Imidazolines structure-activity relationship

This procedure was utilized by the same authors to synthesize a large library of 4-carbohydroxamido-2-(aryl or alkyl)-2-imidazolines, some of which exhibited excellent LpxC inhibitory and antibacterial activities. The technical maneuvers in the syntheses of these compounds and their structure-activity relationships are comprehensively covered by the authors in their paper. 

The workers at American Cyanamid present some of the synthetic and biological characteristics of the sulfur analogs of their imidazoline family of herbicides. This is an example of replacing the carbonyl of the imidazoli-none with an isosteric moiety. This is an interesting account of the synthesis and structure-activity relationships in a very active series of herbicides. 

Thus, initially, an extensive structure-activity relationship study was performed the data of this study suggested the existence of a new class of receptors specific for imidazoline-like compoimds different from the classical a-adrenergic receptors [1]. 

Timmermans, P. B. M. W. M., Hoefke, W., Stahle, H., van Zwieten, P. A., Structure activity relationships in clonidine-like imidazolines and related compounds, Progr. Pharmacol. 3 1-104,1980. 

We have taken advantage of the ease of generating Ru-NHC complexes in situ to help define structure-activity relationships for imidazolin-2-ylidene and imidazolidin-2-ylidene derivatives used as ancillary ligands in metathesis catalysts. For this purpose, a wide range of new imidazolium and imidazoli-nium chlorides bearing aromatic substituents was synthesized. These ionic precursors were deprotonated with potassium tert-butoxide or sodium hydride and combined wMi [RuCl2(p-cymene)]2 in chlorobenzene at 60°C. Cyclooctene was then added and its polymerization was allowed to proceed for 2 h under visible light illumination (Eq. 3)." ... 

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