Synthesis, characterization and antibacterial activity of. Synthesis of novel benzothiazole compounds with an extended conjugated system peddiahgari vasu govardhana reddy, yangwei lin, and huantsung chang department of chemistry, national taiwan university, taipei106, taiwan email. Biologically important benzoxazoles and benzothiazoles were merged with quinolone nucleus. Cell cycle is an ordered set of events, leading to cell growth and. 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. After cooling to room temperature it was poured into the crushed ice with stirring.
Pdf benzothiazole, benzotriazole, and their derivates in. Benzothiazole, benzotriazole, and their derivates in clothing textilesa potential source of environmental pollutants and human exposure. Extraction and analysis of various benzothiazoles from. The resulting solution was stirred at oc under o 2 monitored by tlc and gc. Benzothiazole derivatives have been studied extensively and found to have diverse chemical reactivity and broad spectrum of biological activity such as antitumor. Synthesis of new benzothiazole derivatives bearing. Since oo is my preferred word program, does anyone know if there are any pdf merge programs that would allow me to add my oo documents to a pdf. The product obtained was used for the synthesis of other benzothiazole derivatives. I just wondered if there was an easier way to do it, instead of having to save all the small oo documents into pdf first. Some new hydrazino group substituted benzothiazole derivatives have been synthesized and their characterization was done by ir, nmr and mass spectral data. Design, synthesis and anticancer screening of novel.
A mixture of 1, 3 benzothiazole 2carboxyhydrazide 2 0. In this study, we propose to combine benzothiazole, thiourea and phenols in the. The effect of benzothiazole derivatives on tumor volume, viable and nonviable cell count, and survival time was measured. Synthesis and antimicrobial activity of some new 2.
It is a two membered ring heterocyclic moiety, weak base. Review article recent advances in the chemistry and biology of benzothiazoles rupinder k. Pdf design, synthesis and mode of action of some new 24. Evaluation of inhibitory effects of benzothiazole and 3. Firefly luciferin can be considered a derivative of benzothiazole. Yalcina apharmaceutical chemistry department, faculty of pharmacy, ankara university, ankara, turkey. 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. Ibrahim 2,3, anuj tripathi 4 and chetti prabhakar 4 1 department of medicinal chemistry, faculty of pharmacy, mansoura university, mansoura 35516, egypt 2 department of pharmacognosy, faculty of pharmacy, mansoura university, mansoura. The myriad spectrum of medicinal properties associated with benzothiazole related drugs has encouraged the medicinal chemists to synthesize a large number of novel therapeutic agents. A new and efficient method for the synthesis of pyrimido2. Collecting the lc peaks of interest and subsequent analysis by gcms offers an alternative route for some of the benzothiazole derivatives see below. The first step is to select effective compounds by simple, rapid and.
Synthesis of novel benzothiazole compounds with an. These reports prompted us to synthesize some new benzothiazole derivatives containing benzimidazole or imidazoline moiety. The benzothiazole ring is an important scaffold for the preparation of dyes used in the identification of lanthanide metal ions in aqueous media. The present investigation indicates that benzothiazole derivative showed significant antitumor activity in eac bearing mice. Antibacterial activity of novel benzothiazole derivatives was evaluated by. Table5 and figure2 administration of benzothiazole derivatives reduces the tumor volume. 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. The antimicrobial activities of these synthesized compounds was done by cupplate diffusion method in dmso against some gram positive and gram negative bacteria. A sealed pressure vessel was charged with benzothiazole 68 mg, 0. Synthesis, characterization and biological evaluation of. Benzothiazole ring made from thiazole ring fused with benzene ring. Synthesis and biological evaluation of sulfonamide. Benzothiazole derivatives have been studied and found to have various chemical reactivity and biological activity. These compounds were evaluated as inhibitors for types a and b mao enzymes.
Benzothiazole derivatives have been studied extensively and found to have diverse chemical reactivity and broad spectrum of biological activity such as antitumor agents, antimicro bial,46 analgesics, 7 antiinflammatory, 79 anti hiv, 10 antileish manial,11 etc. Our team of scientists has experience in all areas of research including life science, material science, chemical synthesis, chromatography, analytical and many others. Antibacterial benzothiazole derivatives 5 us8691185 b269 us 548,014 apr 8, 2014 prasad raje et al. Convenient route synthesis of some new benzothiazole. Although the parent compound, benzothiazole is not widely used, many of its derivatives are found in commercial products or in nature. The most interesting series of compounds were those combining a 5fluoro group with two oxygenated.
The analogues of benzothiazole and its derivatives have a significant role in research area especially in synthetic, medicinal and pharmaceutical. Synthesis, characterization and biological evaluation of some benzothiazole derivatives. Convenient route synthesis of some new benzothiazole derivatives and their pharmacological screening as antimicrobial agents published. Synthesis of new quinolone derivatives linked to benzothiazole or. Short communication synthesis of amide and urea derivatives of benzothiazole as raf1 inhibitor eun young song a, navneet kaur a, miyoung park a, yinglan jin a, kyeong lee a, guncheol kim b, ki youn lee b, jee sun yang c, jae hong shin d, kyyoub nam d, kyoung tai no c,d, gyoonhee han c, a korea research institute of bioscience and biotechnology kribb, 52 eoendong, yuseonggu, daejeon. Benzothiazole is a class of heterocyclic compound having two hetero atoms namely sulphur and nitrogen. Introduction derivatives have been associated with a number of highprofile corporate events that roiled the global financial markets over the past two decades. Benzothiazole derivatives play a vital role in biological fields such as antitubercular, antiallergic, antiinflammatory and fungicidal activities 14.
Citric acid catalyzed microwave irradiated solvent free. Synthesis of analogues substituted in the benzothiazole ring was achieved via the reaction of. The synthesised compounds were characterized and evaluated for antimicrobial activities. Bta derivatives possesses broad spectrum biological. An efficient strategy for the synthesis of various 2mercaptobenzothiazole derivatives proceeds from ohaloaniline derivatives and carbon disulfide via a tandem reaction in the presence of 1,8diazabicyclo5. Us81538b2 us12337,433 us33743308a us81538b2 us 81538 b2 us81538 b2 us 81538b2 us 33743308 a us33743308 a us 33743308a us 81538 b2 us81538 b2 us 81538b2 authority us united states prior art keywords yl 1h benzo pyrrolidin piperidin prior art date 20071220 legal status the legal status is an assumption and is not a legal conclusion.
The most important industrial applications of benzothiazole derivatives are recognized as corrosion inhibitors and surfaceactive chelating agents for mineral processing. Synthesis, characterization and carbonic anhydrase inhibitory. A benzothiazole derivative 5g induces dna damage and potent g2m arrest in cancer cells. Pdf benzothiazole derivatives as anticancer agents researchgate. An environmentally benign catalyst for synthesis of benzothiazoles and benzoxazole derivatives in aqueous medium monika a patil, panchsheela a ubale, shrikrishna s karhale and vasant b helavi department of chemistry, rajaram college, kolhapur, 416004, maharashtra, india abstract. Recent studies have shown that numerous benzothiazole derivatives exhibit hmao inhibitory activity in the micromolar concentration range. Evaluation of a new benzothiazole derivative with antioxidant activity. August 29, 2017 3446 1hpyrano2,3dpyrimidin6yl3oxopropanenitrile 6 in 87% yield figure 3. Pandeya 1kmch college of pharmacy, kovai estate, kalapatti road, coimbatore,india. Benzoxazole is an aromatic organic compound with a molecular formula c 7 h 5 no, a benzenefused oxazole ring structure, and an odor similar to pyridine. Abstract various substituted 2aminobenzothiazoles have been synthesized cyclocondensation of various. The rapid evolution of antibiotic resistance poses a serious. Benzothiazole is an aromatic heterocyclic compound with the chemical formula c 7h 5ns.
Biological evaluation of benzothiazole thiourea derivatives, plant extracts and their combinations vrushali patil 1, mrunal ghagsawant2, anjali narayakkadan3, ashish asrondkar, anil bobade1 and mira ramaiya2 1. Benzothiazole and its derivatives bts are high production volume chemicals that have been used for several decades in a large number of industrial and consumer products, including vulcanization accelerators, corrosion inhibitors, fungicides, herbicides, algicides, and ultraviolet uv light stabilizers. Pdf benzothiazole bta belongs to the heterocyclic class of bicyclic compounds. Benzothiazole derivatives possess a wide spectrum of biological applications such as antitumor 2652, antimicrobial 5483, schictosomicidal 84, antiinflammatory 8593, anticonvulsants 94102, antidiabetic 103108, antipsychotic 109 and diuretic 111 etc. Several benzothiazole derivatives are used commercially, and widespread use of these. In continuation of our research work on benzothiazole derivatives 31, we are reporting the synthesis of 6substituted n4,5dihydro1himidazol. Gc gas chromatography was performed with a pe 8420 gas chromatograph perkinehner, ijberlin gen with a flame ionization detector. Benzothiazole derivatives as potential antiinfective agents. General procedures for 2phenyl benzothiazole derivatives from phenylacetic acid and benzothiazole. Evaluation of inhibitory effects of benzothiazole and 3aminobenzothiazolium derivatives on dna topoisomerase ii by molecular modeling studies e. A benzothiazole derivative 5g induces dna damage and. A series of 2 aryl benzothiazole derivatives were synthesized by the condensation reaction of 2 aminothiophenol and aryl aldehyde in presence of catalytic amount of citric acid under microwave irradi ation and solvent free condition s without metals or reactive stoichiometric oxidants in good yield. Benzothiazole derivatives as potential antiinfective.
As an afterthought, i know that oo can be converted to pdf, and thats very cool. 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. From the view point of molecular design, joining two or. Antileishmanial activities of benzothiazole derivatives. Therapeutic advancement of benzothiazole derivatives in. Benzothiazole derivative compounds, compositions, and uses 6 wo2014036242 a370 pctus20. It has been demonstrated that benzothiazole derivatives have potential. Under no circumstances may this pdf file be placed on a network of any sort without our express permission.
Novel benzothiazole derivatives with enhanced biological activity 4 wo2016079688 a168 pctib2015 058919 nov 11, 2015 christine schmitt et al. The onepot threecomponent reaction of 2aminobenzothiazole, benzaldehyde derivatives and. The parent benzothiazole derivative 1d was synthesized by jacobson method using lawessons reagent scheme 1. Synthesis of some new biologically active benzothiazole. The synthesis was carried out by condensation of different aromatic aldehydes with benzothiazole derivative using different procedures. The synthesis of some new hydrazone derivatives containing. 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. Some clinically and commercially approved drugs including carboxyamidotriazole 11, tazobactam 12, and cifatrizine were found to possess the 1,2,3triazole core in their structures. Us81538b2 benzothiazole and benzooxazole derivatives. Bta derivatives possesses broad spectrum biological activities such. Synthesis, characterization and antibacterial activity o f substituted benzothiazole derivatives prachi k.
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