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Agents Chemother."},{"key":"ref18\/cit18","doi-asserted-by":"crossref","first-page":"555","DOI":"10.1016\/j.ijantimicag.2007.07.021","volume":"30","author":"Huang T. L.","year":"2007","journal-title":"Int. J. Antimicrob. Agents"},{"key":"ref19\/cit19","doi-asserted-by":"crossref","first-page":"4761","DOI":"10.1021\/jm0302602","volume":"46","author":"Ismail M. A.","year":"2003","journal-title":"J. Med. Chem."},{"key":"ref20\/cit20","doi-asserted-by":"crossref","first-page":"4185","DOI":"10.1128\/AAC.00225-09","volume":"53","author":"Wenzler T.","year":"2009","journal-title":"Antimicrob. Agents Chemother."},{"key":"ref21\/cit21","doi-asserted-by":"crossref","first-page":"3139","DOI":"10.1021\/jm9509298","volume":"39","author":"Weller T.","year":"1996","journal-title":"J. Med. Chem."},{"key":"ref22\/cit22","doi-asserted-by":"crossref","first-page":"5233","DOI":"10.1016\/j.bmcl.2009.07.001","volume":"19","author":"Degardin M.","year":"2009","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"ref23\/cit23","doi-asserted-by":"crossref","first-page":"6730","DOI":"10.1021\/jm701259d","volume":"50","author":"Reeh C.","year":"2007","journal-title":"J. Med. Chem."},{"key":"ref24\/cit24","doi-asserted-by":"crossref","first-page":"1595","DOI":"10.1002\/cmdc.200900233","volume":"4","author":"Dennis S.","year":"2009","journal-title":"ChemMedChem"},{"key":"ref25\/cit25","doi-asserted-by":"crossref","first-page":"1260","DOI":"10.1002\/cmdc.200600079","volume":"1","author":"Clement B.","year":"2006","journal-title":"ChemMedChem"},{"key":"ref26\/cit26","first-page":"384","volume-title":"Comprehensive Heterocyclic Chemistry","volume":"5","author":"Grimmett M. R.","year":"1984"},{"key":"ref27\/cit27","first-page":"252","volume-title":"Comprehensive Heterocyclic Chemistry","volume":"6","author":"Metzger J. 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Soc., Perkin Trans. 2"},{"key":"ref33\/cit33","unstructured":"Ramuz, H.2-Imino-imidazolidine derivatives. U.S. Patent 4,244,957, 1978."},{"key":"ref34\/cit34","doi-asserted-by":"crossref","first-page":"3155","DOI":"10.1016\/S0960-894X(03)00713-3","volume":"13","author":"Alanine A.","year":"2003","journal-title":"Bioorg. Med. Chem. Lett."},{"key":"ref35\/cit35","doi-asserted-by":"crossref","DOI":"10.1002\/0471220574","volume-title":"Protective Groups in Organic Synthesis","author":"Greene T. W.","year":"1999","edition":"3"},{"key":"ref36\/cit36","doi-asserted-by":"crossref","first-page":"4571","DOI":"10.1016\/j.tetlet.2008.05.098","volume":"49","author":"Mascaraque A.","year":"2008","journal-title":"Tetrahedron Lett."},{"key":"ref37\/cit37","doi-asserted-by":"crossref","first-page":"3815","DOI":"10.1128\/AAC.00124-09","volume":"53","author":"Dardonville C.","year":"2009","journal-title":"Antimicrob. Agents Chemother."},{"key":"ref38\/cit38","doi-asserted-by":"crossref","first-page":"165","DOI":"10.1016\/S0169-409X(98)00083-0","volume":"36","author":"Cecchelli R.","year":"1999","journal-title":"Adv. Drug Delivery Rev."},{"key":"ref39\/cit39","doi-asserted-by":"crossref","first-page":"111","DOI":"10.1002\/jcp.1041320115","volume":"132","author":"Siflinger-Birnboim A.","year":"1987","journal-title":"J. Cell. Physiol."},{"key":"ref40\/cit40","doi-asserted-by":"crossref","first-page":"59","DOI":"10.1007\/s10571-004-1377-8","volume":"25","author":"Deli M.","year":"2005","journal-title":"Cell. Mol. Neurobiol."},{"key":"ref41\/cit41","doi-asserted-by":"crossref","first-page":"666","DOI":"10.1128\/AAC.42.3.666","volume":"42","author":"Hall J. E.","year":"1998","journal-title":"Antimicrob. Agents Chemother."},{"key":"ref42\/cit42","doi-asserted-by":"crossref","first-page":"150","DOI":"10.1016\/S1093-3263(99)00006-6","volume":"16","author":"Dardonville C.","year":"1998","journal-title":"J. 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