@article{brackett_furlani_anderson_krishnamurthy_melander_moskowitz_ernst_melander_2016, title={Second generation modifiers of colistin resistance show enhanced activity and lower inherent toxicity}, volume={72}, ISSN={["0040-4020"]}, DOI={10.1016/j.tet.2015.09.019}, abstractNote={We recently reported a 2-aminoimidazole-based antibiotic adjuvant that reverses colistin resistance in two species of Gram-negative bacteria. Mechanistic studies in Acinetobacter baumannii demonstrated that this compound downregulated the PmrAB two-component system and abolished a lipid A modification that is required for colistin resistance. We now report the synthesis and evaluation of two separate libraries of substituted 2-aminoimidazole analogues based on this parent compound. From these libraries, a new small molecule was identified that lowers the minimum inhibitory concentration of colistin by up to 32-fold greater than the parent compound while also displaying less inherent bacterial effect, thereby minimizing the likelihood of resistance evolution.}, number={25}, journal={TETRAHEDRON}, author={Brackett, Christopher M. and Furlani, Robert E. and Anderson, Ryan G. and Krishnamurthy, Aparna and Melander, Roberta J. and Moskowitz, Samuel M. and Ernst, Robert K. and Melander, Christian}, year={2016}, month={Jun}, pages={3549–3553} }
 @article{richardson_furlani_podell_ackart_haugen_melander_melander_basaraba_2015, title={Inhibition and breaking of advanced glycation end-products (AGEs) with bis-2-aminoimidazole derivatives}, volume={56}, ISSN={["0040-4039"]}, DOI={10.1016/j.tetlet.2015.01.122}, abstractNote={Advanced glycation end-products (AGEs), unregulated modifications to host macromolecules that occur as a result of metabolic dysregulation, play a role in many diabetes related complications, inflammation and aging, and may lead to increased cardiovascular risk. Small molecules that have the ability to inhibit AGE formation, and even break preformed AGEs have enormous therapeutic potential in the treatment of these disease states. We report the screening of a series of 2-aminoimidazloles for anti-AGE activity, and the identification of a bis-2-aminoimidazole lead compound that possesses superior AGE inhibition and breaking activity compared to the known AGE inhibitor aminoguanidine.}, number={23}, journal={TETRAHEDRON LETTERS}, author={Richardson, Mike A. and Furlani, Robert E. and Podell, Brendan K. and Ackart, David F. and Haugen, Jessica D. and Melander, Roberta J. and Melander, Christian and Basaraba, Randall J.}, year={2015}, month={Jun}, pages={3406–3409} }
 @article{furlani_richardson_podell_ackart_haugen_melander_basaraba_melander_2015, title={Second generation 2-aminoimidazole based advanced glycation end product inhibitors and breakers}, volume={25}, ISSN={["1464-3405"]}, DOI={10.1016/j.bmcl.2015.06.080}, abstractNote={The formation of advanced glycation end-products (AGE) as a result of the action of reducing sugars on host macromolecules plays a role in increased morbidity of diabetic patients. There are currently no clinically available therapeutics for the prevention or eradication of AGEs. Following our previous identification of 2-aminoimidazole (2-AI) based AGE inhibitors and breakers, we now report the use of a rapid, scalable, two-step procedure to access a second generation of 2-AI based anti-AGE compounds from commercially available amino acids. Several second generation compounds exhibit increased AGE inhibition and breaking activty compared to the first generation compounds and to the known AGE inhibitor aminoguanidine.}, number={21}, journal={BIOORGANIC & MEDICINAL CHEMISTRY LETTERS}, author={Furlani, Robert E. and Richardson, Mike A. and Podell, Brendan K. and Ackart, David F. and Haugen, Jessica D. and Melander, Roberta J. and Basaraba, Randall J. and Melander, Christian}, year={2015}, month={Nov}, pages={4820–4823} }
 @article{furlani_yeagley_melander_2013, title={A flexible approach to 1,4-di-substituted 2-aminoimidazoles that inhibit and disperse biofilms and potentiate the effects of beta-lactams against multi-drug resistant bacteria}, volume={62}, ISSN={["1768-3254"]}, DOI={10.1016/j.ejmech.2012.12.005}, abstractNote={The pyrrole-imidazole alkaloids are a 2-aminoimidazoles containing family of natural products that possess anti-biofilm activity. A library of 1,4-di-substituted 2-aminoimidazole/triazoles (2-AITs) was synthesized, and its anti-biofilm activity as well as oxacillin resensitization efficacy toward methicillin resistant Staphylococcus aureus (MRSA) was investigated. These 2-AITs were found to inhibit biofilm formation by MRSA with low micromolar IC50 values. Additionally, the most active compound acted synergistically with oxacillin against MRSA lowering the minimum inhibitory concentration (MIC) 4-fold.}, journal={EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY}, author={Furlani, Robert E. and Yeagley, Andrew A. and Melander, Christian}, year={2013}, month={Apr}, pages={59–70} }