- IMIDAZO[2,1-B]THIAZOLE AND 5,6-DIHYDROIMIDAZO[2,1-B]THIAZOLE DERIVATIVES USEFUL AS S100-INHIBITORS
-
A compound of formula (I) or a pharmaceutically acceptable salt thereof. The compound is useful for use in the treatment of cancer, an inflammatory disorder,an autoimmunity disorder or a neurodegenerative disorder.
- -
-
-
- Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)- thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors
-
4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (4a) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand 4a with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water molecule.
- Malmstroem, Jonas,Viklund, Jenny,Slivo, Can,Costa, Ana,Maudet, Mickael,Sandelin, Catrin,Hiller, Goesta,Olsson, Lise-Lotte,Aagaard, Anna,Geschwindner, Stefan,Xue, Yafeng,Vasaenge, Mervi
-
p. 5919 - 5923
(2012/11/07)
-
- Synthesis and comparative study of anti-mycobacterium activity of a novel series of fluoronitrobenzothiazolopyrazoline regioisomers
-
In an attempt to find a new and a safer drug for tuberculosis, we have synthesized a series of fluoronitrobenzothiazolopyrazolines for antitubercular activity. The series comprises three subclasses: fluorobenzothiazolopyrazolines (11a-f), fluoronitrobenzo
- Hazra,Nargund,Rashmi,Chandra, J. N. Narendra Sharath,Nandha,Harish
-
experimental part
p. 137 - 146
(2012/03/27)
-
- NOVEL COMPOUNDS
-
The invention relates to tricyclic derivatives, and their use in treating diseases and conditions mediated by antagonism of the mGluR5 receptor, in particular substance related disorders. In addition, the invention relates to compositions containing the derivatives and processes for their preparation.
- -
-
Page/Page column 49
(2011/12/14)
-
- Antimycobacterial activity of some synthesized fluorinated benzothiazolo imidazole compounds
-
4-Fluoro-3-chloroanilline treated with potassium thiocyanate in presence of glacial acetic acid and bromine was converted into 2-amino-6-fluoro-7- chlorobenzothiazole, resulting into 2-amino benzothiazole. The synthesized compound in presence of 2-phenyl-
- Sathe,Jaychandran,Sreenivasa,Jagtap
-
experimental part
p. 830 - 834
(2012/03/09)
-
- 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)
-
- Synthesis and antidiabetic activity of 2-amino [5′(4- sulphonylbenzylidine)-2,4-thiazolidinedione]-7-chloro-6-fluorobenzothiazole
-
A new series of 2-amino[5′(4-sulphonylbenzylidine)-2,4- thiazolidinedione]-7-chloro-6-fluorobenzothiazole were synthesized. The structures of the compounds were continued by UV-Vis, IR and NMR spectroscopy. The title compounds were screened for their antidiabetic activity on albino rats.
- Pattan,Suresh,Pujar,Reddy,Rasal,Koti
-
p. 2404 - 2408
(2007/10/03)
-
- Synthesis and antifungal activity against strains of Candida albicans of 6-fluoro-4(5 or 7)-chloro-2-(difluorobenzoyl)aminobenzothiazoles
-
A series of 6-fluoro-4-(5 or 7)-chloro-2-(difluorobenzoyl) aminobenzothiazoles 3a-r were prepared to investigate their potential biological activity. In this work, the results of their in vitro antifungal activity against some strains of Candida albicans
- Armenise, Domenico,De Laurentis, Nicolino,Reho, Antonia,Rosato, Antonio,Morlacchi, Flaviano
-
p. 771 - 775
(2007/10/03)
-
- Quinolonecarboxylic Acids. 2. Synthesis and Antibacterial Evaluation of 7-Oxo-2,3-dihydro-7H-pyridobenzothiazine-6-carboxylic Acids
-
A series of pyridobenzothiazine acid derivatives was synthesized and their in vitro antibacterial activity was evaluated.The 1,4-benzothiazine intermediates, which by Gould-Jacobs quinoline synthesis produced pyridobenzothiazine acids, were prepared by hydrolytic basic cleavage of substituted 2-aminobenzothiazoles and successive cyclocondensation with 1-bromo-2-chloroethane or alternatively with monochloroacetic acid, hence reduction by LiAlH4.The pyridobenzothiazine acids 10c, 30, and 31 show potent antibacterial activities against Gram-positive and Gram-negative pathogens.Structure-activity relationships are discussed.The compound 9-fluoro-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyridobenzothiazine-6-carboxylic acid (31) (MF-934) has been found to possess, together with the antibacterial activity, a weak acute toxicity and interesting pharmacokinetic characteristics in several animal species (rat, dog, monkey, man).
- Cecchetti, Violetta,Fravolini, Arnaldo,Fringuelli, Renata,Mascellani, Giuseppe,Pagella, Piergiuseppe,et al.
-
p. 465 - 473
(2007/10/02)
-