Oxidative treatments of benzothiazole and benzothiazole derivatives 2. Synthesis of novel benzimidazole and benzothiazole. Pongamia pinnatasyzigium cumini, delonix regia, adathoda. Convenient route synthesis of some new benzothiazole. Novel benzothiazole derivatives as fluorescent probes for. Fluorescence intensity of all ppbta derivatives significantly increased upon binding to a. Synthesis and biological evaluation of sulfonamide thiazole and benzothiazole derivatives as antimicrobial agents iro argyropoulou,a athina geronikaki,a paola vicini,b and franca zanib adepartment of pharmaceutical chemistry, school of pharmacy, aristotelian university of thessaloniki, thessaloniki 54006, greece. The reaction of orthosubstituted anilines with functionalized orthoesters yields benzoxazole, benzothiazole, and benzimidazole derivatives in an efficient and connective methodology. Pdf is not rendering correctly, you can download the pdf file here.
This subject was already covered extensively in checii1996 and since then no new work has appeared. The versatility of this approach enables the development of new libraries. Pharmacy australia center of excellence, university of queensland, woollongabba, brisbane, qld 4102, australia. Bta derivatives possesses broad spectrum biological activities such as. H 2 o system without any other acid additive or organic solvent. Benzothiazole has been the primary rubberrelated chemical found in synthetic turf studies. Synthesis of benzothiazole derivatives and their biological. Take equimolar amount of substituted 2hydrazinyl 1,3benzothiazole derivatives and substituted acetophenone in methanol, add 24ml of formaldehyde and add few drops of conc. Benzothiazole is among the usually occurring heterocyclic nuclei in many marine as well as natural plant products. Benzothiazole, antibacterial activity, antifungal activity, pyrazole.
Benzothiazole is an aromatic heterocyclic compound with the chemical formula c 7 h 5 ns. Benzothiazole derivatives as potential antiinfective agents volume. This pdf is available for free download from a site hosted by medknow publications. Although the parent compound, benzothiazole is not widely used, many of its derivatives are found in commercial products or in nature.
Therapeutic advancement of benzothiazole derivatives in. Cyclization process for substituted benzothiazole derivatives download pdf. Synthesis and biological activity of new 1, 3benzothiazole. A series of new benzothiazole derivatives 6ah have been synthesized, in five steps, from substituted phenols via the 1,3,4oxadiazole2thiones 5ah. Synthesis of novel benzothiazole compounds with an. However, pet and spect, due to their low spatial resolution, are unable to detect individual plaques and earlystage amyloid deposition. The test compound sc7 showed good invitro antioxidant activity. Experimental runs have been carried out in the ph range 3.
Synthesis of some new biologically active benzothiazole derivatives bull. Synthesis and biological evaluation of sulfonamide. Antioxidant activity of novel coumarin substituted. However, risks associated with bzt have not been thoroughly assessed, primarily because of gaps in the database. Synthesis, characterization and antibacterial activity of. Synthesis, characterization and carbonic anhydrase inhibitory activity of novel benzothiazole derivatives.
A new and efficient method for the synthesis of pyrimido2. In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Brominated derivatives iii, in particular hetarylamide iiic, had the greatest hypoglycemic activity. Synthesis, characterization and biological evaluation of. Antitumor evaluation of some novel cyano and amidino benzothiazole derivatives 1. A variety of new pyrido2,1bbenzothiazole and benzothiazoles, have been prepared via the reaction of 2substituted methylthiazole with. In vitro antitumor and antiviral activities of new. Benzothiazole is a privileged bicyclic ring system with multiple applications.
The benzothiazole moiety from tht and the hpo moiety from deferiprone were connected with vinyl linker to achieve. Benzothiazolyl derivatives have much better chemical, thermal, and photochemical stabilities than structurally similar compounds. Benzothiazole derivatives possess a wide spectrum of biological applications such as antitumor. In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4oxadiazole2thione derivatives. Synthesis of novel derivatives of benzothiazole and benzothiazole isosters of expected activity against breast cancer. Benzothiazole derivatives as potential antiinfective. August 29, 2017 3446 1hpyrano2,3dpyrimidin6yl3oxopropanenitrile 6 in 87% yield figure 3. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. A straight forward and highly efficient onepot annulation of 2aminobenzothiazole, enmethyl1methylthio2nitroethenamine, and aldehydes in the presence of fef3 is described. Click here to view the university of florida catalog record. Pdf of the article will no longer be available online. An environmental friendly method was developed for preparing benzothiazole derivatives via the reaction of ortho.
Pyridine and benzothiazole derivatives in carbanionic. Novel benzothiazole derivatives with enhanced biological activity 4 wo2016079688 a168 pctib2015 058919 nov 11, 2015 christine schmitt et al. Benzothiazole c7h5ns cid 7222 structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety. Metallizable azo dyes prepared from aminobenzothiazole derivatives and betanaphthol derivatives download pdf info publication number us2868774a. Correspond ingly, benzothiazole and its derivatives are widely distributed and have been detected by screening analyses in industrial and municipal wastewater lo121 as well as in. Us2868774a metallizable azo dyes prepared from amino. Us81538b2 benzothiazole and benzooxazole derivatives. Synthesis of new benzothiazole derivatives bearing.
Synthesis and evaluation of antifungal activity of. Oxidative ringopening of benzothiazole derivatives. Four isomers and three transition states of their transformations for each compound of hbo, hbt, hpybo, and hpybt and two isomers and one transition state for each hbi and hpybi compounds. Novel synthesis of pyrido2,1bbenzothiazoles and 1,3. A novel series of 2subsituted benzothiazole derivatives as mtdls were designed and synthesized for ad therapy using pharmacophorecombine strategy. Pyridine conataining piperazine benzothiazole derivative 18. The importance of benzothiazole and derivatives as potential antimicrobial agents has been well established and a large number of papers have been published in this regard. Hofmann in 1879, while use of 2sulfanylbenzothiazoles as vulcanization accelerators for natural and synthetic rubber was. Benzothiazole toxicity assessment in support of synthetic. Diverse functionalized nmethyl3nitro4hpyrimido 2, 1b 1, 3 benzothiazole2amine derivatives were obtained with excellent yields under neat conditions. Prabodh chander sharma, kushal kumar bansal, aakash deep and meenakshi pathak affiliation. Screening and molecular docking of novel benzothiazole. This assessment provides toxicity information for a.
Journal of enzyme inhibition and medicinal chemistry 2016, 31 6, 12211225. Almost all amidino derivatives showed noticeable antiproliferative effect on several tumor cell lines while cyano derivatives showed considerably less pronounced activity due to poor solubility in aqueous cell culture 31,32. Recent studies have shown that numerous benzothiazole derivatives exhibit hmao inhibitory activity in the micromolar concentration range. Synthesis of some new biologically active benzothiazole. Firefly luciferin can be considered a derivative of benzothiazole. The in vitro antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives 6d and 6e showed strong. A series of 20 novel benzimidazole and benzothiazole derivatives linked to a 1,2,3triazole ring system was synthesised, characterised and evaluated for in vitro acetylcholinesterase ache inhibitory activity. The onepot threecomponent reaction of 2aminobenzothiazole, benzaldehyde derivatives and. Department of chemistry, university of waterloo, waterloo, on n2l 3n1, canada. Synthesis and evaluation of antifungal activity of benzothiazole derivatives. Today 3,4dihydropyrimidin21hones dhpmand its derivatives have received considerable amount of attention due to its several biological activities such as antiviral, antibacterial, antitumor and antiinflammatory properties11.
The first step is to select effective compounds by simple, rapid and. Design of new anticancer prodrugs is important source to the development of antitumoral agents that can be effective on resistant cancer cell types and have fewer side effects. Benzothiazole derivative compounds, compositions, and uses 6 wo2014036242 a370 pctus20. Antibacterial benzothiazole derivatives 5 us8691185 b269 us 548,014 apr 8, 2014 prasad raje et al. Iodinated benzothiazole derivatives radiolabeled with either c 11 or i 125 i 123 have also been developed for dual modal in vivo imaging of amyloid deposits in mice using pet or spect wang et al. The same compound was selected for invivo antioxidant studies by administering different doses in ehrlich ascites carcinoma eac treated mice. Benzothiazole derivative an overview sciencedirect topics. Benzothiazole, synthesis, click chemistry, antiinfective activity. Synthesis and antidiabetic evaluation of benzothiazole derivatives. The structural formula of all derivatives was confirmed and characterized by elemental analysis and spectral studies. Benzothiazole bzt may volatilize from crumb rubber and result in inhalation exposure. Benzothiazole derivatives encompass an attractive heterocyclic class. Synthesis and biological activity of new 1,3 benzothiazole derivatives.
Screening and molecular docking of novel benzothiazole derivatives as potential antimicrobial agents by mohamed a. Pdf synthesis of novel derivatives of benzothiazole and. Indole, benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product. Pdf benzothiazole bta belongs to the heterocyclic class of bicyclic compounds. Review article recent advances in the chemistry and biology of benzothiazoles rupinder k. In this study, we newly designed and synthesized three pushpull benzothiazole ppbta derivatives as fluorescent probes for detection of a. The structures of the reaction products were established based on the elemental analyses and spectral data ir, 1 h, cnmr, ms. Benzothiazole bta belongs to the heterocyclic class of bicyclic compounds. Isomeric structures of benzimidazole, benzoxazole, and. Rawal 1, and jitender bariwal 1 department of pharmaceutical sciences, isf college of pharmacy, moga, punjab, india 2 research scholar, punjab technical university, jalandhar, punjab, india benzothiazole is a privileged heterocyclic scaffold having a benzene ring fused with a. The synthesis of benzothiazole derivatives and investigation of their chemical and biological behavior have gained more importance in recent decades. Benzothiazole is a conjugated sp 2hybridized bicyclic 10. Thus, this reaction system greatly simplifies post. An attempt was made to synthesize newer coumarin substituted derivatives of benzothiazole and they were evaluated for antioxidant activity by dpph radical scavenging activity.
Extraction and analysis of various benzothiazoles from. Benzothiazole derivatives as potential antiinfective agents. The benzothiazole moiety with various substitutions has shown antitumor activity. Pdf benzothiazole derivatives as anticancer agents researchgate. Pandeya 1kmch college of pharmacy, kovai estate, kalapatti road, coimbatore,india. Benzoxazole and benzothiazole derivatives as potential.
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