Year |
Citation |
Score |
2023 |
Carter HE, Wildman B, Schwanz HA, Kerns RJ, Aldred KJ. Role of the Water-Metal Ion Bridge in Quinolone Interactions with Gyrase. International Journal of Molecular Sciences. 24. PMID 36769202 DOI: 10.3390/ijms24032879 |
0.754 |
|
2020 |
Aguirre AL, Chheda PR, Lentz SRC, Held HA, Groves NP, Hiasa H, Kerns RJ. Identification of an ethyl 5,6-dihydropyrazolo[1,5-c]quinazoline-1-carboxylate as a catalytic inhibitor of DNA gyrase. Bioorganic & Medicinal Chemistry. 115439. PMID 32234278 DOI: 10.1016/J.Bmc.2020.115439 |
0.398 |
|
2019 |
Delgado JL, Lentz SRC, Kulkarni CA, Chheda PR, Held HA, Hiasa H, Kerns RJ. Probing structural requirements for human topoisomerase I inhibition by a novel N1-Biphenyl fluoroquinolone. European Journal of Medicinal Chemistry. 172: 109-130. PMID 30959322 DOI: 10.1016/J.Ejmech.2019.03.040 |
0.421 |
|
2019 |
Lentz SRC, Chheda PR, Oppegard LM, Towle TR, Kerns RJ, Hiasa H. The C7-aminomethylpyrrolidine group rescues the activity of a thio-fluoroquinolone. Biochimie. 160: 24-27. PMID 30763638 DOI: 10.1016/J.Biochi.2019.02.002 |
0.42 |
|
2018 |
Oppegard LM, Delgado JL, Kulkarni CA, Towle TR, Hart DE, Williams BP, Lentz SRC, Norris BJ, Flory CM, Schumacher RJ, Murry DJ, Kerns RJ, Hiasa H. Novel N-1 substituted fluoroquinolones inhibit human topoisomerase I activity and exhibit anti-proliferative activity. Investigational New Drugs. PMID 30198058 DOI: 10.1007/S10637-018-0666-X |
0.362 |
|
2018 |
Towle TR, Kulkarni CA, Oppegard LM, Williams BP, Picha TA, Hiasa H, Kerns RJ. Design, synthesis, and evaluation of novel N-1 fluoroquinolone derivatives: Probing for binding contact with the active site tyrosine of gyrase. Bioorganic & Medicinal Chemistry Letters. PMID 29661533 DOI: 10.1016/J.Bmcl.2018.03.085 |
0.386 |
|
2017 |
Ashley RE, Lindsey RH, McPherson SA, Turnbough CL, Kerns RJ, Osheroff N. Interactions between quinolones and Bacillus anthracis gyrase and the basis of drug resistance. Biochemistry. PMID 28708938 DOI: 10.1021/Acs.Biochem.7B00203 |
0.407 |
|
2016 |
Malik M, Mustaev A, Schwanz HA, Luan G, Shah N, Oppegard LM, de Souza EC, Hiasa H, Zhao X, Kerns RJ, Drlica K. Suppression of gyrase-mediated resistance by C7 aryl fluoroquinolones. Nucleic Acids Research. PMID 26984528 DOI: 10.1093/Nar/Gkw161 |
0.788 |
|
2016 |
Craciun I, Fenner AM, Kerns RJ. N-Arylacyl O-sulfonated aminoglycosides as novel inhibitors of human neutrophil elastase, cathepsin G and proteinase 3. Glycobiology. PMID 26850997 DOI: 10.1093/Glycob/Cww011 |
0.747 |
|
2016 |
Blower TR, Williamson BH, Kerns RJ, Berger JM. Crystal structure and stability of gyrase-fluoroquinolone cleaved complexes from Mycobacterium tuberculosis. Proceedings of the National Academy of Sciences of the United States of America. PMID 26792525 DOI: 10.1073/Pnas.1525047113 |
0.388 |
|
2016 |
Aldred KJ, Blower TR, Kerns RJ, Berger JM, Osheroff N. Fluoroquinolone interactions with Mycobacterium tuberculosis gyrase: Enhancing drug activity against wild-type and resistant gyrase. Proceedings of the National Academy of Sciences of the United States of America. PMID 26792518 DOI: 10.1073/Pnas.1525055113 |
0.364 |
|
2016 |
Oppegard LM, Schwanz HA, Towle TR, Kerns RJ, Hiasa H. Fluoroquinolones stimulate the DNA cleavage activity of topoisomerase IV by promoting the binding of Mg(2+) to the second metal binding site. Biochimica Et Biophysica Acta. 1860: 569-75. PMID 26723176 DOI: 10.1016/J.Bbagen.2015.12.019 |
0.762 |
|
2015 |
Aldred KJ, Schwanz HA, Li G, Williamson BH, McPherson SA, Turnbough CL, Kerns RJ, Osheroff N. Activity of quinolone CP-115,955 against bacterial and human type II topoisomerases is mediated by different interactions. Biochemistry. 54: 1278-86. PMID 25586498 DOI: 10.1021/Bi501073V |
0.783 |
|
2014 |
Drlica K, Mustaev A, Towle TR, Luan G, Kerns RJ, Berger JM. Bypassing fluoroquinolone resistance with quinazolinediones: studies of drug-gyrase-DNA complexes having implications for drug design. Acs Chemical Biology. 9: 2895-904. PMID 25310082 DOI: 10.1021/Cb500629K |
0.415 |
|
2014 |
Aldred KJ, Breland EJ, McPherson SA, Turnbough CL, Kerns RJ, Osheroff N. Bacillus anthracis GrlAV96A topoisomerase IV, a quinolone resistance mutation that does not affect the water-metal ion bridge. Antimicrobial Agents and Chemotherapy. 58: 7182-7. PMID 25246407 DOI: 10.1128/Aac.03734-14 |
0.35 |
|
2014 |
Aldred KJ, Breland EJ, VlÄková V, Strub MP, Neuman KC, Kerns RJ, Osheroff N. Role of the water-metal ion bridge in mediating interactions between quinolones and Escherichia coli topoisomerase IV. Biochemistry. 53: 5558-67. PMID 25115926 DOI: 10.1021/Bi500682E |
0.378 |
|
2014 |
Malik M, Li L, Zhao X, Kerns RJ, Berger JM, Drlica K. Lethal synergy involving bicyclomycin: an approach for reviving old antibiotics. The Journal of Antimicrobial Chemotherapy. 69: 3227-35. PMID 25085655 DOI: 10.1093/Jac/Dku285 |
0.328 |
|
2014 |
Aldred KJ, Kerns RJ, Osheroff N. Mechanism of quinolone action and resistance. Biochemistry. 53: 1565-74. PMID 24576155 DOI: 10.1021/Bi5000564 |
0.373 |
|
2014 |
Mustaev A, Malik M, Zhao X, Kurepina N, Luan G, Oppegard LM, Hiasa H, Marks KR, Kerns RJ, Berger JM, Drlica K. Fluoroquinolone-gyrase-DNA complexes: two modes of drug binding. The Journal of Biological Chemistry. 289: 12300-12. PMID 24497635 DOI: 10.1074/Jbc.M113.529164 |
0.351 |
|
2013 |
Aldred KJ, Schwanz HA, Li G, McPherson SA, Turnbough CL, Kerns RJ, Osheroff N. Overcoming target-mediated quinolone resistance in topoisomerase IV by introducing metal-ion-independent drug-enzyme interactions. Acs Chemical Biology. 8: 2660-8. PMID 24047414 DOI: 10.1021/Cb400592N |
0.78 |
|
2013 |
Fenner AM, Oppegard LM, Hiasa H, Kerns RJ. Selective inhibition of bacterial and human topoisomerases by N-arylacyl O-sulfonated aminoglycoside derivatives. Acs Medicinal Chemistry Letters. 4: 470-474. PMID 23814643 DOI: 10.1021/Ml3004507 |
0.779 |
|
2013 |
Aldred KJ, McPherson SA, Turnbough CL, Kerns RJ, Osheroff N. Topoisomerase IV-quinolone interactions are mediated through a water-metal ion bridge: mechanistic basis of quinolone resistance. Nucleic Acids Research. 41: 4628-39. PMID 23460203 DOI: 10.1093/Nar/Gkt124 |
0.35 |
|
2013 |
Towle T, Chang I, Chang I, Kerns RJ, Bhanot P. Chemical probes of a trisubstituted pyrrole to identify its protein target(s) in Plasmodium sporozoites. Bioorganic & Medicinal Chemistry Letters. 23: 1874-7. PMID 23395653 DOI: 10.1016/J.Bmcl.2013.01.010 |
0.317 |
|
2012 |
Fink BD, Herlein JA, Yorek MA, Fenner AM, Kerns RJ, Sivitz WI. Bioenergetic effects of mitochondrial-targeted coenzyme Q analogs in endothelial cells. The Journal of Pharmacology and Experimental Therapeutics. 342: 709-19. PMID 22661629 DOI: 10.1124/Jpet.112.195586 |
0.744 |
|
2012 |
Malik M, Chavda K, Zhao X, Shah N, Hussain S, Kurepina N, Kreiswirth BN, Kerns RJ, Drlica K. Induction of mycobacterial resistance to quinolone class antimicrobials. Antimicrobial Agents and Chemotherapy. 56: 3879-87. PMID 22564842 DOI: 10.1128/Aac.00474-12 |
0.331 |
|
2012 |
Aldred KJ, McPherson SA, Wang P, Kerns RJ, Graves DE, Turnbough CL, Osheroff N. Drug interactions with Bacillus anthracis topoisomerase IV: biochemical basis for quinolone action and resistance. Biochemistry. 51: 370-81. PMID 22126453 DOI: 10.1021/Bi2013905 |
0.387 |
|
2011 |
Fenner AM, Kerns RJ. Synthesis, separation, and characterization of amphiphilic sulfated oligosaccharides enabled by reversed-phase ion pairing LC and LC-MS methods. Carbohydrate Research. 346: 2792-800. PMID 22015170 DOI: 10.1016/J.Carres.2011.09.020 |
0.757 |
|
2011 |
Marks KR, Malik M, Mustaev A, Hiasa H, Drlica K, Kerns RJ. Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones. Bioorganic & Medicinal Chemistry Letters. 21: 4585-8. PMID 21705218 DOI: 10.1016/J.Bmcl.2011.05.112 |
0.393 |
|
2011 |
Malik M, Marks KR, Mustaev A, Zhao X, Chavda K, Kerns RJ, Drlica K. Fluoroquinolone and quinazolinedione activities against wild-type and gyrase mutant strains of Mycobacterium smegmatis. Antimicrobial Agents and Chemotherapy. 55: 2335-43. PMID 21383100 DOI: 10.1128/Aac.00033-11 |
0.422 |
|
2010 |
Malik M, Marks KR, Schwanz HA, German N, Drlica K, Kerns RJ. Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality. Antimicrobial Agents and Chemotherapy. 54: 5214-21. PMID 20855738 DOI: 10.1128/Aac.01054-10 |
0.768 |
|
2010 |
Oppegard LM, Streck KR, Rosen JD, Schwanz HA, Drlica K, Kerns RJ, Hiasa H. Comparison of in vitro activities of fluoroquinolone-like 2,4- and 1,3-diones. Antimicrobial Agents and Chemotherapy. 54: 3011-4. PMID 20404126 DOI: 10.1128/Aac.00190-10 |
0.773 |
|
2010 |
Malik M, Hoatam G, Chavda K, Kerns RJ, Drlica K. Novel approach for comparing the abilities of quinolones to restrict the emergence of resistant mutants during quinolone exposure. Antimicrobial Agents and Chemotherapy. 54: 149-56. PMID 19805561 DOI: 10.1128/Aac.01035-09 |
0.38 |
|
2010 |
LINHARDT RJ, KERNS RJ, VLAHOV IR. ChemInform Abstract: Heparin and Heparin Oligosaccharides: Preparation, Analysis, Applications and Biological Activities Cheminform. 28: no-no. DOI: 10.1002/chin.199702249 |
0.668 |
|
2010 |
KERNS RJ, TOIDA T, LINHARDT RJ. ChemInform Abstract: Synthesis of the Bis-tetrahydropyrano(2,3-b:2′,3′-e)piperazine Ring System: A New Tricyclic Heterocycle from D-Glucosamine. Cheminform. 27: no-no. DOI: 10.1002/chin.199646234 |
0.324 |
|
2010 |
KERNS RJ, LINHARDT RJ. ChemInform Abstract: Selective N-Sulfation of Glucosamine Derivatives Using Phenyl Chlorosulfate in Non-Aqueous Solvent. Cheminform. 27: no-no. DOI: 10.1002/chin.199642223 |
0.349 |
|
2009 |
Rosen JD, German N, Kerns RJ. Efficient Synthesis of the 2-amino-6-chloro-4-cyclopropyl-7-fluoro-5-methoxy-pyrido[1,2-c]pyrimidine-1,3-dione core ring system. Tetrahedron Letters. 50: 785-789. PMID 20160840 DOI: 10.1016/J.Tetlet.2008.11.121 |
0.695 |
|
2009 |
Drlica K, Hiasa H, Kerns R, Malik M, Mustaev A, Zhao X. Quinolones: action and resistance updated. Current Topics in Medicinal Chemistry. 9: 981-98. PMID 19747119 DOI: 10.2174/156802609789630947 |
0.345 |
|
2008 |
German N, Malik M, Rosen JD, Drlica K, Kerns RJ. Use of gyrase resistance mutants to guide selection of 8-methoxy-quinazoline-2,4-diones. Antimicrobial Agents and Chemotherapy. 52: 3915-21. PMID 18765690 DOI: 10.1128/Aac.00330-08 |
0.683 |
|
2008 |
German N, Wei P, Kaatz GW, Kerns RJ. Synthesis and evaluation of fluoroquinolone derivatives as substrate-based inhibitors of bacterial efflux pumps. European Journal of Medicinal Chemistry. 43: 2453-63. PMID 18358571 DOI: 10.1016/J.Ejmech.2008.01.042 |
0.676 |
|
2008 |
German N, Kaatz GW, Kerns RJ. Synthesis and evaluation of PSSRI-based inhibitors of Staphylococcus aureus multidrug efflux pumps. Bioorganic & Medicinal Chemistry Letters. 18: 1368-73. PMID 18242086 DOI: 10.1016/J.Bmcl.2008.01.014 |
0.692 |
|
2008 |
Drlica K, Malik M, Kerns RJ, Zhao X. Quinolone-mediated bacterial death. Antimicrobial Agents and Chemotherapy. 52: 385-92. PMID 17724149 DOI: 10.1128/Aac.01617-06 |
0.37 |
|
2008 |
Kerns RJ, Fenner AM. Book Review of The Synthetic Organic Chemist’s Companion The Synthetic Organic Chemistʼs Companion.By Michael C. Pirrung . Wiley-Interscience , Hoboken, NJ . 2007 . xiii + 198 pp. ISBN 9780470107072 (Paperback). $50.00. Journal of Medicinal Chemistry. 51: 1073-1073. DOI: 10.1021/Jm701180D |
0.742 |
|
2007 |
Hattan CM, Kerns RJ. Variability in the carbazole assay for N-desulfonated/N-acylated heparin derivatives. Carbohydrate Research. 342: 2664-9. PMID 17850773 DOI: 10.1016/J.Carres.2007.08.004 |
0.75 |
|
2007 |
Huang L, Fernández C, Kerns RJ. Different protein-binding selectivities for N-acyl heparin derivatives having N-phenylacetyl and heterocycle analogs of N-phenylacetyl substituted in place of N-sulfo groups. Bioorganic & Medicinal Chemistry Letters. 17: 419-23. PMID 17070049 DOI: 10.1016/J.Bmcl.2006.10.026 |
0.351 |
|
2006 |
Zhao X, Quinn B, Kerns R, Drlica K. Bactericidal activity and target preference of a piperazinyl-cross-linked ciprofloxacin dimer with Staphylococcus aureus and Escherichia coli. The Journal of Antimicrobial Chemotherapy. 58: 1283-6. PMID 17003060 DOI: 10.1093/Jac/Dkl388 |
0.338 |
|
2006 |
Fernández C, Hattan CM, Kerns RJ. Semi-synthetic heparin derivatives: chemical modifications of heparin beyond chain length, sulfate substitution pattern and N-sulfo/N-acetyl groups. Carbohydrate Research. 341: 1253-65. PMID 16712822 DOI: 10.1016/J.Carres.2006.04.014 |
0.765 |
|
2006 |
Huang L, Kerns RJ. Diversity-oriented chemical modification of heparin: Identification of charge-reduced N-acyl heparin derivatives having increased selectivity for heparin-binding proteins. Bioorganic & Medicinal Chemistry. 14: 2300-13. PMID 16314105 DOI: 10.1016/J.Bmc.2005.11.013 |
0.361 |
|
2005 |
Wei P, Kerns RJ. Factors affecting stereocontrol during glycosidation of 2,3-oxazolidinone-protected 1-tolylthio-N-acetyl-D-glucosamine. The Journal of Organic Chemistry. 70: 4195-8. PMID 15876119 DOI: 10.1021/Jo047812O |
0.317 |
|
2005 |
Malik M, Lu T, Zhao X, Singh A, Hattan CM, Domagala J, Kerns R, Drlica K. Lethality of quinolones against Mycobacterium smegmatis in the presence or absence of chloramphenicol. Antimicrobial Agents and Chemotherapy. 49: 2008-14. PMID 15855526 DOI: 10.1128/Aac.49.5.2008-2014.2005 |
0.774 |
|
2005 |
Wei P, Kerns RJ. Chemoselective deprotection and functional group interconversion of ring-fused 2N,3O-oxazolidinones of N-acetyl-D-glucosamine Tetrahedron Letters. 46: 6901-6905. DOI: 10.1016/J.Tetlet.2005.08.013 |
0.317 |
|
2004 |
Gould KA, Pan XS, Kerns RJ, Fisher LM. Ciprofloxacin dimers target gyrase in Streptococcus pneumoniae Antimicrobial Agents and Chemotherapy. 48: 2108-2115. PMID 15155208 DOI: 10.1128/Aac.48.6.2108-2115.2004 |
0.406 |
|
2004 |
Wei P, Kaatz GW, Kerns RJ. Structural differences between paroxetine and femoxetine responsible for differential inhibition of Staphylococcus aureus efflux pumps. Bioorganic & Medicinal Chemistry Letters. 14: 3093-7. PMID 15149651 DOI: 10.1016/J.Bmcl.2004.04.018 |
0.316 |
|
2003 |
Kerns RJ, Rybak MJ, Kaatz GW, Vaka F, Cha R, Grucz RG, Diwadkar VU. Structural features of piperazinyl-linked ciprofloxacin dimers required for activity against drug-resistant strains of Staphylococcus aureus. Bioorganic & Medicinal Chemistry Letters. 13: 2109-12. PMID 12798315 DOI: 10.1016/S0960-894X(03)00376-7 |
0.363 |
|
2003 |
Kerns RJ, Rybak MJ, Kaatz GW, Vaka F, Cha R, Grucz RG, Diwadkar VU, Ward TD. Piperazinyl-linked fluoroquinolone dimers possessing potent antibacterial activity against drug-resistant strains of Staphylococcus aureus. Bioorganic & Medicinal Chemistry Letters. 13: 1745-9. PMID 12729656 DOI: 10.1016/S0960-894X(03)00208-7 |
0.35 |
|
2003 |
Kerns RJ, Zha C, Benakli K, Liang YZ. Extended applications and potential limitations of ring-fused 2,3-oxazolidinone thioglycosides in glycoconjugate synthesis Tetrahedron Letters. 44: 8069-8072. DOI: 10.1016/J.Tetlet.2003.09.058 |
0.317 |
|
2001 |
Kim YS, Thanawiroon C, Bazin HG, Kerns RJ, Linhard RJ. Enzymatic preparation of heparin disaccharides as building blocks in glycosaminoglycan synthesis. Preparative Biochemistry & Biotechnology. 31: 113-24. PMID 11426699 DOI: 10.1081/Pb-100103377 |
0.753 |
|
1997 |
Bazin HG, Kerns RJ, Linhardt RJ. Regio and stereoselective conversion of Δ4-uronic acids to L-ido- and D-glucopyranosiduronic acids Tetrahedron Letters. 38: 923-926. DOI: 10.1016/S0040-4039(96)02514-2 |
0.394 |
|
1996 |
Kerns RJ, Toida T, Linhardt RJ. Synthesis of the Bis-Tetrahydropyrano[2,3-b:2′,3′-e] Piperazine Ring System: A New Tricyclic Heterocycle from D-Glucosamine Journal of Carbohydrate Chemistry. 15: 581-590. DOI: 10.1080/07328309608005676 |
0.434 |
|
1996 |
Kerns RJ, Linhardt RJ. SelectiveN-Sulfation of Glucosamine Derivatives using Phenyl Chlorosulfate in Non-Aqueous Solvent Synthetic Communications. 26: 2671-2680. DOI: 10.1080/00397919608004583 |
0.442 |
|
1995 |
Kerns RJ, Vlahov IR, Linhardt RJ. Capillary electrophoresis for monitoring chemical reactions: sulfation and synthetic manipulation of sulfated carbohydrates Carbohydrate Research. 267: 143-152. PMID 7697664 DOI: 10.1016/0008-6215(94)00288-Q |
0.667 |
|
1995 |
Kerns RJ, Linhardt RJ. Separation of hydroxyl protected heparin derived disaccharides using reversed-phase high-performance liquid chromatography Journal of Chromatography A. 705: 369-373. PMID 7640772 DOI: 10.1016/0021-9673(95)00293-V |
0.441 |
|
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