- An efficient one-pot synthesis of 2-aminobenzothiazoles from substituted anilines using benzyltrimethylammonium dichloroiodate and ammonium thiocyanate in DMSO:H2O
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Treatment of a variety of substituted anilines with benzyltrimethylammonium dichloroiodate (1.2 equiv) and ammonium thiocyanate (1.0 equiv) in DMSO:H2O (9:1) at 70 °C gave the corresponding 2-aminobenzothiazoles in excellent isolated yields (75–97%; ave. yield for all substrates = 90%). The reaction worked well for 2(4)-mono-, 2,4-di-, or 3,4,5-tri-substituted anilines, and a wide range of both electron donating groups (MeO, HO, CF3O, Me) and electron withdrawing groups (NO2, CN, CO2Et, CO2H, Cl, F) were well tolerated. This method provides a useful alternative to other methods that are either less efficient (requiring 3–7 fold equivalents of reagents) or utilize highly toxic and corrosive liquid Br2 as the oxidizing agent.
- Dass, Reuben,Peterson, Matt A.
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supporting information
(2021/10/04)
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- Dye compounds
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The present invention relates to dye compounds represented by Formulae I and II, which are described in the specification. The dye compounds of the present invention have markedly improved quantum yields and emit strong fluorescence compared to existing cyanine dyes. Due to these advantages, the dye compounds of the present invention can find applications in various fields, for example, as probes for various biological systems where optical imaging is required. Particularly, the dye compounds of the present invention can be used as mitotrackers capable of labeling and tracking mitochondria. Therefore, the dye compounds of the present invention can be used to quantitatively image mitochondria in live tissues and cells. Furthermore, the dye compounds of the present invention can be applied as pH probes for measuring the pH of live cells.
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Page/Page column 64-65
(2019/11/26)
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- Compound with dopamine D3 receptor adjusting activity, and applications thereof
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The invention relates to a compound with dopamine D3 receptor adjusting activity, and applications thereof, and more specifically discloses dopamine receptor D3R as a novel target of post-traumatic stress disorder (PTSD) in prevention, treatment/or auxiliary treatment of PTSD, and screening of anti-PTSD medicines, and relates to applications of a compound with dopamine receptor D3R adjusting activity in preparation of medicines used for preventing, treatment and/or auxiliary treatment of PTSD.
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Paragraph 0155; 0159
(2019/03/22)
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- Dye compounds
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The present invention relates to a dye compound represented by chemical formula I. According to the present invention, the dye compound has an effect of remarkably improved quantum efficiency compared to an existing cyanine dye, and can be effectively used in a wide range of fields such as a probe or the like with respect to various biological systems requiring an optical image by exhibiting strong fluorescence. In particular, the dye compound can quantitatively image mitochondria in a living body or a cell tissue since the dye compound can be utilized as a Mitotracker capable of marking and tracing mitochondria. Moreover, the dye compound can be applied as a pH probe capable of checking pH values of live cells.COPYRIGHT KIPO 2018
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Paragraph 0132; 0144-0147
(2018/08/24)
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- Chrysin-benzothiazole conjugates as antioxidant and anticancer agents
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7-(4-Bromobutoxy)-5-hydroxy-2-phenyl-4H-chromen-4-one, obtained from chrysin with 1,4-dibromobutane, was combined with a wide range of 6-substituted 2-aminobenzthiazoles, which had been prepared from the corresponding anilines with potassium thiocyanate. Free radical scavenging efficacies of newer analogues were measured using DPPH and ABTS assays, in addition to the assessment of their anticancer activity against cervical cancer cell lines (HeLa and CaSki) and ovarian cancer cell line (SK-OV-3) implementing the SRB assay. Cytotoxicity of titled compounds was checked using Madin-Darby canine kidney (MDCK) non-cancer cell line. Overall, 6a-r indicated remarkable antioxidant power as DPPH and ABTS+ scavengers; particularly the presence of halogen(s) (6g, 6h, 6j-6l) was favourable with IC50 values comparable to the control ascorbic acid. Unsubstituted benzothiazole ring favored the activity of resultant compounds (6a and 6r) against HeLa cell line, whereas presence of chlorine (6g) or a di-fluoro group (6k) was a key to exert strong action against CaSki. Moreover, a mono-fluoro (6j) and a ketonic functionality (6o) were beneficial to display anticipated anticancer effects against ovarian cancer cell line SK-OV-3. The structural assignments of the new products were done on the basis of IR, 1H NMR, 13C NMR spectroscopy and elemental analysis.
- Mistry, Bhupendra M.,Patel, Rahul V.,Keum, Young-Soo,Kim, Doo Hwan
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supporting information
p. 5561 - 5565
(2015/11/17)
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- A novel system for the synthesis of 2-aminobenzthiazoles using sodium dichloroiodate
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2-Aminobenzthiazole is a privileged scaffold with a range of biological activities. However, to date, an efficient protocol for the synthesis of this ring system using aniline as a starting material has been lacking. Herein, for the first time, we describe a highly efficient and mild protocol for the synthesis of 2-aminiobenzthiazole using NaICl Georg Thieme Verlag Stuttgart ? New York.
- Telvekar, Vikas N.,Bachhav, Harshal M.,Bairwa, Vinod Kumar
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p. 2219 - 2222
(2012/10/30)
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- Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2, 1, b]-benzothiazole derivatives
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A novel series of substituted diaryl imidazo[2, 1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted a-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.
- Malik, Jitender K.,Noolvi, Malleshappa N.,Manvi, Fakkirappa V.,Nanjwade,Patel, Harun M.,Manjula,Rao, Mallikarjuna C.,Barve, Ashutosh
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experimental part
p. 717 - 724
(2012/04/05)
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- Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2,1,b]-benzothiazole derivatives
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A novel series of substituted diaryl imidazo[2,1-b]benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compounds 8p, 8u and 8y were found most effective with an IC50 range of 0.56-27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.
- Malik, Jitender K.,Noolvi, Malleshappa N.,Manvi, Fakkirappa V.,Nanjwade,Patel, Harun M.,Manjula,Mallikarjuna Rao,Barve, Ashutosh
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experimental part
p. 717 - 724
(2012/05/20)
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- NOVEL DOPAMINE D3 RECEPTOR LIGANDS, THE PREPARATION AND USE THEREOF
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The invention discloses novel piperazine derivatives represented by formula I having activity for modulating dopamine D3 receptor, their stereoisomers, pharmaceutical salts, solvates, and the pharmaceutical compositions containing such compounds, their preparation and the use of such compounds for preventing or treating the diseases correlated with central nervous system disorder, such as Parkinson's disease, schizophrenia, drug addiction and relapse and the like, as well as the use of such compounds for kidney protection and immune modulation, or as implemental medicine for researching the function of D3R and the diseases correlated with disorder of D3R function.
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Page/Page column 16
(2011/09/12)
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- NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME
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The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson''s disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.
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Page/Page column 10
(2012/01/13)
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- NOVEL CC-1065 ANALOGS AND THEIR CONJUGATES
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This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.
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Page/Page column 156
(2010/06/17)
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- AMYLOID-IMAGING AGENTS
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A molecular probe for use in the detection of amyloid in a subject includes a dibenzothiazole derivative.
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Page/Page column 14-15
(2009/05/28)
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- Phenylimidazole derivatives as new inhibitors of bacterial enoyl-ACP reductase FabK
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Novel FabK inhibitors with antibacterial activity against Streptococcus pneumoniae were synthesized and evaluated. Through SAR studies of our initial hit compound 2-(1H-benz[d]imidazol-2-ylthio)-N-(6-methoxycarbonylbenzo[d]thiazol-2-yl)acetamide, a series of novel phenylimidazole derivatives were discovered as potent FabK inhibitors.
- Kitagawa, Hideo,Ozawa, Tomohiro,Takahata, Sho,Iida, Maiko
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p. 4982 - 4986
(2008/03/13)
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- INHIBITORS OF HISTONE DEACETYLASE
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The invention relates to a series of compounds useful for inhibiting histone deacetylase (HDAC) enzymatic activity. The invention also provides a method for inhibiting histone descetylase in a cell using said compounds as well as a method for treating cell proliferative diseases and conditions using said HDAC inhibitors. Further, the invention provides pharmaceutical compositions comprising the HDAC inhibiting compounds and a pharmaceutically acceptable carrier.
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Page/Page column 100
(2010/02/14)
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- Mono azo dyes
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The invention relates to novel azo dyestuffs of formula (I), the use of such compounds and/or mixtures for printing recording materials, especially paper or papery substrates, textile fibre materials, plastic films and plastic transparencies by the inkjet printing process and also to the recording materials printed thereby.
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- Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors
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PCT No. PCT/US94/09139 Sec. 371 Date Jan. 24, 1996 Sec. 102(e) Date Jan. 24, 1996 PCT Filed Aug. 23, 1994 PCT Pub. No. WO95/06030 PCT Pub. Date Mar. 2, 1995The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.
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- Salt of 6-carboxy-3-methylbenzothiazolone hydrazone hydrate in colorimetric determination of hydrogen peroxide
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Water soluble salts of hydrazone compounds react quickly with aniline compounds in the presence of a peroxidase and hydrogen peroxide to provide a color which can be measured spectrophotometrically or visually, either in solution or when incorporated in a device for the measurement of analytes of interest. These water-soluble hydrazone salts are useful in determining hydrogen peroxide or an analyte which reacts to produce hydrogen peroxide in an aqueous liquid, by, in the presence of a substance having peroxidative activity, physically contacting a sample of a liquid with a dye-forming composition comprising a water-soluble salt of a hydrazone compound and a substituted or unsubstituted aniline compound to produce a colored dye; and detecting the dye formed as a result of the presence of hydrogen peroxide or an analyte which reacts to produce hydrogen peroxide.
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- Studies in antiparasitic agents: Part 17 - Synthesis of 2-acylamino-6-substituted-benzthiazoles as potential anthelmintic agents
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The syntheses of a series of 2-acetamido-6-alkoxycarbonylbenzthiazoles (12-17), 2-alkoxycarbonylamino-6-alkoxycarbonylbenzthiazoles (18-27), 2-alkoxycarbonylamino-6-benzoylbenzthiazoles (29,30), and 2,2'-dicarbalkoxyamino-6,6'-dibenzthiazolyl oxides, sulphides and sulphones (38-43) have been carried out as structural congeners of tioxidazole (2) and related anthelmintics (3 and 4).All the benzthiazoles have been evaluated for their anthelmintic activity against Ancylostoma ceylanicum in hamsters, Hymenolepis nana in mice and Litomosoides carinii in cotton rats.Compound 15 showes more than 85percent clearance of hookworms (A. ceylanicum) at an oral dose of 250 mg/kg, while compound 24 eliminates nearly 90percent of the microfilariae in blood and also kills 50percent of the adult filarial worms at an intraperitonial dose of 30 mg/kg * 5 from the cotton rats infected with Litomosoides carinii.
- Naim, S Shawkat,Singh, Sudhir K,Sharma, Satyavan
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p. 494 - 498
(2007/10/02)
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