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Page 1
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: grotz d. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
DeMong D, Dai X, Hwa J, Miller M, Lin SI, Kang L, Stamford A, Greenlee W, Yu W, Wong M, Lavey B, Kozlowski J, Zhou G, Yang DY, Patel B, Soriano A, Zhai Y, Sondey C, Zhang H, Lachowicz J, Grotz D, Cox K, Morrison R, Andreani T, Cao Y, Liang M, Meng T, McNamara P, Wong J, Bradley P, Feng KI, Belani J, Chen P, Dai P, Gauuan J, Lin P, Zhao H. DeMong D, et al. Among authors: grotz d. J Med Chem. 2014 Mar 27;57(6):2601-10. doi: 10.1021/jm401858f. Epub 2014 Feb 26. J Med Chem. 2014. PMID: 24527772
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.
Mandal M, Mitra K, Grotz D, Lin X, Palamanda J, Kumari P, Buevich A, Caldwell JP, Chen X, Cox K, Favreau L, Hyde L, Kennedy ME, Kuvelkar R, Liu X, Mazzola RD, Parker E, Rindgen D, Sherer E, Wang H, Zhu Z, Stamford AW, Cumming JN. Mandal M, et al. Among authors: grotz d. J Med Chem. 2018 Dec 13;61(23):10700-10708. doi: 10.1021/acs.jmedchem.8b01326. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30388368
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
Wang Y, Chackalamannil S, Hu Z, Greenlee WJ, Clader J, Boyle CD, Kaminski JJ, Billard W, Binch H 3rd, Crosby G, Ruperto V, Duffy RA, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Lachowicz JE. Wang Y, et al. Among authors: grotz de. J Med Chem. 2002 Dec 5;45(25):5415-8. doi: 10.1021/jm0255163. J Med Chem. 2002. PMID: 12459007
Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.
Boyle CD, Chackalamannil S, Clader JW, Greenlee WJ, Josien HB, Kaminski JJ, Kozlowski JA, McCombie SW, Nazareno DV, Tagat JR, Wang Y, Zhou G, Billard W, Binch H, Crosby G, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE. Boyle CD, et al. Among authors: grotz de. Bioorg Med Chem Lett. 2001 Sep 3;11(17):2311-4. doi: 10.1016/s0960-894x(01)00435-8. Bioorg Med Chem Lett. 2001. PMID: 11527721
Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice.
Hastings NB, Wang X, Song L, Butts BD, Grotz D, Hargreaves R, Fred Hess J, Hong KK, Huang CR, Hyde L, Laverty M, Lee J, Levitan D, Lu SX, Maguire M, Mahadomrongkul V, McEachern EJ, Ouyang X, Rosahl TW, Selnick H, Stanton M, Terracina G, Vocadlo DJ, Wang G, Duffy JL, Parker EM, Zhang L. Hastings NB, et al. Among authors: grotz d. Mol Neurodegener. 2017 May 18;12(1):39. doi: 10.1186/s13024-017-0181-0. Mol Neurodegener. 2017. PMID: 28521765 Free PMC article.
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.
Boyle CD, Vice SF, Campion J, Chackalamannil S, Lankin CM, McCombie SW, Billard W, Binch H 3rd, Crosby G, Williams MC, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE. Boyle CD, et al. Among authors: grotz de. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3479-82. doi: 10.1016/s0960-894x(02)00742-4. Bioorg Med Chem Lett. 2002. PMID: 12419388
Development of an automated mass spectrometry system for the quantitative analysis of liver microsomal incubation samples: a tool for rapid screening of new compounds for metabolic stability.
Korfmacher WA, Palmer CA, Nardo C, Dunn-Meynell K, Grotz D, Cox K, Lin CC, Elicone C, Liu C, Duchoslav E. Korfmacher WA, et al. Among authors: grotz d. Rapid Commun Mass Spectrom. 1999;13(10):901-7. doi: 10.1002/(SICI)1097-0231(19990530)13:10<901::AID-RCM583>3.0.CO;2-5. Rapid Commun Mass Spectrom. 1999. PMID: 10353225