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Page 1
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.
Duplantier AJ, Becker SL, Bohanon MJ, Borzilleri KA, Chrunyk BA, Downs JT, Hu LY, El-Kattan A, James LC, Liu S, Lu J, Maklad N, Mansour MN, Mente S, Piotrowski MA, Sakya SM, Sheehan S, Steyn SJ, Strick CA, Williams VA, Zhang L. Duplantier AJ, et al. Among authors: maklad n. J Med Chem. 2009 Jun 11;52(11):3576-85. doi: 10.1021/jm900128w. J Med Chem. 2009. PMID: 19438227
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
Duplantier AJ, Efremov I, Candler J, Doran AC, Ganong AH, Haas JA, Hanks AN, Kraus KG, Lazzaro JT Jr, Lu J, Maklad N, McCarthy SA, O'Sullivan TJ, Rogers BN, Siuciak JA, Spracklin DK, Zhang L. Duplantier AJ, et al. Among authors: maklad n. Bioorg Med Chem Lett. 2009 May 1;19(9):2524-9. doi: 10.1016/j.bmcl.2009.03.032. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19328692
Discovery of 4-(5-methyloxazolo[4,5-b]pyridin-2-yl)-1,4-diazabicyclo[3.2.2]nonane (CP-810,123), a novel alpha 7 nicotinic acetylcholine receptor agonist for the treatment of cognitive disorders in schizophrenia: synthesis, SAR development, and in vivo efficacy in cognition models.
O'Donnell CJ, Rogers BN, Bronk BS, Bryce DK, Coe JW, Cook KK, Duplantier AJ, Evrard E, Hajós M, Hoffmann WE, Hurst RS, Maklad N, Mather RJ, McLean S, Nedza FM, O'Neill BT, Peng L, Qian W, Rottas MM, Sands SB, Schmidt AW, Shrikhande AV, Spracklin DK, Wong DF, Zhang A, Zhang L. O'Donnell CJ, et al. Among authors: maklad n. J Med Chem. 2010 Feb 11;53(3):1222-37. doi: 10.1021/jm9015075. J Med Chem. 2010. PMID: 20043678
1-[(1-methyl-1H-imidazol-2-yl)methyl]-4-phenylpiperidines as mGluR2 positive allosteric modulators for the treatment of psychosis.
Zhang L, Brodney MA, Candler J, Doran AC, Duplantier AJ, Efremov IV, Evrard E, Kraus K, Ganong AH, Haas JA, Hanks AN, Jenza K, Lazzaro JT, Maklad N, McCarthy SA, Qian W, Rogers BN, Rottas MD, Schmidt CJ, Siuciak JA, Tingley FD 3rd, Zhang AQ. Zhang L, et al. Among authors: maklad n. J Med Chem. 2011 Mar 24;54(6):1724-39. doi: 10.1021/jm101414h. Epub 2011 Mar 2. J Med Chem. 2011. PMID: 21366332
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: maklad n. J Med Chem. 2017 Jul 13;60(13):5673-5698. doi: 10.1021/acs.jmedchem.7b00397. Epub 2017 Jun 16. J Med Chem. 2017. PMID: 28574706
Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.
Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Pandit J, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, McGinnis D, O'Connor RE, O'Donnell CJ, Ogden A, Piotrowski M, Schmidt CJ, Seymour PA, Ueno H, Vansell N, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: maklad n. J Med Chem. 2018 Feb 8;61(3):1001-1018. doi: 10.1021/acs.jmedchem.7b01466. Epub 2018 Jan 16. J Med Chem. 2018. PMID: 29293004
Correction to Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, LaChapelle EA, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX. Helal CJ, et al. Among authors: maklad n. J Med Chem. 2018 Apr 26;61(8):3753. doi: 10.1021/acs.jmedchem.8b00475. Epub 2018 Apr 6. J Med Chem. 2018. PMID: 29624389 No abstract available.
Combination Treatment with Verinurad and Allopurinol in CKD: A Randomized Placebo and Active Controlled Trial.
Heerspink HJL, Stack AG, Terkeltaub R, Jongs N, Inker LA, Bjursell M, Maklad N, Perl S, Eklund O, Rikte T, Sjöström CD, Perkovic V; SAPPHIRE Investigators. Heerspink HJL, et al. Among authors: maklad n. J Am Soc Nephrol. 2024 Feb 20. doi: 10.1681/ASN.0000000000000326. Online ahead of print. J Am Soc Nephrol. 2024. PMID: 38564654 No abstract available.
77 results