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Page 1
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists part 2: A hybrid strategy combining key fragments of HTS hits.
Chen CA, Jiang Y, Lu K, Daniewska I, Mazza CG, Negron L, Forray C, Parola T, Li B, Hegde LG, Wolinsky TD, Craig DA, Kong R, Wetzel JM, Andersen K, Marzabadi MR. Chen CA, et al. Among authors: hegde lg. J Med Chem. 2007 Aug 9;50(16):3883-90. doi: 10.1021/jm060383x. J Med Chem. 2007. PMID: 17668922
Synthesis and SAR investigations for novel melanin-concentrating hormone 1 receptor (MCH1) antagonists Part 1. The discovery of arylacetamides as viable replacements for the dihydropyrimidinone moiety of an HTS hit.
Jiang Y, Chen CA, Lu K, Daniewska I, De Leon J, Kong R, Forray C, Li B, Hegde LG, Wolinsky TD, Craig DA, Wetzel JM, Andersen K, Marzabadi MR. Jiang Y, et al. Among authors: hegde lg. J Med Chem. 2007 Aug 9;50(16):3870-82. doi: 10.1021/jm060381c. J Med Chem. 2007. PMID: 17668921
The novel neuropeptide Y Y5 receptor antagonist Lu AA33810 [N-[[trans-4-[(4,5-dihydro[1]benzothiepino[5,4-d]thiazol-2-yl)amino]cyclohexyl]methyl]-methanesulfonamide] exerts anxiolytic- and antidepressant-like effects in rat models of stress sensitivity.
Walker MW, Wolinsky TD, Jubian V, Chandrasena G, Zhong H, Huang X, Miller S, Hegde LG, Marsteller DA, Marzabadi MR, Papp M, Overstreet DH, Gerald CP, Craig DA. Walker MW, et al. Among authors: hegde lg. J Pharmacol Exp Ther. 2009 Mar;328(3):900-11. doi: 10.1124/jpet.108.144634. Epub 2008 Dec 19. J Pharmacol Exp Ther. 2009. PMID: 19098165
Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocampal neurogenesis.
David DJ, Klemenhagen KC, Holick KA, Saxe MD, Mendez I, Santarelli L, Craig DA, Zhong H, Swanson CJ, Hegde LG, Ping XI, Dong D, Marzabadi MR, Gerald CP, Hen R. David DJ, et al. Among authors: hegde lg. J Pharmacol Exp Ther. 2007 Apr;321(1):237-48. doi: 10.1124/jpet.106.109678. Epub 2007 Jan 19. J Pharmacol Exp Ther. 2007. PMID: 17237257
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors.
Keylor MH, Gulati A, Kattar SD, Johnson RE, Chau RW, Margrey KA, Ardolino MJ, Zarate C, Poremba KE, Simov V, Morriello GJ, Acton JJ, Pio B, Yan X, Palte RL, McMinn SE, Nogle L, Lesburg CA, Adpressa D, Lin S, Neelamkavil S, Liu P, Su J, Hegde LG, Woodhouse JD, Faltus R, Xiong T, Ciaccio PJ, Piesvaux J, Otte KM, Wood HB, Kennedy ME, Bennett DJ, DiMauro EF, Fell MJ, Fuller PH. Keylor MH, et al. Among authors: hegde lg. J Med Chem. 2022 Jan 13;65(1):838-856. doi: 10.1021/acs.jmedchem.1c01968. Epub 2021 Dec 30. J Med Chem. 2022. PMID: 34967623
Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Zhang H, Lapointe BT, Anthony N, Azevedo R, Cals J, Correll CC, Daniels M, Deshmukh S, van Eenenaam H, Ferguson H, Hegde LG, Karstens WJ, Maclean J, Miller JR, Moy LY, Simov V, Nagpal S, Oubrie A, Palte RL, Parthasarathy G, Sciammetta N, van der Stelt M, Woodhouse JD, Trotter BW, Barr K. Zhang H, et al. Among authors: hegde lg. ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13. ACS Med Chem Lett. 2020. PMID: 32071676 Free PMC article.
Characterization of the Onset, Progression, and Reversibility of Morphological Changes in Mouse Lung after Pharmacological Inhibition of Leucine-Rich Kinase 2 Kinase Activity.
Bryce DK, Ware CM, Woodhouse JD, Ciaccio PJ, Ellis JM, Hegde LG, Kuruvilla S, Maddess ML, Markgraf CG, Otte KM, Poulet FM, Timmins LM, Kennedy ME, Fell MJ. Bryce DK, et al. Among authors: hegde lg. J Pharmacol Exp Ther. 2021 Apr;377(1):11-19. doi: 10.1124/jpet.120.000217. Epub 2021 Jan 28. J Pharmacol Exp Ther. 2021. PMID: 33509901
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Gulati A, Yeung CS, Lapointe B, Kattar SD, Gunaydin H, Scott JD, Childers KK, Methot JL, Simov V, Kurukulasuriya R, Pio B, Morriello GJ, Liu P, Tang H, Neelamkavil S, Wood HB, Rada VL, Ardolino MJ, Yan XC, Palte R, Otte K, Faltus R, Woodhouse J, Hegde LG, Ciaccio P, Minnihan EC, DiMauro EF, Fell MJ, Fuller PH, Ellis JM. Gulati A, et al. Among authors: hegde lg. RSC Med Chem. 2021 Jun 4;12(7):1164-1173. doi: 10.1039/d1md00097g. eCollection 2021 Jul 21. RSC Med Chem. 2021. PMID: 34355182 Free PMC article.
24 results