- Visible light-mediated oxidative quenching reaction to electron-rich epoxides: Highly regioselective synthesis of α-bromo (di)ketones and mechanism study
-
A novel and simple procedure was developed for the regioselective synthesis of α-bromo (di)ketones from electron-rich epoxides via visible light photoredox catalysis. Through optimization of solvent and light source, the reaction can be rapidly achieved under mild conditions. Moreover, the possible reaction mechanism was proposed and further supported by control experiments.
- Guo, Lin,Yang, Chao,Zheng, Lewei,Xia, Wujiong
-
supporting information
p. 5787 - 5792
(2013/09/12)
-
- Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2, 1, b]-benzothiazole derivatives
-
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
-
experimental part
p. 717 - 724
(2012/04/05)
-
- Synthesis and preliminary in-vitro cytotoxic activity of novel substituted diaryl-imidazo [2,1,b]-benzothiazole derivatives
-
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
-
experimental part
p. 717 - 724
(2012/05/20)
-
- Synthesis and antibacterial activity of a novel series of 2,3-diaryl-substituted-imidazo(2,1-b)-benzothiazole derivatives
-
Benzothiazole and imidazole compounds are extensively studied heterocyclics due to their wide spectrum of bioactivities. Among them, the imidazo(2,1-b)-benzothiazole derivatives are pharmacologically important because of their immunostimulant, anti-inflammatory, antifungal, antimicrobial, antitumor, and other activities. In the present research work, a novel series of 2,3-diaryl-substituted imidazo(2,1-b)-benzothiazoles 13a-o have been synthesized by reaction of substituted 2-aminobenzothiazoles 1-8 and an appropriately substituted a-bromo-1-(4″-substituted)-phenyl-2-(4′- substituted)-phenyl-1-ethanones 9-12 in the presence of anhydrous acetonitrile. They were characterized by physicochemical, elemental, and spectral (IR, 1H-NMR, and Mass) data. All the synthesized compounds were screened for their in-vitro antibacterial activity against Gram-positive, Gram-negative bacteria. The investigation of antibacterial screening data revealed that most of the compounds tested have demonstrated congruent activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa as compared with the standard ampicillin. Among the series, compounds 13d, 13h, and 13m exhibited excellent an antibacterial activity profile as compared with the standard. In summary, preliminary results indicate that some of the newly synthesized title compounds exhibited promising antibacterial activities and they warrant more consideration as prospective antimicrobials.
- Palkar, Mahesh,Noolvi, Malleshappa,Sankangoud, Ramappa,Maddi, Veeresh,Gadad, Andanappa,Nargund, Laxmi Venkat G.
-
experimental part
p. 353 - 359
(2011/07/08)
-
- UREIDE DERIVATIVE AND USE THEREOF FOR MEDICAL PURPOSES
-
This invention relates to a pharmaceutical comprising, as an active ingredient, a ureide derivative represented by formula: or a pharmaceutically acceptable salt thereof. The ureide derivative or a pharmaceutically acceptable salt thereof according to the present invention is useful for relieving pain and treating or preventing neuropathic pain.
- -
-
Page/Page column 43
(2009/01/24)
-
- A novel synthesis of arylpyrrolo[1,2-a]pyrazinone derivatives
-
Some aryl-2-methyl-1-pyrrolo[1,2-a]pyrazinones were designed and prepared to study the Structure-Activity Relationships (SAR) of pyrrolo[1,2-a]pyrazinone derivatives. With methyl pyrrole-2-carboxylate as the starting material, the title compounds were prepared through N-alkylation and two novel cyclizations. Eleven aryl-2-methyl-1-pyrrolo[1,2-a]pyrazinone derivatives not previously reported in the literature are presented in this paper. Some of them show potent anti-inflammatory and analgesic activities.
- Wang, Fei,Wang, Jiawei,Zhang, Shoufang
-
p. 574 - 582
(2007/10/03)
-