenzimidazol2ylbenzamide derivatives. Journal of chemical and pharmaceutical research, 2017, 98. The fascinated biological activity of benzimidazole and its derivatives are seen against many human pathogens and microbial attacks. Nowadays infectious microbial diseases are causing problems worldwide, because of resistance to no. Synthesis and antimicrobial activities of some new.
Some new 2azetidinone derivatives possessing benzimidazole nucleus were synthesized and characterized by ir, nmr and mass spectral analysis. Pdf synthesis and antimicrobial activity evaluation of some. Benzimidazole derivatives as potential antimicrobial and antiulcer agents. Microwaveassisted synthesis of some new benzimidazole. Pharmacological activities benzoxazole is an aromatic organic compound with a molecular formula c7h5no, a benzene fused oxazole ring structure, and an odour similar to pyridine. The novel heterocycles were characterized by melting point range, r f value, ir, nmr and mass spectral analysis. Among various benzimidazole derivatives, promising biological.
Twenty eight analogues of benzimidazoles had been synthesized and tested for their antimicrobial activity against four bacteria staphylococcus auerus, escherichia coli, bacillus pumilus and proteus vulgaris and two fungi aspergillus flavus and aspergilus niger. The synthesis of novel benzimidazole derivatives remains a main focus of medicinal research. All the compounds showed moderate to good antimicrobial activity and anti fungal activity. Benzimidazole, a bioactive heterocyclic compound that contain nitrogen and benzene ring fused at 4,5positions of imidazole. Benzimidazole derivatives have found the application in diverse therapeutic areas including antiulcers, antihypertensive, antiviral, antifungal, anticancer, anti histaminics 3, antitublercular 4, antiallergic 5. Synthesis, characterization and evaluation for antimicrobial. Again a new series of benzimidazole derivatives bearing various benzazolylthio moieties were synthesized by the same group of researcher and screened them for their antimicrobial activity by using e. Substituted benzimidazoles, antimicrobial activity, antifungal.
Department of chemistry, faculty of arts and sciences, recep tayyip erdogan university, rize, turkey. Introduction benzimidazole derivatives are very useful intermediates or subunits of the development of pharmaceutical or biological interest. Dec 16, 20 finally, compound 4 was treated with 11 different aromatic aldehydes to obtain benzimidazole derivatives containing imine function. Antimicrobial activity of benzimidaz ole derivatives against microorganism with zone of inhib ition mm compounds code e. Synthesis, characterization and antimicrobial activity of 2. Antimicrobial activity of benzimidazole authorstream. Toxicity of the most effective compounds was established by performing brineshrimp lethality assay.
A series of novel benzimidazole derivatives was synthesized and evaluated for their antihepatitis b virus hbv activity and cytotoxicity in vitro. Antibacterial activity of benzimidazole derivatives. Synthesis and biological activity of novel 2, 5disubstituted. Benzimidazolecontaining compounds have numerous medical and biological activities, such as antitumor 6 antibacterial 710, antifungal 11. Synthesis and antimicrobial activity of some novel n. A detailed study of the structureactivity relationship of these derivatives will pave the road to.
Design, synthesis, antitubercular and antimicrobial. Benzimidazole derivatives as potential antimicrobial and. The first one comprise methyl, the second one comprise of 2 phenyl substitution on benzimidazole moiety. Introduction benzimidazole is a heterocyclic aromatic organic compound. The most promising compounds were 12a and 12b, with similar high antiviral potency ic50 0. Due to antimicrobial importance of benzimidazoles and hydrazones, some benzimidazolehydrazone compounds were synthesized to screen their antimicrobial activity.
Benzimidazole, antimicrobial activity, anthelmintic activity, ampicillin, nalidixic acid, piperazine citrate. Thus, the necessity of this study for the syntheses of more derivatives of benzimidazole and their metal complexes as possible antimicrobial agents. In case of gram negative bacteria, 3c showed moderate activity against e. The antimicrobial potentials of the investigated benzimidazole derivatives are similar to those of different benzimidazoles that were determined in the previous studies 24, 1014. Synthesis and antimicrobial activity of some new 1,2,4. Benzimidazole and its derivatives are used as bioactive molecules in drug and pharmaceutical research sectors. Carbohydrazide 1 was reacted with ethyl acetoacetate. The synthesized benzimidazolehydrazones exhibited very weak antibacterial activity.
Finally, the key intermediate 16 was alkylated with benzyl chloride in aqueous sodium hydroxide. Pdf synthesis of benzimidazole derivatives containing schiff. However, antifungal activity of some of the synthesized compounds was very notable against candida species. The synthesized benzimidazole hydrazones exhibited very weak antibacterial activity. Reaction of 32methylbenzimidazol1ylpropanoic acid hydrazide 1 with cs2koh gave oxadiazole 2 which underwent mannich reaction to give 3. Synthesis and evaluation of selected benzimidazole derivatives as.
Ali mohd ganie, ayaz mahmood dar, fairooz ahmad khan and bashir ahmad dar affiliation. The study of antibacterial activity of benzimidazole derivative. Synthesis and antimicrobial activity of some new benzimidazole derivatives dhaval j. Nalkyl and nacyl derivatives of 24 thiazolyl1hbenzimidazole 3. They used 9 bacterial strains of following bacteria e. A green and convenient approach toward benzimidazole. Microwaveassisted synthesis of some new benzimidazole derivatives with their antimicrobial activity authors. Synthesis and antihepatitis b virus activity of novel. A detailed study of the structure activity relationship of these derivatives will pave the road to. Synthesis and antimicrobial activity of certain benzimidazole. Pdf synthesis and antimicrobial activity of some new. Emre e mentes, department of chemistry, faculty of arts and sciences, recep tayyip erdogan university, rize, turkey. International journal of drug research and technology. Again a new series of benzimidazole derivatives bearing various benzazolylthio moieties were synthesized by the same group of researcher and screened them for.
Benzimidazole, schiff base, antimicrobial activity, staphylococcus aureus, synthesized 1. Synthesis of benzimidazole 2 benzimidazole was prepared according to the reported literature. Synthesis and antimicrobial studies of novel benzimidazole. Introduction benzimidazoles are remarkably effective compounds both with respect to their. Conclusion present study reveals that benzimidazole derivatives plays important role in medicinal field with their antimicrobial activity. The results displayed that, when there are nitro or dichloro substitutents at 5 andor 6position of the benzimidazole moiety and p. Evalution and molecular docking of benzimidazole and its. The effect of the structure of the ligands and complexes on the antimicrobial activity is discussed. The azetidinone ring bearing compounds showed varied biological. Some of the newly synthesized compounds showed moderate antimicrobial activity against some tested. On the basis of data it is clear that 2methylbenzimidazole and its derivatives possesses moderate. Based on these findings, and in continuation of our drug research program concerning synthesis of new, safer and more biologically active compounds, it was of interest to synthesize a new series of benzimidazole coupled pyrazole derivatives with the hope to obtain more active and lesstoxic antimicrobial agents. Antibacterial evaluation of some benzimidazole derivatives. Carbohydrazide 1 was reacted with ethyl acetoacetate, acetylacetone and aldehydes to give 7, 8.
Synthesis and invitro antimicrobial activity of some novel substituted benzimidazole derivatives having potent activity against mrsa. The reported method, overcoming the inactivation of palladium under the equivalent nitrogenous conditions, has the advantages of convenient. The synthesized benzimidazolehydrazones exhibited very weak. Furthermore, the bioactivity of benzimidazole derivatives containing electrondonating group on the phenyl group was superior to that of electronwithdrawing group, and especially 5,6dimethyl substituents benzimidazole derivative 3c exhibited higher inhibitory activity against b. Department of pharmaceutical chemistry, delhi institute of pharmaceutical sciences and research dipsar, sector3, pushp vihar, new delhi110017, india some new 2substituted benzimidazole derivatives were synthesized from microwave. Synthesis of benzimidazole derivatives containing schiff. On the basis of data it is clear that 2methylbenzimidazole and its derivatives possesses moderate antibacterial activity. Benzimidazole and its derivatives interact easily with biopolymers and promise to be forming good systems for the development of biologically active compounds with structural similarity to vitaminb12 derivatives. Introduction benzimidazoles and its derivatives represent one of the most biologically active class of. Antiinflammatory synthesis and antiinflammatory activity of phenyl benzimidazole 1 was reported by. Synthesis and antimicrobial activity evaluation of some benzimidazole and indole derivatives article pdf available in african journal of microbiology research 717. Pdf antimicrobial activity and a sar study of some novel. Benzimidazoles were reported to have antimicrobial properties 1 against bacteria or fungi.
In the past few decades, benzimidazole and its derivatives have received much attention due to their chemotherapeutic values. A new series of 2, 5 disubstituted benzimidazole derivatives have been. Antimicrobial properties of benzimidazole and mannich. Experimental and qsar studies on antimicrobial activity of. The broad umbrella of antimicrobial activity comprises antibacterialof, antifungal, antiviral and antiparasitic agents. A series of novel 5amino1,3,4thiadiazole2thiol and 1,3,4thiadiazole2,5dithiol derivatives of benzimidazole were synthesized through nucleophilic substitution reaction of 5substituted2chloromethyl1hbenzimidazole, structures of the synthesized compounds were proved by spectral methods of analysis ftir, 1 h and c nmr.
Heterocyclic species like benzimidazole derivatives have received much interest in the field of medicinal chemistry because of its synthetic utility and broad spectrum of biological activity. Finally, compound 4 was treated with 11 different aromatic aldehydes to obtain benzimidazole derivatives containing imine function. The synthesized benzimidazole derivatives showed remarkable antioxidant activity furthermore their effects on various antioxidant enzymes are discussed and evaluated from the perspective of structureactivity relationships. The synthesis of benzimidazoles from 1, 2diamino compounds and. Again a new series of benzimidazole derivatives bearing various benzazolylthio moieties were synthesized by the same group of researcher and screened them for their antimicrobial activity by. Two series of novel benzimidazole derivatives were synthesized. Bisbenzimidazole derivatives, antibacterial activity, antifungal activity introduction despite signi. Synthesis and antimicrobial evaluation of benzimidazole. The novel benzimidazole derivatives 3, 5, 8, 9, 1214, 1841 were prepared in this paper and the antimicrobial activities of these compounds against staphylococcus aureus, methicillinresistant. The resulting solution was cooled and made alkaline to litmus with 10% sodium hydroxide solution. The complexes were found to be more toxic than the ligands.
Antimicrobial activity of 2substituted benzimidazole derivatives kuldeep kumar1, prof. Antimicrobial activity and a sar study of some novel benzimidazole derivatives bearing hydrazone moiety. Eisa et alsynthesis and antimicrobial activity of benzimidazole derivatives 1517 of the cyclized structure was obtained from the absence of ester band in ir, and by 1h nmr, mass spectrometry and elemental analysis scheme ii. Substituted benzimidazoles, chemistry, antimicrobial activity. In this study, 16 benzimidazole and indole derivatives were synthesized and tested for in vitro antimicrobial activity by tube dilution and disc diffusion susceptibility test methods. In this investigation, as a continuation on the synthesis of antimicrobial benzimidazoles, it was planned to modify the amide. Some new 2azetidinone derivatives possessing benzimidazole nucleus were synthesized and characterized by io, kmr and mass spectral analysis. Nalkylated benzimidazole derivatives have been synthesized via the azamichael addition reactions of 1hbenzimidazoles to. All reactions were carried out with microwave irradiation and conventional heating, and results were compared. All synthesized compounds were screened for antimicrobial activity using cup plate method. Antimicrobial properties of benzimidazole and mannich bases. Microwaveassisted synthesis of some new benzimidazole derivatives with their antimicrobial activity volume. Benzimidazole, hydrazine hydrate, azomethine, antimicrobial activity monitored by tlc and the structures of all the derivatives were assigned by. Synthesis, characterization and antimicrobial activity of.
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