Department of chemistry, university of waterloo, waterloo, on n2l 3n1, canada. Firefly luciferin can be considered a derivative of benzothiazole. Us2868774a metallizable azo dyes prepared from amino. 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 derivatives as potential antiinfective agents volume. Fluorescence intensity of all ppbta derivatives significantly increased upon binding to a. Pharmacy australia center of excellence, university of queensland, woollongabba, brisbane, qld 4102, australia. Pdf synthesis of novel derivatives of benzothiazole and. Synthesis, characterization and antibacterial activity of. Indole, benzothiazole and its derivatives are used in organic synthesis and they are used in evaluating new product. In vitro antitumor and antiviral activities of new. Synthesis and biological activity of new 1,3 benzothiazole derivatives. Benzothiazole, synthesis, click chemistry, antiinfective activity.
Antitumor evaluation of some novel cyano and amidino benzothiazole derivatives 1. Pdf benzothiazole bta belongs to the heterocyclic class of bicyclic compounds. Pyridine conataining piperazine benzothiazole derivative 18. Bta derivatives possesses broad spectrum biological activities such as. Synthesis and biological evaluation of sulfonamide. Oxidative ringopening of benzothiazole derivatives. Pongamia pinnatasyzigium cumini, delonix regia, adathoda. 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. Antibacterial benzothiazole derivatives 5 us8691185 b269 us 548,014 apr 8, 2014 prasad raje et al. Benzothiazole derivatives encompass an attractive heterocyclic class. 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.
Synthesis of novel derivatives of benzothiazole and benzothiazole isosters of expected activity against breast cancer. Click here to view the university of florida catalog record. The same compound was selected for invivo antioxidant studies by administering different doses in ehrlich ascites carcinoma eac treated mice. Convenient route synthesis of some new benzothiazole. Benzothiazolyl derivatives have much better chemical, thermal, and photochemical stabilities than structurally similar compounds. Synthesis, characterization and carbonic anhydrase inhibitory activity of novel benzothiazole derivatives. Synthesis and biological activity of new 1, 3benzothiazole. In recent years heterocyclic compounds analogues and derivatives have attracted wide attention due to their useful biological and pharmacological properties. Prabodh chander sharma, kushal kumar bansal, aakash deep and meenakshi pathak affiliation. Benzothiazole derivative compounds, compositions, and uses 6 wo2014036242 a370 pctus20. The initial pdf document will be replaced by a retraction note. Benzothiazole derivative an overview sciencedirect topics.
Synthesis of novel benzothiazole compounds with an. Isomeric structures of benzimidazole, benzoxazole, and. Thus, this reaction system greatly simplifies post. Pdf is not rendering correctly, you can download the pdf file here. Benzothiazole has been the primary rubberrelated chemical found in synthetic turf studies. A variety of new pyrido2,1bbenzothiazole and benzothiazoles, have been prepared via the reaction of 2substituted methylthiazole with.
H 2 o system without any other acid additive or organic solvent. Benzothiazole bzt may volatilize from crumb rubber and result in inhalation exposure. Benzoxazole and benzothiazole derivatives as potential. The reaction of orthosubstituted anilines with functionalized orthoesters yields benzoxazole, benzothiazole, and benzimidazole derivatives in an efficient and connective methodology.
Synthesis of some new biologically active benzothiazole. Oxidative treatments of benzothiazole and benzothiazole derivatives 2. An attempt was made to synthesize newer coumarin substituted derivatives of benzothiazole and they were evaluated for antioxidant activity by dpph radical scavenging activity. Experimental runs have been carried out in the ph range 3. Novel benzothiazole derivatives with enhanced biological activity 4 wo2016079688 a168 pctib2015 058919 nov 11, 2015 christine schmitt et al. Benzothiazole derivatives as potential antiinfective agents. Brominated derivatives iii, in particular hetarylamide iiic, had the greatest hypoglycemic activity. The versatility of this approach enables the development of new libraries. Benzothiazole toxicity assessment in support of synthetic. Benzothiazole bta belongs to the heterocyclic class of bicyclic compounds. Screening and molecular docking of novel benzothiazole derivatives as potential antimicrobial agents by mohamed a. August 29, 2017 3446 1hpyrano2,3dpyrimidin6yl3oxopropanenitrile 6 in 87% yield figure 3. 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. The onepot threecomponent reaction of 2aminobenzothiazole, benzaldehyde derivatives and.
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. This subject was already covered extensively in checii1996 and since then no new work has appeared. 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. Although the parent compound, benzothiazole is not widely used, many of its derivatives are found in commercial products or in nature. 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. This assessment provides toxicity information for a. Antioxidant activity of novel coumarin substituted. Synthesis of novel benzimidazole and benzothiazole. Novel synthesis of pyrido2,1bbenzothiazoles and 1,3.
Novel benzothiazole derivatives as fluorescent probes for. Diverse functionalized nmethyl3nitro4hpyrimido 2, 1b 1, 3 benzothiazole2amine derivatives were obtained with excellent yields under neat conditions. 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. Benzothiazole is among the usually occurring heterocyclic nuclei in many marine as well as natural plant products. Benzothiazole derivatives as potential antiinfective. The test compound sc7 showed good invitro antioxidant activity.
Pdf of the article will no longer be available online. 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. Identification of 2subsituted benzothiazole derivatives. Several copper catalysts and solvents were screened to establish the optimal conditions for the preparation of the target compounds. The in vitro antitumor activity of the compounds obtained was investigated and the benzothiazol derivatives 6d and 6e showed strong. Synthesis of benzothiazole derivatives and their biological. Benzothiazole derivatives possess a wide spectrum of biological applications such as antitumor. Cyclization process for substituted benzothiazole derivatives download pdf. Metallizable azo dyes prepared from aminobenzothiazole derivatives and betanaphthol derivatives download pdf info publication number us2868774a. The benzothiazole moiety with various substitutions has shown antitumor activity. Journal of enzyme inhibition and medicinal chemistry 2016, 31 6, 12211225. 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. A novel series of 2subsituted benzothiazole derivatives as mtdls were designed and synthesized for ad therapy using pharmacophorecombine strategy. Recent studies have shown that numerous benzothiazole derivatives exhibit hmao inhibitory activity in the micromolar concentration range.
Synthesis and antidiabetic evaluation of benzothiazole derivatives. Benzothiazole is an aromatic heterocyclic compound with the chemical formula c 7 h 5 ns. Pandeya 1kmch college of pharmacy, kovai estate, kalapatti road, coimbatore,india. A series of new benzothiazole derivatives 6ah have been synthesized, in five steps, from substituted phenols via the 1,3,4oxadiazole2thiones 5ah. 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. An environmental friendly method was developed for preparing benzothiazole derivatives via the reaction of ortho.
Hofmann in 1879, while use of 2sulfanylbenzothiazoles as vulcanization accelerators for natural and synthetic rubber was. Therapeutic advancement of benzothiazole derivatives in. The first step is to select effective compounds by simple, rapid and. Benzothiazole is a privileged bicyclic ring system with multiple applications. Us81538b2 benzothiazole and benzooxazole derivatives. Extraction and analysis of various benzothiazoles from.
Synthesis of new benzothiazole derivatives bearing. Synthesis of some new biologically active benzothiazole derivatives bull. Review article recent advances in the chemistry and biology of benzothiazoles rupinder k. Benzothiazole c7h5ns cid 7222 structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety. However, pet and spect, due to their low spatial resolution, are unable to detect individual plaques and earlystage amyloid deposition. The structural formula of all derivatives was confirmed and characterized by elemental analysis and spectral studies. Screening and molecular docking of novel benzothiazole. Pdf benzothiazole derivatives as anticancer agents researchgate. In vitro antitumor and antiviral activities of new benzothiazole and 1,3,4oxadiazole2thione derivatives. Convenient route synthesis of some new benzothiazole derivatives and their pharmacological screening as antimicrobial agents published.
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