- INHIBITORS OF BACTERIAL GLYCOSYL TRANSFERASES
-
Described herein are compounds of Formula (I'), Formula (IA), Formulae (I)-(VII), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrug sthereof. The invention also provides pharmaceutical compositions of the compounds for human and veterinary use. Compounds of the present invention are useful for inhibiting bacterial growth and therefore are useful in treating and/or preventing bacterial infections. Methods of using the compounds for treating and/or preventing a bacterial infection in a subject are also described.
- -
-
Paragraph 00370; 00429
(2016/12/22)
-
- Synthesis and antiplatelet activity of new imidazole-4-carboxylic acid derivatives
-
1-Arylalkyl-5-phenylsulfonamino-imidazole-4-carboxylic acid esters and their carboxamides with an additional secondary amino group were synthesized and identified as antiplatelet agents in a low micromolar range (Born-test, inducer collagen). To describe the mechanism of action more precisely the Born-test was carried out as well with ADP, adrenaline or PAF, respectively. In addition, two compounds were investigated for their COX-1 inhibitory activities. Provided the essential structural criteria are met i.e. amide group or ester, sulfonylamino rest, hydrophobic moieties, and a secondary amino function, slight structural modifications are able to shift the pattern of activity among the above platelet receptors. So, the ester 5c exhibits PAF antagonistic activity at IC 50 = 1 μM and COX-1 inhibition (IC50 = 0.4 μM). The carboxamide 6c shows ADP antagonistic properties (IC50 = 2 μM). Compound 6g is as well PAF antagonistic (IC50 = 4 μM) and a COX-1 inhibitor (IC50 = 1 μM). The derivative 6i shows a strong antiadrenergic (IC50 = 0.15 μM) and PAF antagonistic (IC 50 = 0.66 μM) effect.
- Rehse, Klaus,Steege, Jens
-
p. 539 - 547
(2007/10/03)
-
- Poly-bis-triazinylimides, their preparation
-
Poly-bis-triazinylimides of the formula STR1 are prepared from bis-(2,4-dichloro-1,3,5-triazin-6-yl)imides and polyalkylpiperidylamines. They are used as light stabilizers for polymers.
- -
-
-