731822-49-4Relevant academic research and scientific papers
Synthesis and antibacterial evaluation of new, unsymmetrical triaryl bisamidine compounds
Nguyen, Son T.,Williams, John D.,Butler, Michelle M.,Ding, Xiaoyuan,Mills, Debra M.,Tashjian, Tommy F.,Panchal, Rekha G.,Weir, Susan K.,Moon, Chaeho,Kim, Hwa-Ok,Marsden, Jeremiah A.,Peet, Norton P.,Bowlin, Terry L.
supporting information, p. 3366 - 3372 (2014/07/22)
Herein we describe the synthesis and antibacterial evaluation of a new, unsymmetrical triaryl bisamidine compound series, [Am]-[indole]-[linker]-[HetAr/ Ar]-[Am], in which [Am] is an amidine or amino group, [linker] is a benzene, thiophene or pyridine ring, and [HetAr/Ar] is a benzimidazole, imidazopyridine, benzofuran, benzothiophene, pyrimidine or benzene ring. When the [HetAr/Ar] unit is a 5,6-bicyclic heterocycle, it is oriented such that the 5-membered ring portion is connected to the [linker] unit and the 6-membered ring portion is connected to the [Am] unit. Among the 34 compounds in this series, compounds with benzofuran as the [HetAr/Ar] unit showed the highest potencies. Introduction of a fluorine atom or a methyl group to the triaryl core led to the more potent analogs. Bisamidines are more active toward bacteria while the monoamidines are more active toward mammalian cells (as indicated by low CC 50 values). Importantly, we identified compound P12a (MBX 1887) with a relatively narrow spectrum against bacteria and a very high CC50 value. Compound P12a has been scaled up and is currently undergoing further evaluations for therapeutic applications.
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8,-tetrahydro-imidazo[1,2,-a]pyridines as antiprotozoal agents
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Page/Page column 17; 21, (2008/06/13)
A method for treating a microbial infection, including an infection from a protozoan pathogen, such as Trypanosoma brucei rhodesiense and Plasmodium falciparum, in a subject in need thereof by administering to the subject an effective amount of a dication
Novel dicationic imidazo[1,2-a]pyridines and 5,6,7,8-tetrahydro-imidazo[1, 2-a]pyridines as antiprotozoal agents
Ismail, Mohamed A.,Brun, Reto,Wenzler, Tanja,Tanious, Farial A.,Wilson, W. David,Boykin, David W.
, p. 3658 - 3664 (2007/10/03)
2-[5-(4-Amidinophenyl)-furan-2-yl]-5,6,7,8-tetrahydro-imidazo [1,2-a]pyridine-6-carboxamidine acetate salt (7) was synthesized from 2-[5-(4-cyanophenyl)-furan-2-yl]-imidazo[1,2-a]pyridine-6-carbonitrile (4a), through the bis-O-acetoxyamidoxime followed by
