15965-31-8Relevant articles and documents
Synthesis and characterization of new N-(4-(4-chloro-1H-imidazol-1-yl)-3- methoxyphenyl)amide/sulfonamide derivatives as possible antimicrobial and antitubercular agents
Ranjith, Pakkath Karuvalam,Pakkath, Rajeesh,Haridas, Karickal R.,Kumari, Suchetha N.
, p. 354 - 365 (2014/01/17)
In this paper we report the SAR studies of a series of N-(4-(4-chloro-1H- imidazol-1-yl)-3-methoxyphenyl)amide and N-(4-(4-chloro-1H-imidazol-1-yl)-3- methoxyphenyl)sulfonamide derivatives 6(a-o) and 7(a-o), were synthesized in good yields and characterized by 1H NMR, 13C NMR and mass spectral analyses. The preparation of the key intermediate highlights an optimized palladium catalyzed (Pd2(dba)3/RuPhos) Buchwald cross-coupling of intermediate 2 and 3. The newly synthesized compounds were evaluated for their in vitro antibacterial activity against Staphylococcus aureus, (Gram-positive), Escherichia coli and Klebsiella pneumoniae (Gram-negative), antifungal activity against Candida albicans, Aspergillus flavus and Rhizopus sp. and antitubercular activity against Mycobacterium tuberculosis H37Rv, Mycobacterium smegmatis, Mycobacterium fortuitum and MDR-TB strains. The synthesized compounds displayed interesting antimicrobial activity. The compounds 7d, 7f, 7h and 7n displayed significant activity against Mycobacterium tuberculosis H37Rv strain.
Novel Bicyclic Pyridinones
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Page/Page column 30, (2012/10/08)
Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
Novel imidazobenzazepine derivatives as dual H1/5-HT 2A antagonists for the treatment of sleep disorders
Gianotti, Massimo,Corti, Corrado,Fratte, Sonia Delle,Di Fabio, Romano,Leslie, Colin P.,Pavone, Francesca,Piccoli, Laura,Stasi, Luigi,Wigglesworth, Mark J.
supporting information; experimental part, p. 5069 - 5073 (2010/10/20)
A novel imidazobenzazepine template (5a) with potent dual H 1/5-HT2A antagonist activity was identified. Application of a zwitterionic approach to this poorly selective and poorly developable starting point successfully delivered a class of high quality leads, 3-[4-(3-R1-2-R-5H-imidazo[1,2-b][2]benzazepin-11-yl)-1-piperazinyl]- 2,2-dimethylpropanoic acids (e.g., 9, 19, 20, and 21), characterized by potent and balanced H1/5-HT2A receptor antagonist activities and good developability profiles.