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Page 1
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.
Stavenger RA, Cui H, Dowdell SE, Franz RG, Gaitanopoulos DE, Goodman KB, Hilfiker MA, Ivy RL, Leber JD, Marino JP Jr, Oh HJ, Viet AQ, Xu W, Ye G, Zhang D, Zhao Y, Jolivette LJ, Head MS, Semus SF, Elkins PA, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Doe CP, Bentley R, Chen ZX, Hu E, Lee D. Stavenger RA, et al. J Med Chem. 2007 Jan 11;50(1):2-5. doi: 10.1021/jm060873p. J Med Chem. 2007. PMID: 17201404
Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.
Doe C, Bentley R, Behm DJ, Lafferty R, Stavenger R, Jung D, Bamford M, Panchal T, Grygielko E, Wright LL, Smith GK, Chen Z, Webb C, Khandekar S, Yi T, Kirkpatrick R, Dul E, Jolivette L, Marino JP Jr, Willette R, Lee D, Hu E. Doe C, et al. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. doi: 10.1124/jpet.106.110635. Epub 2006 Oct 3. J Pharmacol Exp Ther. 2007. PMID: 17018693
Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors.
Goodman KB, Cui H, Dowdell SE, Gaitanopoulos DE, Ivy RL, Sehon CA, Stavenger RA, Wang GZ, Viet AQ, Xu W, Ye G, Semus SF, Evans C, Fries HE, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D. Goodman KB, et al. Among authors: stavenger ra. J Med Chem. 2007 Jan 11;50(1):6-9. doi: 10.1021/jm0609014. J Med Chem. 2007. PMID: 17201405
Structure-guided design of antibacterials that allosterically inhibit DNA gyrase.
Thalji RK, Raha K, Andreotti D, Checchia A, Cui H, Meneghelli G, Profeta R, Tonelli F, Tommasi S, Bakshi T, Donovan BT, Howells A, Jain S, Nixon C, Quinque G, McCloskey L, Bax BD, Neu M, Chan PF, Stavenger RA. Thalji RK, et al. Among authors: stavenger ra. Bioorg Med Chem Lett. 2019 Jun 1;29(11):1407-1412. doi: 10.1016/j.bmcl.2019.03.029. Epub 2019 Mar 22. Bioorg Med Chem Lett. 2019. PMID: 30962087
Discovery and Characterization of a Class of Pyrazole Inhibitors of Bacterial Undecaprenyl Pyrophosphate Synthase.
Concha N, Huang J, Bai X, Benowitz A, Brady P, Grady LC, Kryn LH, Holmes D, Ingraham K, Jin Q, Pothier Kaushansky L, McCloskey L, Messer JA, O'Keefe H, Patel A, Satz AL, Sinnamon RH, Schneck J, Skinner SR, Summerfield J, Taylor A, Taylor JD, Evindar G, Stavenger RA. Concha N, et al. Among authors: stavenger ra. J Med Chem. 2016 Aug 11;59(15):7299-304. doi: 10.1021/acs.jmedchem.6b00746. Epub 2016 Jul 20. J Med Chem. 2016. PMID: 27379833
Imidazopyrazinones (IPYs): Non-Quinolone Bacterial Topoisomerase Inhibitors Showing Partial Cross-Resistance with Quinolones.
Jeannot F, Taillier T, Despeyroux P, Renard S, Rey A, Mourez M, Poeverlein C, Khichane I, Perrin MA, Versluys S, Stavenger RA, Huang J, Germe T, Maxwell A, Cao S, Huseby DL, Hughes D, Bacqué E. Jeannot F, et al. Among authors: stavenger ra. J Med Chem. 2018 Apr 26;61(8):3565-3581. doi: 10.1021/acs.jmedchem.7b01892. Epub 2018 Apr 10. J Med Chem. 2018. PMID: 29596745
Thiophene antibacterials that allosterically stabilize DNA-cleavage complexes with DNA gyrase.
Chan PF, Germe T, Bax BD, Huang J, Thalji RK, Bacqué E, Checchia A, Chen D, Cui H, Ding X, Ingraham K, McCloskey L, Raha K, Srikannathasan V, Maxwell A, Stavenger RA. Chan PF, et al. Among authors: stavenger ra. Proc Natl Acad Sci U S A. 2017 May 30;114(22):E4492-E4500. doi: 10.1073/pnas.1700721114. Epub 2017 May 15. Proc Natl Acad Sci U S A. 2017. PMID: 28507124 Free PMC article.
Structural basis of DNA gyrase inhibition by antibacterial QPT-1, anticancer drug etoposide and moxifloxacin.
Chan PF, Srikannathasan V, Huang J, Cui H, Fosberry AP, Gu M, Hann MM, Hibbs M, Homes P, Ingraham K, Pizzollo J, Shen C, Shillings AJ, Spitzfaden CE, Tanner R, Theobald AJ, Stavenger RA, Bax BD, Gwynn MN. Chan PF, et al. Among authors: stavenger ra. Nat Commun. 2015 Dec 7;6:10048. doi: 10.1038/ncomms10048. Nat Commun. 2015. PMID: 26640131 Free PMC article.
22 results