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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
Wei B, Robarge K, Labadie SS, Chen J, Corson LB, DiPasquale A, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Hitz A, Hong R, Lai KW, Liu W, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Ultsch M, Xu Z, Yen I, Yu D, Yue Q, Zhou A, Purkey HE. Wei B, et al. Among authors: dragovich ps. Bioorg Med Chem Lett. 2022 Mar 1;59:128576. doi: 10.1016/j.bmcl.2022.128576. Epub 2022 Jan 19. Bioorg Med Chem Lett. 2022. PMID: 35065235
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 2. Peptide structure-activity studies.
Dragovich PS, Webber SE, Babine RE, Fuhrman SA, Patick AK, Matthews DA, Reich SH, Marakovits JT, Prins TJ, Zhou R, Tikhe J, Littlefield ES, Bleckman TM, Wallace MB, Little TL, Ford CE, Meador JW 3rd, Ferre RA, Brown EL, Binford SL, DeLisle DM, Worland ST. Dragovich PS, et al. J Med Chem. 1998 Jul 16;41(15):2819-34. doi: 10.1021/jm9800696. J Med Chem. 1998. PMID: 9667971
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements.
Dragovich PS, Prins TJ, Zhou R, Webber SE, Marakovits JT, Fuhrman SA, Patick AK, Matthews DA, Lee CA, Ford CE, Burke BJ, Rejto PA, Hendrickson TF, Tuntland T, Brown EL, Meador JW 3rd, Ferre RA, Harr JE, Kosa MB, Worland ST. Dragovich PS, et al. J Med Chem. 1999 Apr 8;42(7):1213-24. doi: 10.1021/jm9805384. J Med Chem. 1999. PMID: 10197965
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. Part 7: structure-activity studies of bicyclic 2-pyridone-containing peptidomimetics.
Dragovich PS, Prins TJ, Zhou R, Johnson TO, Brown EL, Maldonado FC, Fuhrman SA, Zalman LS, Patick AK, Matthews DA, Hou X, Meador JW, Ferre RA, Worland ST. Dragovich PS, et al. Bioorg Med Chem Lett. 2002 Mar 11;12(5):733-8. doi: 10.1016/s0960-894x(02)00008-2. Bioorg Med Chem Lett. 2002. PMID: 11858991
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics.
Dragovich PS, Prins TJ, Zhou R, Brown EL, Maldonado FC, Fuhrman SA, Zalman LS, Tuntland T, Lee CA, Patick AK, Matthews DA, Hendrickson TF, Kosa MB, Liu B, Batugo MR, Gleeson JP, Sakata SK, Chen L, Guzman MC, Meador JW 3rd, Ferre RA, Worland ST. Dragovich PS, et al. J Med Chem. 2002 Apr 11;45(8):1607-23. doi: 10.1021/jm010469k. J Med Chem. 2002. PMID: 11931615
Structure-based design of a parallel synthetic array directed toward the discovery of irreversible inhibitors of human rhinovirus 3C protease.
Johnson TO, Hua Y, Luu HT, Brown EL, Chan F, Chu SS, Dragovich PS, Eastman BW, Ferre RA, Fuhrman SA, Hendrickson TF, Maldonado FC, Matthews DA, Meador JW 3rd, Patick AK, Reich SH, Skalitzky DJ, Worland ST, Yang M, Zalman LS. Johnson TO, et al. Among authors: dragovich ps. J Med Chem. 2002 May 9;45(10):2016-23. doi: 10.1021/jm010435c. J Med Chem. 2002. PMID: 11985469
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 8. Pharmacological optimization of orally bioavailable 2-pyridone-containing peptidomimetics.
Dragovich PS, Prins TJ, Zhou R, Johnson TO, Hua Y, Luu HT, Sakata SK, Brown EL, Maldonado FC, Tuntland T, Lee CA, Fuhrman SA, Zalman LS, Patick AK, Matthews DA, Wu EY, Guo M, Borer BC, Nayyar NK, Moran T, Chen L, Rejto PA, Rose PW, Guzman MC, Dovalsantos EZ, Lee S, McGee K, Mohajeri M, Liese A, Tao J, Kosa MB, Liu B, Batugo MR, Gleeson JP, Wu ZP, Liu J, Meador JW 3rd, Ferre RA. Dragovich PS, et al. J Med Chem. 2003 Oct 9;46(21):4572-85. doi: 10.1021/jm030166l. J Med Chem. 2003. PMID: 14521419
91 results