21970-14-9Relevant articles and documents
AZETIDINE AND SPIROAZETIDINE COMPOUNDS AND USES THEREOF
-
Page/Page column 45; 46; 49-51; 57-58, (2021/12/30)
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
Structural Studies on 4,5-Disubstituted 2-Aminoimidazole-Based Biofilm Modulators that Suppress Bacterial Resistance to β-Lactams
Su, Zhaoming,Yeagley, Andrew A.,Su, Rui,Peng, Lingling,Melander, Christian
, p. 2030 - 2039 (2013/01/15)
A library of 4,5-disubstituted 2-aminoimidazole triazole amide (2-AITA) conjugates has been successfully assembled. Upon biological screening, this class of small molecules was discovered as enhanced biofilm regulators through non-microbicidal mechanisms against methicillin-resistant Staphylococcus aureus (MRSA) and multidrug-resistant Acinetobacter baumannii (MDRAB), with active concentrations in the low micromolar range. The library was also subjected to synergism and resensitization studies with β-lactam antibiotics against MRSA. Lead compounds were identified that suppress the antibiotic resistance of MRSA by working synergistically with oxacillin, a β-lactam antibiotic resistant to penicillinase. A further structure-activity relationship (SAR) study on the parent 2-AITA compound delivered a 2-aminoimidazole diamide (2-AIDA) conjugate with significantly increased synergistic activity with oxacillin against MRSA, decreasing the MIC value of the β-lactam antibiotic by 64-fold. Increased anti-biofilm activity did not necessarily lead to increased suppression of antibiotic resistance, which indicates that biofilm inhibition and resensitization are most likely occurring via distinct mechanisms.
Process for the preparation of aryl-piridyl compounds
-
Page/Page column 3, (2008/06/13)
A method is described for the preparation of aryl-pyridine compounds of formula (I) by cross-coupling reaction, promoted by catalytic systems based on palladium or nickel between compounds of formula (II) and (III) in which:—Met represents Mg or Zn,—Y represents Cl, Br, I or acetoxy,—Z represents I, Br, Cl, triflate, sulphonate, phosphate,—R1, R2, R3, R4, which are the same as one another or different, represent hydrogen, a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or R1 and R2 and/or R3 and R4, taken together, form a C3-C8 ring, an aryl and/or a heteroaryl,—A represents —COR5 where R5 represents hydrogen, a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or—A represents —CRs5(OR6)(OR7) where R5 has the meaning described above and R6 and R7, which are the same as one another or different, represent a linear and/or branched C1-C4 alkyl, and/or an aryl, and/or a heteroaryl, or R6 and R7, joined together, represent a C1-C8 alkyl or alkenyl.