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dc.contributor.authorMoraski, Garrett C.
dc.contributor.authorMiller, Patricia
dc.contributor.authorBailey, Mai Ann
dc.contributor.authorOllinger, Juliane
dc.contributor.authorParish, Tanya
dc.contributor.authorBoshoff, Helena I.
dc.contributor.authorCho, Sanghyun
dc.contributor.authorAnderson, Jeffery
dc.contributor.authorMulugeta, Surafel
dc.contributor.authorFranzblau, Scott G.
dc.contributor.authorMiller, Marvin J.
dc.identifier.citationMoraski, Garrett C., Patricia A. Miller, Mai Ann Bailey, Juliane Ollinger, Tanya Parish, Helena I. Boshoff, Sanghyun Cho, Jeffery R. Anderson, Surafel Mulugeta, Scott G. Franzblau, and Marvin J. Miller. Putting Tuberculosis (TB) To Rest: Transformation of the Sleep Aid, Ambien, and "Anagrams" Generated Potent Antituberculosis Agents. ACS Infectious Diseases. December 2014.
dc.description.abstractZolpidem (Ambien, 1) is an imidazo[1,2-a]pyridine-3-acetamide and an approved drug for the treatment of insomnia. As medicinal chemists enamored by how structure imparts biological function, we found it to have strikingly similar structure to the antitubercular imidazo[1,2-a]pyridine-3-carboxyamides. Zolpidem was found to have antituberculosis activity (MIC of 10–50 μM) when screened against replicating Mycobacterium tuberculosis (Mtb) H37Rv. Manipulation of the Zolpidem structure, notably, to structural isomers (“anagrams”), attains remarkably improved potency (5, MIC of 0.004 μM) and impressive potency against clinically relevant drug-sensitive, multi- and extensively drug-resistant Mtb strains (MIC < 0.03 μM). Zolpidem anagrams and analogues were synthesized and evaluated for their antitubercular potency, toxicity, and spectrum of activity against nontubercular mycobacteria and Gram-positive and Gram-negative bacteria. These efforts toward the rational design of isomeric anagrams of a well-known sleep aid underscore the possibility that further optimization of the imidazo[1,2-a]pyridine core may well “put TB to rest”.en_US
dc.titlePutting Tuberculosis (TB) To Rest: Transformation of the Sleep Aid, Ambien, and “Anagrams” Generated Potent Antituberculosis Agentsen_US
mus.citation.journaltitleACS Infectious Diseasesen_US
mus.identifier.categoryChemical & Material Sciencesen_US
mus.relation.collegeCollege of Letters & Scienceen_US
mus.relation.departmentChemistry & Biochemistry.en_US
mus.relation.universityMontana State University - Bozemanen_US
mus.contributor.orcidMoraski, Garrett C.|0000-0002-6992-5584en_US

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