Selective Synthesis of 2-Substituted and 1,2 …
Keywords: Benzimidazole Derivatives; O-Phynelyenediamine; Substituted Aldehydes; Zinc Triflate
Synthesis of Multifunctionalised 2-Substituted Benzimidazoles ..
Benzimidazole derivatives are eminent biologically active N-containing heterocycles, it is well known that benzimidazole derivatives attain antimicrobial analgesic and anti-inflammatory activities, as well as proved to have activities against HIV and cancer. Heterocyclic nucleus and substituted amino group at 1-position of the benzimidazole were reported to be associated with potent anti-inflammatory activity. Therefore it was thought that preparing Mannich base derivatives from 2-substituted benzimidazoles would probably result in compounds of having high biological activities toward many diseases.
Mannich Bases were prepared by a solution of 2-substituted benzimidazole (0.005 mol) in 10 ml ethanol, 0.005 mol of secondary amine and 0.005 mol of formaldehyde and then the reaction mixture was refluxed for 8 h. On cooling, the product formed was filtered, dried and recrystallised from Di methyl foramide (DMF). Specific details given to each compounds.
Synthesis of multifunctionalised 2-substituted ..
Synthesis of bioactive molecule fluoro substituted benzothiazole comprising sulphonamide quinazolinyl imidazole for biological and pharmacological screening, Ultra science vol.20(2),281-296 (2008)
The replacement of 2,2‘-bipyridine (bpy) by 6,6‘-dimethyl-substituted 2,2‘-bipyridine (dmbpy) is suggested to change the steric and electronic factors involved in ...Ru(II) bipyridine complexes were synthesized and their spectroscopic properties studied.
shown synthesis of substituted benzimidazole via ..
The extensively used as drugs such as proton pump inhibitor (Omeprazole), Antihelmenthetics (Albendazole), antidopaminergic (Domperidone), specifically, the 2-substituted analogs of benzimidazoles are known to be potent biologically active compounds against inflammation, viral and microbial infection. Furthermore, benzimidazole derivatives are structural isosteres of naturally occurring nucleotides, which allows them to interact easily with the biopolymers of the living systems.
Benzimidazole compounds were prepared from the condensation reaction between ortho phenylene diamine and various acids. Mannich base of newly synthesized Benzimidazole derivatives were synthesized from 2-substituted Benzimidazoles by reacting with secondary amines. The purity of the compounds was ascertained by melting point (m.p) and thin layer chromatography (TLC). Structures of the synthesized compounds were elucidated by spectral data. Antimicrobial assay was performed by microbroth dilution method. Bacterial genomic DNA cleavage was assessed by Agarose gel electrophoresis. Toxicity of the most effective compounds was studied by Brine-shrimp lethality assay.
2-substituted phenoxymethyl benzimidazole derivatives
Imidazole and Benzimidazole Synthesis is a comprehensive survey of ..
3.2. Zinc Triflate Catalyzed Synthesis of 2-Substituted Benzimidazole Derivatives from Aldehydes
Research of benzimidazole derivatives
Benzimidazoles and its derivatives represent one of the mainly biological active classes of literature.
activity of some 2-substituted 3- acetic acid benzimidazole ..
Synthesis, antiviral and cytotoxic investigations of 2-(4-chlorophenyl)-3-substituted quinazolin-4(3H) ones.
Imidazole and benzimidazole synthesis - Organic …
Mannich reaction is a condensation between a compound containing atleast one active hydrogen atom, formaldehyde and ammonia, secondary amine have been used as a synthetic tool in the preparation of various therapeutic agents like, fluoxetine as antidepressant agent, ethacrynic acid a high ceiling loop diuretic, benzoquinamide, a high psychotic agent, Ranitidine, Triprolidine an H-receptor antagonist, and Trihexylphenidyl hydrochloride, an antispasmodic. Mannich bases are physiologically reactive because of the basic function rendering the molecule soluble in aqueous solvent when it is transformed into ammonium salt. Over the past few decades, Mannich bases of heterocyclic molecules have been grabbing the attention of the synthetic chemists for their wide gamut of biological activities ranging from antibacterial, anticancer, antiparkinson to anticonvulsant, analgesic, antispasmodic, anti-HIV, anti-malarial as well as intermediates in drug synthesis. 2-Substituted benzimidazole derivatives, one of the most important derivatives of benzimidazole are known to possess varied biological activities. In SAR, the biological activities of benzimidazole compounds depend upon the substitution at the N-1 or C-2 position. These observations have been guiding for the development of new mannich bases of 2-substituted benzimidazole derivatives and evaluated for antibacterial and anthelmintic activity.
Synthesis of Benzoxazoles - Organic Chemistry Portal
In this present study aimed to synthesize N-mannich bases derivatives compounds bearing of 2-substituted benzimidazole moiety, in order to investigate their possible biological activity.
1,2-Amino Alcohols and Their Heterocyclic Derivatives …
In this present study, we aim to synthesis of a number of Mannich bases derived from substituted benzimidazole, then these compounds were characterized by FT-IR, 1H NMR spectra and their most probable antimicrobial and lethality test.
PDF Downloads : Oriental Journal of Chemistry
Benzimidazole and their derivative were reported to have wide biological activities and were synthesized by using different solvents and ring closing agents. The present work deals with the comparative synthesis of 2-alkyl and aryl substituted benzimidazole derivative in the presence of polyphosphoric acid through microwave and conventional methods and also studied the effect of salt form of reactant for completion of the reaction. The 2-substituted aryl and alkyl benzimidazole derivative were synthesized microwave and was observed to be more beneficial, in respect of yield (increases up to 10 to 50%) and time (96 to 98% was reduced) than conventional method of synthesis. This study was concluded that the salt form of reactant (-phenylenediamine dihydrochloride) gave reduced colour impurities, homogenous mixing and reduced time for completion of reaction.
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