Synthesis and reactivity in inorganic, metalorganic, and. Iodine is a commercial and environmentally benign catalyst. Synthesis, reactions and biological activity of quinoxaline. Synthesis and biological activity of some heterocyclic compounds containing benzimidazole and betalactam moiety. The small and simple benzothiazole nucleus if present in compounds involved in research aimed at evaluating new products that possess interesting biological activities. Functionalization and cyclization reactions of benzimidazoles lead to a wide variety of novel benzimidazole structures. The synthesis and chemistry of certain anthelmintic. Synthesis, reactivity and biological activity of benzimidazoles find, read and cite all the research. Condensation of ophenylene diamine with chloro acetic acid gave 2chloromethyl benzimdazole, which undergoes halide replacement with phenylhydrazines to give the corresponding nn. Journal of chemical sciences 2009, 121 6, 10171025. Request pdf on apr 14, 2009, mahiuddin alamgir and others published cheminform abstract. Pulla reddy college of pharmacy, mehdipatnam, hyderabad 500.
The reactions of substituted 1,2phenylenediamines and carboxylic acids can. Synthesis, characterisation, and biological evaluation of. Synthesis and anthelmintic activity of some hybrid. Synthesis and biological activity of novel benzimidazole. A series of novel bisbenzofuranimidazolium salts were designed and prepared. Synthesis and biological activity of novel benzimidazoles nopr. Further a wide range of therapeutic activities of benzimidazole show that. Synthesis of n4methylbenzenesulfonyl n4methylbenzenesulfonyl benzimida zol2ylmethylthiobenzimidazole 9.
Jun 05, 2015 read structure activity relationship sar study of benzimidazole scaffold for different biological activities. Some studies conducted with azaindole and indazole derivatives showed cardiovascular activity associated with these compounds. The synthesized compounds were subjected to microbiological screening and invitro antiinflammatory activity. Some of these compounds showed promising analgesic activity when. General procedure for the synthesis of 2chloromethyl1hbenzimidazole. The resulting solution was cooled and made alkaline to litmus with 10% sodium hydroxide solution. Biological activity analgesic activity by acetic acid induced writhing test. Syntheses of quinoxaline derivatives via many different methods of synthetic strategies have been presented. The yield of all benzimidazole derivatives were found to be in the range of 75 94%. It is a tautomer of a 4h benzimidazole, a 2h benzimidazole and a 3ah benzimidazole.
Synthesis and antihepatitis b virus activity of novel. The purity of the compounds were ascertained by a melting point and tlc. Synthesis and antibacterial evaluation of some novel. Benzimidazole and its derivatives are regarded as an important heterocyclic motif that exhibits a wide range of pharmaceutical applications including anticancers, antihypertensives, antivirals. Warsaw university of technology, faculty of chemistry, 3 noakowskiego st. Synthesis and biological evaluation of 2substituted. Structure activity relationship sar study of benzimidazole.
Synthesis of phenyl hydrazine substituted benzimidazole. The synthesis of title compounds could be achieved by the schemei. Synthesis of commercially available benzimidazole involves condensation of ophenylenediamine with formic acid. Synthesis of 2substituted benzimidazole analogs a mixture of 5. The overall reactivity of imidazoles and benzimidazole is referred from sets of resonance structure in which the dipolar contributors have finite importance. Chapter 2 benzoxazole, benzimidazole 40 synthesis of this compound is of considerable interest. All the compounds were characterized by uv, ir, 1 h nmr, mass spectral data and chn elemental analysis. Synthesis and biological activity of new bisbenzofuran. In recent years, there has been considerable interest of researchers in thiazolo3,2abenzimidazoles, stimulated by their biological activities. Synthesis and in vitro antibacterial activity of 5halogenomethylsulfonyl benzimidazole and benzotriazole derivatives volume. Synthesis and analgesic activity of novel derivatives of 1,2.
Benzimidazole is a biologically important scaffold which displays important biological activities. Molecular hybrids integrated with benzimidazole and. The synthesized derivatives were screened for analgesic and antiinflammatory activities. The chemical structures of some of the benzimidazole based anticancer drugs which are candidates in different stages of clinical trials by various pharmaceutical companies. Ramineni srinivasulu, kannasani ravi kumar and peruri veera venkata satyanarayana, facile and efficient method for synthesis of benzimidazole derivatives catalyzed by zinc triflate, green and sustainable chemistry, 04, 01, 33, 2014. Wise a basis for interest in the benzimidazole ring system as a nucleus from which to develop potential chemotherapeutic agents was established in the i95os when it was found that 5,6dimethyl i. Synthesis and biological activity of benzimidazole5. The results of anthelmintic tests table 1 showed that four compounds 6a, 6g, 6w and 6y have good nematicidal activity lc 100 at 0. Pdf benzimidazole and its derivatives are used in organic synthesis and they. The reactivity of 2chlorobenzimidazole with respect to piperidine is like the. Molecules free fulltext thiazolo3,2abenzimidazoles. This method has been used to obtain 2aminobenzimidazole derivatives that have the most diverse substituents at one position of the benzimidazole ring, in the amino group, and in the benzene ring 62,63.
An efficient synthesis of schiff bases containing benzimidazole moiety catalysed by transition metal nitrates had been done 14. A convenient method for the synthesis of 2substituted benzimidazoles and benzothizoles offers short reaction times, largescale synthesis, easy and quick isolation of the products, excellent chemoselectivity, and excellent yields as main advantages. A new synthesis and their antiinflammatory activity of a group of 1hbenzimidazole 76 were reported. It is a benzimidazole and a polycyclic heteroarene.
Generally, the condensation of ophenylene diamine with carboxylic acids and their nitrile, imidates and orthoester 8 derivatives have been widely used for benzimidazole synthesis. Pdf synthesis, characterization and biological activity of some. Synthesis and biological activity of some heterocyclic compounds containing benzimidazole and. Synthesis and biological screening of benzimidazole derivatives html full text. The study was designed to determine the sites on the molecule most relevant for activity and through their modification develop more.
Synthesis, reactivity and biological activity of benzimidazoles. The infrared spectrum of compound 8 indicated the absence of a free sh absorption band and the appearance of sc stretching at 748 cm. Black and naresh kumar, synthesis, reactivity and biological activity of benzimidazoles, bioactive heterocycles iii, 10. Finally, the key intermediate 16 was alkylated with benzyl chloride in aqueous sodium hydroxide. The most prominent benzimidazole compound in nature is nriosyldimethylbenzimidazole, which serves as a axial ligand for cobalt in vitamin b12. Further a wide range of therapeutic activities of benzimidazole show that they are also anticancer, 12 antihyper. Among the four supplied synthetic compounds, benzimidazole2thiol and 3bromopropyl ammonium bromide at a dose of 50 mgkg body wt revealed significant analgesic activity with 37. Their antimicrobial, cytotoxic and diuretic activities have been investigated. Synthesis and biological activity of ferrocenyl furoyl derivatives tombul et al. Synthesis and antimicrobial activity of certain benzimidazole. Synthesis and biological activity of benzimidazole5carboxamides.
The synthesis of benzimidazoles derivative involves subsequent synthesis of 42chloroethoxybenzaldehyde, 4 methyl benzaldehyde followed by benzimidazoles derivative by reaction between amines derivatives and ophenylenediamine in dimethyl farmamide dmf as solvent in the presence of iodine as a catalyst. The synthesised compound exhibited the biological activity. Zbigniew ochal, maria bretner, renata wolinowska and stefan tyski affiliation. Medicinal chemistry is the discipline concerned with determing the influence of chemical structure on biological activity and in the practice of medicinal chemistry developed from an empirical one involving organic synthesis of new compound based largely on the modification of structure and then identifies their biological activity. We elicited a new method for the synthesis of benzimidazoles with aromatic acid. Reactivity of 21methyl1hbenzodimidazol2yl2nitrosoacetonitrile. Preston, synthesis, reactions, and spectroscopic properties of benzimidazoles. These predict electrophilic attack in imidazole at n3 or any ring carbon atom, nucleophilic attack at c2 or. In 1991 benzimidazole derivatives were synthesized by derivatization at nh of benzimidazole by electron donating group and substitution with long chain of propyl, acetamido, thio, thiazoleamino, tetramethyl piperidine on pyridine resulting in good antiulcer activity 2,3. The in vitro antitumor activity of these derivatives was evaluated again. Design, synthesis, chemistry and biological evaluation of.
Synthesis of indole derivatives with biological activity current organic chemistry, 2010, vol. However, owing to fast developing benzimidazole containing new drugs numerous reports have appeared on the synthesis of this privileged scaffold. Fast and easy structural modification of these organic molecules can be. Synthesis and evaluation of selected benzimidazole.
Simon associate professor, department of chemistry, dhanalakshmi srinivasan engineering college, perambalur, tamilnadu ug scholar, department of electronics and communication engineering. The synthesis, physicochemical characterization, and biological activity of 2aminobenzimidazole complexes with different metal ions have been reported. New synthetic procedures, including microwaveassisted synthesis, solid phase synthesis, natural product synthesis, and synthesis of bisbenzimidazoles are briefly. Synthesis and biological activity of novel benzimidazoles.
Synthesis of indole derivatives with biological activity by. Biological activity of heterocyclic compounds the extraordinary role of pyrimidine ring in dihydropyrimidine presumes as essential part in nucleic bases, vitamins, enzymes, chlorophyll, hemoglobin, hormones and. Synthesis of 3,3diphenylcyclopropene 16 list of tables ii. This book provides the series of novel and significant compounds containing pyrazole substituted benzimidazoles which have been synthesized under. Scope of the experiment chemical modifications of drug molecule of a series having optimum activity is widely used and. Synthesis characterization and biological activity benzimidazole derivatives dr.
Antimicrobial, anticancer and anti tubercular activities of some pyrazole substituted benzimidazoles kalirajan rajagopal on. Preliminary investigation of biological activity indicated that all of the compounds exhibited lower activity than that of betacypermethrin against plutella xylostella and lipaphis erysimi. Antimicrobial activity against bacteria and fungi was studied. In this contribution, we report the synthesis, structural information, biological activity, and structure activity relationship sar study of separase inhibitors based on structural modification of sepin1 1. Synthesis and analgesic activity evaluation of some new. The present study describes a simple, inexpensive, and easy method for synthesis of benzimidazole derivatives in a stipulated time, without using any drastic conditions. The synthesised compound was exhibited significant antiinflammatory activity at 100mgkg and it possesses antifungal activity against aspergillus. Benzimidazole is a heterocyclic aromatic organic compound. Read structure activity relationship sar study of benzimidazole scaffold for different biological activities. Synthesis and medicinal applications of benzimidazoles. Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis b virus. Abstract a series of nsubstituted benzimidazole derivatives 15 was synthesized.
Benzimidazole, green synthesis, biological activity, 2arylbenzimidazole, 2aminobenzimidazole, 2alkylarylthiobenzimidazole. The synthesis and chemistry of certain anthelmintic benzimidazoles lb. Synthesis of indole derivatives with biological activity. Quinoxalines and fused ring systems show diverse pharmacological activities. Cicbia 2010 11 1 87 to conclude this part of biological activity, we will mention a few patents showing.
Aminopropylbenzimidazole dichloride dihydrate via various hydrogen bonds and x. It is a tautomer of a 4hbenzimidazole, a 2hbenzimidazole and a 3ahbenzimidazole. Synthesis and in vitro antibacterial activity of 5. Synthesis and reactivity in inorganic, metalorganic, and nanometal chemistry. Concise on some biologically important 2substituted. Synthesis, characterization, and biological evaluation of. Additionally an enormous variety of thiazolo3,2abenzimidazoles with unique pharmaceutical and medicinal applications have been reported in the patent literature. The compounds were assessed on rat adjuvant arthritis screen. Synthesis, reactions, and spectroscopic properties of.
The convenient synthesis of benzimidazole derivatives. Benzimidazole nucleus was acylated in 1position with benzoyl chloride in basic. There is an increasing number of compounds developed to target one or more pathways involved in vasodilation. Synthesis of benzimidazole 2 benzimidazole was prepared according to the reported literature. Among the various possible routes to the formation, isomeric structures have been cited because of patented reaching advanced phases of clinical trials. In the present study, a series of novel benzimidazole derivatives containing chrysanthemum acid moieties was designed and synthesized. Compounds 1a, 1b, 1c and 1d were screened for antiinflammatory. Photoluminescent benzobisimidazolium salts 9 and their physical and photophysical properties. Substituted benzimidazole derivatives have found commercial application in veterinarian medicine as anthelmintic agents and in diverse human therapeutic pharm chemistry synthesis, characterization, and biological evaluation of benzimidazole derivatives as potential anxiolytics nannapaneni dt, gupta atyam vsss1, reddy mi, sarva raidu ch1. Synthesis of novel thiophene, thiazole and coumarin. Jul 21, 2007 benzimidazole is a biologically important scaffold which displays important biological activities. Synthesis and analgesic activity evaluation of some new benzimidazole derivatives.
Diverse ranges of biological potencies of agents possessing a benzimidazole unit are ascribed to the unique fused imidazole and benzene rings, which can interact with a variety of targets of biological importance in a noncovalent mode because of the. Synthesis and biological activities of some benzimidazoles. Benzimidazole derivatives are known to have microbial. Compounds 1a, 1b, 1c and 1d were screened for antiinflammatory activity and they showed percent inhibition 22. 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. A novel series of 2substituted benzimidazole derivatives 3a3j were synthesized by the reaction of 2chloro methyl benzimidazole with substituted primary aromatic amines. Pulla reddy college of pharmacy, mehdipatnam, hyderabad 500 028, india. Antiinflammatory synthesis and antiinflammatory activity of phenyl benzimidazole 1 was reported by leonardo et al 6.