The synthesized materials include not only small coordination complexes but also isolated crystals. Google has not performed a legal analysis and makes no. 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. Omeprazole, pantoprazole, lansoprazole and ofendazole like few drug molecules possessing benzimidazole core, these are already in use figure 1. Antibacterial activity of benzimidazole derivatives. A new series of 2, 5 disubstituted benzimidazole derivatives have been synthesized. Two lone pair electrons are contributed to the aromatic sextet by an imino group, the other nitrogen is therefore pyridinelike, its lone. The reaction yields and product stability were significantly affected by the identity of the diamine and anhydride substituents. The general applications of benzimidazole derivatives in materials chemistry, electronics, technology, dyes, pigments, and agriculture open up new research horizons. A novel series of 2substituted benzimidazole derivatives 3a3j were synthesized by the reaction of 2chloro methyl benzimidazole with substituted primary aromatic amines.
Department of pharmaceutical chemistry, federal urdu university of arts sciences and technology, gulshane iqbal campus, karachi. Debenzylation of the 2methyl derivative of imidazo1,2abenzimidazole is not accompanied by hydrogenation but gives. Most of the synthesized compounds exhibited high or very high affinity for the 5ht3 binding site and low to no significant affinity for the 5ht4 receptor. It was also used in the preparation of benzimidazolium surfactant, 1hexadecyl. This compound is the most potent of a series of substituted 2amino derivatives, is active against a wide variety of animal nematodes. A mixture of 3 and 1,zdiaminobenzene 7 was heated in phosphoric acid to give 1. The present study describes a simple, inexpensive, and easy method for synthesis of benzimidazole derivatives in a stipulated time, without using any drastic conditions. Substitution of benzimidazole nucleus is an important synthetic strategy.
Prior art keywords dichloro benzimidazole ribofuranosylbenzimidazole ribofuranosyl ribofuranose prior art date 19530505 legal status the legal status is an assumption and is not a legal conclusion. Supramolecular assembly of benzimidazole derivatives and. All the compounds were characterized by uv, ir, 1 h nmr, mass spectral data and chn elemental analysis. Compared to imidazole ring systems, benzimidazole derivatives are very stable towards heat and oxidizing agents. The benzimidazole and its derivatives play a very important role as a therapeutic agent e. Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents fatmah a. 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.
Synthesis, characterization and biological evaluation of benzimidazole derivatives keshav anand and sharad wakode department of pharmaceutical chemistry, delhi institute of pharmaceutical sciences and research dipsar, sector 3, pushp vihar, new delhi. Effects of benzimidazole derivative, b1b8, on spinal tnf. Synthesis and evaluation of selected benzimidazole. It is a tautomer of a 4hbenzimidazole, a 2hbenzimidazole and a 3ahbenzimidazole. New heterocyclic derivatives of benzimidazole with. Synthesis and antibacterial activity of novel benzimidazole. Benzimidazole and imidazole both act as good ligands to transition metal ions 1 and they exhibit several coordination modes as shown in scheme 1. Pdf benzimidazole derivatives are versatile nitrogen containing heterocyclic compounds which have long been. The purity of the compounds were ascertained by a melting point and tlc.
It is a tautomer of a 4h benzimidazole, a 2h benzimidazole and a 3ah benzimidazole. The subject compounds are 2aminoimidazole derivatives. Benzimidazole derivatives are versatile nitrogen containing heterocyclic compounds which have long been known as a promising class of biologically active compounds. Several types of benzimidazole derivatives were prepared and were screened for h 1. The purity of the compounds was ascertained by a melting point and tlc. Parbendazole has been shown to exhibit a broadspectrum anthelmintic activity.
The synthesized compounds were characterized by using ir, 1h nmr, and mass spectral data together with elemental analysis. Benzimidazole derivatives and its biological importance. The structures of the synthesized compounds were confirmed by ir, 1h. Benzimidazoles and its derivatives represent one of the most biologically active class. May 15, 2019 benzimidazole derivatives as antiproliferative agents. Synthesis and biological evaluation of 2substituted. Phosphoric acid h,po, is known to be a good condensing agent for the preparation of 2alkyl substituted benzimidazole derivatives.
Preparation and applications first defines the structure, physical and chemical properties of the benzimidazole compound class. Synthesis, characterization, and biological evaluation of. Pdf benzimidazole is a heterocyclic aromatic organic compound. Studies in vitro and in vivo demonstrated that the antioxidant activity of the test compounds decreased gi toxicity. Ch 2 oh, cooh, coor 3 and 4,4dimethyl2oxazolinyl, r 3 being a short chain alkyl group such as methyl, ethyl, etc. Ds method and their physical properties were investigated. Synthesis and biological activity of novel benzimidazole derivatives. Active class of antioxidants arfa kamil 1, shamim akhtar. Benzimidazole, a heterocyclic aromatic organic compound consisting of a fusion of benzene and imidazole, in an extension of the wellelaborated imidazole system, has been used as a carbon skeleton for n heterocyclic carbenes, usually used as ligand for transition metal complexes. It is a benzimidazole and a polycyclic heteroarene. The synthesized derivatives were screened for analgesic and antiinflammatory activities. The synthesized benzimidazole compounds were screened for acute. Benzimidazole derivative an overview sciencedirect topics. The purity of the compounds was ascertained by melting point and tlc.
As antihypertensive agents article pdf available in ejournal of chemistry 34 january 2006 with 861 reads. 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. Gayathri 1, srujana 1, aary divya 2 1 department of pharmaceutical chemistry, sitha institute of pharmaceutical sciences, hyderabad, andhra pradesh. Joshi, dstjrf inspire fellow, mnschngu, patan observed that benzimidazole derivatives are found to possess antihiv,24 anthelmintic,25. Chapter 4 studies on benzimidazole derivatives 2 ph. The yield of all benzimidazole derivatives were found to be in the range of 7594%. Synthesis, characterization and biological evaluation of benzimidazole derivatives keshav anand and sharad wakode department of pharmaceutical chemistry, delhi institute of pharmaceutical sciences and research dipsar, sector 3, pushp vihar, new delhi 110017, delhi, india. Synthesis of benzimidazoles the synthesis of benzimidazole. Apart from this the benzimidazole derivatives exhibit pharmacological activities. Introduction benzimidazoles and its derivatives represent one of the most biologically active class of. Benzimidazole scaffolds as promising antiproliferative agents.
Benzimidazole plays an important role in the medicinal chemistry and drug discovery with many pharmacological activities which have made an indispensable anchor for discovery of novel therapeutic agents. Antiinflammatory synthesis and antiinflammatory activity of phenyl benzimidazole 1 was reported by leonardo et al 6. Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of inflammatory and immunerelated conditions or disorders. Furthermore, some benzimidazole derivatives have been demonstrated to be inhibitors of mao enzyme 10, angiotensin ii receptor 11, enzyme topoisomerase i 12 and enzyme lipase etc. Elnassans group showed novel 1,2,3,4tetrahydro1,2,4triazino4,5abenzimidazole 6 analogs of aryl and heteroaryl groups showing antitumor activity in human breast adenocarcinoma cell line mcf7. Benzimidazole derivatives act by interfering with metabolic pathways. Us5877187a benzimidazole derivatives with antihistaminic. Several benzimidazole derivatives have been tested in vitro for their ability to inhibit human placental aromatase activity. View enhanced pdf access article on wiley online library html view download pdf for offline viewing. Synthesis, characterization and antibacterial activity of benzimidazole derivatives carrying quinoline moiety. Process for the optical purification of the single enantiomers of some 2sulphinyl1hbenzimidazole derivatives and another structurally related sulphoxide from the respective enantiomerically enriched preparation thereof. Benzimidazoles heterocyclic building blocks sigmaaldrich.
Benzimidazole derivatives as antiproliferative agents. Benzimidazole is produced by condensation of ophenylenediamine with formic acid, or the equivalent trimethyl orthoformate. Synthesis and biological evaluation of novel benzimidazole derivatives and their binding behavior with bovine serum albumin. 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. Synthesis of benzimidazole substituted pyridone azo. In particular, the invention provides compounds which modulate the expression andor function of proteins involved in inflammation, immune response regulation and cell proliferation. A new series of azabicyclic benzimidazole4carboxamides 2. Download fulltext pdf download fulltext pdf synthesis of benzimidazole derivatives.
Further conventional and alternative synthesis methods and important reactions of these compound derivatives are illustrated with examples. The design and modification of benzimidazole opens the scope of the diversity of structures different sizes and morphologies that can be built. The results show that five out of the six compounds tested are more active in the inhibition of aromatase activity than aminoglutethimide ag, which we chose as the reference compound and which, as an aromatase inhibitor, is currently being used in the treatment of. Benzimidazole derivatives and their complexes as accelerators for curing of epoxy resin. As antihypertensive agents article pdf available in ejournal of chemistry 34. Synthesis of benzimidazole derivatives as potential h1. Process for the optical purification of the single enantiomers of some 2sulphinyl1h benzimidazole derivatives and another structurally related sulphoxide from the respective enantiomerically enriched preparation thereof. Novel research strategies of benzimidazole derivatives. Benzimidazole is prepared from ophenylenediamine which is treated with formic acid in presence of alkali. This paper describes the synthesis and biological evaluation of n1phenylsulfonyl2methylaminosubstituted1hbenzimidazole derivatives as antiinflammatory analgesic agents with lower gastrointestinal gi toxicity. Benzimidazole ribosides were first reported by drach and townsend. A,b at 96 h after the last dose of morphine, the animals were sacrificed after. Benzimidazole derivatives and their complexes as accelerators. Benzimidazole derivatives download pdf info publication number us28601a.
Pharmacological compounds of benzimidazole derivatives are potent inhibitors for a variety of enzymes. Chemistry and applications of benzimidazole and its. Synthesis and biological activities of some benzimidazoles. 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. Synthesis and biological activities of some benzimidazoles derivatives. Most of the compounds showed potent antihistaminic activity in vitro. A series of new benzimidazole derivatives were synthesized by the solid. Synthesis of benzimidazole substituted pyridone azo disperse. Compounds 1a, 1b, 1c and 1d were screened for antiinflammatory.
Synthesis and pharmacological profile of benzimidazoles. Joshi, dstjrf inspire fellow, mnschngu, patan observed that benzimidazole derivatives are found to possess antihiv,24 anthelmintic,25 antimycobacterial,26 antidiabetic27 and antioxidant properties. Unlimited viewing of the articlechapter pdf and any associated supplements and figures. Research on imidazo 1, 2a benzimidazole derivatives. The yield of all benzimidazole derivatives was found to be in the range of 75 94%. View the article pdf and any associated supplements and figures for a period of 48 hours. Benzimidazole scaffolds as promising antiproliferative. A wide variety of benzimidazole derivatives have been describedfor. Pdf benzimidazole derivatives and its biological importance. This gene encodes a serinethreonineprotein kinase that play a central role in mitosis. Pdf green chemistry is the new and rapidly emerging field of chemistry. Synthesis of benzimidazoles the synthesis of benzimidazole derivatives starts with the benzene derivatives having nitrogen at ortho position to each other. The multitude of benzimidazole derivatives marketed as drugs has led to intensive research in the field for the discovery of new biologically active structures. The yield of all benzimidazole derivatives were found to be in the range of 75 94%.
Awaad 5 and nazira karodia 2,6, 1 chemistry department, college of science, king saud university, riyadh 162, saudi arabia. Us5929244a process for the optical purification of. Apart from this the benzimidazole derivatives exhibit pharmacological activities such as antimicrobial, antiviral, anticancer, antiinflammatory, analgesic, etc. The fascinated biological activity of benzimidazole and its derivatives are seen against many human pathogens and microbial attacks.
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