62179-79-7Relevant academic research and scientific papers
Identification of Anti-Mycobacterial Biofilm Agents Based on the 2-Aminoimidazole Scaffold
Nguyen, T. Vu,Minrovic, Bradley M.,Melander, Roberta J.,Melander, Christian
, p. 927 - 937 (2019/03/26)
Tuberculosis (TB) remains a significant global health problem for which new therapeutic options are sorely needed. The ability of the causative agent, Mycobacterium tuberculosis, to reside within host macrophages and form biofilm-like communities contributes to the persistent and drug-tolerant nature of the disease. Compounds that can prevent or reverse the biofilm-like phenotype have the potential to serve alongside TB antibiotics to overcome this tolerance, and decrease treatment duration. Using Mycobacterium smegmatis as a surrogate organism, we report the identification of two new 2-aminoimidazole compounds that inhibit and disperse mycobacterial biofilms, work synergistically with isoniazid and rifampicin to eradicate preformed M. smegmatis biofilms in vitro, are nontoxic toward Galleria mellonella, and exhibit stability in mouse plasma.
Lipopeptide Compounds and Their Use
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, (2011/10/04)
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as “LP compounds”), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
SUBSTITUTE 4-ARYLBUTYRIC ACID DERIVATIVES AS MATRIX METALLOPROTEASE INHIBITORS
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, (2008/06/13)
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have generalized formula (I) wherein R represents C6-C12 alkyl; C5-C12 alkoxy; C5-C12 alkylthio; a polyether of formula RO(C2H4O)a- in which a is 1 or 2 and R is C1-C5 alkyl, phenyl, or benzyl; and substituted alkynyl of formula R(CH2)b-CC-; in which b is 1-10 and R is H-, HO-, or RO- in which R is C1-C3 alkyl, phenyl, or benzyl. The alkyl, phenyl, and benzyl portions of R may bear at least one pharmaceutically-acceptable substituent. The subscript n is 2-4. R represents phenyl; imidoyl of 4-12 carbon atoms; (3H)-benzo-1,2,3-triazin-4-on-3-yl; N-saccharinyl; (2H)-phthalazin-1-on-2-yl; 2-benzoxazolin-2-on-3-yl; 5,5-dimethyloxazolidine-2,4-dion-3-yl; and thiazolidine-2,4-dion-3-yl; with the phenyl and benzo portions of R permissibly bearing at least one pharmaceutically-acceptable substituent. Pharmaceutically acceptable salts of these materials are also included.
SUBSTITUTED 4-ARYLBUTYRIC ACID DERIVATIVES AS MATRIX METALLOPROTEASE
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, (2008/06/13)
Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula STR1 wherein R 1 represents C 6-C
