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Benzyl vinylogous amide substituted aryldihydropyridazinones and aryldimethylpyrazolones as potent and selective PDE3B inhibitors.
Edmondson SD, Mastracchio A, He J, Chung CC, Forrest MJ, Hofsess S, MacIntyre E, Metzger J, O'Connor N, Patel K, Tong X, Tota MR, Van der Ploeg LH, Varnerin JP, Fisher MH, Wyvratt MJ, Weber AE, Parmee ER. Edmondson SD, et al. Among authors: van der ploeg lh. Bioorg Med Chem Lett. 2003 Nov 17;13(22):3983-7. doi: 10.1016/j.bmcl.2003.08.056. Bioorg Med Chem Lett. 2003. PMID: 14592490
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Guo L, Ye Z, Ujjainwalla F, Sings HL, Sebhat IK, Huber J, Weinberg DH, Tang R, MacNeil T, Tamvakopoulos C, Peng Q, MacIntyre E, van der Ploeg LH, Goulet MT, Wyvratt MJ, Nargund RP. Guo L, et al. Among authors: van der ploeg lh. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3242-7. doi: 10.1016/j.bmcl.2008.04.049. Epub 2008 Apr 25. Bioorg Med Chem Lett. 2008. PMID: 18479920
The role of tryptophan 1072 in human PDE3B inhibitor binding.
Chung C, Varnerin JP, Morin NR, MacNeil DJ, Singh SB, Patel S, Scapin G, Van der Ploeg LH, Tota MR. Chung C, et al. Among authors: van der ploeg lh. Biochem Biophys Res Commun. 2003 Aug 8;307(4):1045-50. doi: 10.1016/s0006-291x(03)01299-3. Biochem Biophys Res Commun. 2003. PMID: 12878217
Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-2-methyl-2-azabicyclo[2.2.2]octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist.
Ye Z, Guo L, Barakat KJ, Pollard PG, Palucki BL, Sebhat IK, Bakshi RK, Tang R, Kalyani RN, Vongs A, Chen AS, Chen HY, Rosenblum CI, MacNeil T, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen DE, Martin WJ, Metzger JM, Strack AM, MacIntyre DE, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP. Ye Z, et al. Among authors: van der ploeg lh. Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5. doi: 10.1016/j.bmcl.2005.05.109. Bioorg Med Chem Lett. 2005. PMID: 15982875
Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands.
Hong Q, Bakshi RK, Dellureficio J, He S, Ye Z, Dobbelaar PH, Sebhat IK, Guo L, Liu J, Jian T, Tang R, Kalyani RN, Macneil T, Vongs A, Rosenblum CI, Weinberg DH, Peng Q, Tamvakopoulos C, Miller RR, Stearns RA, Cashen D, Martin WJ, Chen AS, Metzger JM, Chen HY, Strack AM, Fong TM, Maclntyre E, Van der Ploeg LH, Wyvratt MJ, Nargund RP. Hong Q, et al. Among authors: van der ploeg lh. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4483-6. doi: 10.1016/j.bmcl.2010.06.038. Epub 2010 Jun 10. Bioorg Med Chem Lett. 2010. PMID: 20598533
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.
Armstrong HE, Galka A, Lin LS, Lanza TJ Jr, Jewell JP, Shah SK, Guthikonda R, Truong Q, Chang LL, Quaker G, Colandrea VJ, Tong X, Wang J, Xu S, Fong TM, Shen CP, Lao J, Chen J, Shearman LP, Stribling DS, Rosko K, Strack A, Ha S, Van der Ploeg L, Goulet MT, Hagmann WK. Armstrong HE, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2184-7. doi: 10.1016/j.bmcl.2007.01.087. Epub 2007 Feb 2. Bioorg Med Chem Lett. 2007. PMID: 17293109
220 results