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Items: 1 to 50 of 112

1.

Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.

He S, Dobbelaar PH, Liu J, Jian T, Sebhat IK, Lin LS, Goodman A, Guo C, Guzzo PR, Hadden M, Henderson AJ, Ruenz M, Sargent BJ, Yet L, Kelly TM, Palyha O, Kan Y, Pan J, Chen H, Marsh DJ, Shearman LP, Strack AM, Metzger JM, Feighner SD, Tan C, Howard AD, Tamvakopoulos C, Peng Q, Guan XM, Reitman ML, Patchett AA, Wyvratt MJ Jr, Nargund RP.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1913-7. doi: 10.1016/j.bmcl.2010.01.154. Epub 2010 Feb 4.

PMID:
20167483
2.

Melanocortin subtype 4 receptor agonists: structure-activity relationships about the 4-alkyl piperidine core.

Sebhat IK, Lai Y, Barakat K, Ye Z, Tang R, Kalyani RN, Vongs A, Macneil T, Weinberg DH, Cabello MA, Maroto M, Teran A, Fong TM, Van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5720-3. Epub 2006 Dec 3.

PMID:
17768046
3.

Highly potent growth hormone secretagogues.

Lu Z, Tata JR, Cheng K, Wei L, Chan WW, Butler B, Schleim KD, Jacks TM, Hickey G, Patchett AA.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3657-9. Epub 2007 Apr 25.

PMID:
17482461
4.

Antidiabetic activity of a highly potent and selective nonpeptide somatostatin receptor subtype-2 agonist.

Strowski MZ, Cashen DE, Birzin ET, Yang L, Singh V, Jacks TM, Nowak KW, Rohrer SP, Patchett AA, Smith RG, Schaeffer JM.

Endocrinology. 2006 Oct;147(10):4664-73. Epub 2006 Jul 20.

PMID:
16857751
5.

Optimization of a privileged structure leading to potent and selective human melanocortin subtype-4 receptor ligands.

Bakshi RK, Hong Q, Tang R, Kalyani RN, Macneil T, Weinberg DH, Van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1130-3. Epub 2005 Dec 20.

PMID:
16364639
6.

Structure-activity relationship of linear tetrapeptides Tic-DPhe-Arg-Trp-NH2 at the human melanocortin-4 receptor and effects on feeding behaviors in rat.

Ye Z, MacNeil T, Weinberg DH, Kalyani RN, Tang R, Strack AM, Murphy BA, Mosley RT, Euan MacIntyre D, Van der Ploeg LH, Patchett AA, Wyvratt MJ, Nargund RP.

Peptides. 2005 Oct;26(10):2017-25.

PMID:
15993513
7.

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.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5.

PMID:
15982875
8.

1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.

Bakshi RK, Hong Q, Olson JT, Ye Z, Sebhat IK, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Martin WJ, Strack A, McGowan E, Tamvakopoulos C, Miller RR, Stearns RA, Tang W, Maclntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3430-3.

PMID:
15951175
9.

2-Piperazinecarboxamides as potent and selective melanocortin subtype-4 receptor agonists.

Palucki BL, Park MK, Nargund RP, Tang R, MacNeil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, Van der Ploeg LH, Patchett AA.

Bioorg Med Chem Lett. 2005 Apr 15;15(8):1993-6.

PMID:
15808454
10.

Discovery of (2S)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxoethyl]-4-methyl-2-piperazinecarboxamide (MB243), a potent and selective melanocortin subtype-4 receptor agonist.

Palucki BL, Park MK, Nargund RP, Ye Z, Sebhat IK, Pollard PG, Kalyani RN, Tang R, Macneil T, Weinberg DH, Vongs A, Rosenblum CI, Doss GA, Miller RR, Stearns RA, Peng Q, Tamvakopoulos C, McGowan E, Martin WJ, Metzger JM, Shepherd CA, Strack AM, Macintyre DE, Van der Ploeg LH, Patchett AA.

Bioorg Med Chem Lett. 2005 Jan 3;15(1):171-5.

PMID:
15582434
11.

Substituted bridged phenyl piperidines: orally active growth hormone secretagogues.

Lu Z, Tata JR, Cheng K, Wei L, Chan WW, Butler B, Schleim KD, Jacks TM, Hickey G, Patchett AA.

Bioorg Med Chem Lett. 2003 May 19;13(10):1817-20.

PMID:
12729672
12.

Lewis Hastings Sarett, December 22, 1917 - November 29, 1999.

Patchett AA.

Biogr Mem Natl Acad Sci. 2002;81:278-92. No abstract available.

PMID:
12661563
13.
14.

Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.

Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP.

J Med Chem. 2002 Oct 10;45(21):4589-93.

PMID:
12361385
15.

A role for the melanocortin 4 receptor in sexual function.

Van der Ploeg LH, Martin WJ, Howard AD, Nargund RP, Austin CP, Guan X, Drisko J, Cashen D, Sebhat I, Patchett AA, Figueroa DJ, DiLella AG, Connolly BM, Weinberg DH, Tan CP, Palyha OC, Pong SS, MacNeil T, Rosenblum C, Vongs A, Tang R, Yu H, Sailer AW, Fong TM, Huang C, Tota MR, Chang RS, Stearns R, Tamvakopoulos C, Christ G, Drazen DL, Spar BD, Nelson RJ, MacIntyre DE.

Proc Natl Acad Sci U S A. 2002 Aug 20;99(17):11381-6. Epub 2002 Aug 9.

16.

Spiro(indoline-3,4'-piperidine) growth hormone secretagogues as ghrelin mimetics.

Palucki BL, Feighner SD, Pong S, McKee KK, Hreniuk DL, Tan C, Howard AD, Van der Ploeg LH, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1955-7.

PMID:
11459669
17.

Angiotensin-converting enzyme inhibitors.

Menard J, Patchett AA.

Adv Protein Chem. 2001;56:13-75. Review. No abstract available.

PMID:
11329852
18.

Orphan G-protein-coupled receptors and natural ligand discovery.

Howard AD, McAllister G, Feighner SD, Liu Q, Nargund RP, Van der Ploeg LH, Patchett AA.

Trends Pharmacol Sci. 2001 Mar;22(3):132-40. Review.

PMID:
11239576
19.

Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists.

Zhou C, Guo L, Morriello G, Pasternak A, Pan Y, Rohrer SP, Birzin ET, Huskey SE, Jacks T, Schleim KD, Cheng K, Schaeffer JM, Patchett AA, Yang L.

Bioorg Med Chem Lett. 2001 Feb 12;11(3):415-7.

PMID:
11212124
20.

Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.

Ye Z, Gao Y, Bakshi RK, Chen MH, Rohrer SP, Feighner SD, Pong SS, Howard AD, Blake A, Birzin ET, Locco L, Parmar RM, Chan WW, Schaeffer JM, Smith RG, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 2000 Jan 3;10(1):5-8.

PMID:
10636230
21.

Ligand activation domain of human orphan growth hormone (GH) secretagogue receptor (GHS-R) conserved from Pufferfish to humans.

Palyha OC, Feighner SD, Tan CP, McKee KK, Hreniuk DL, Gao YD, Schleim KD, Yang L, Morriello GJ, Nargund R, Patchett AA, Howard AD, Smith RG.

Mol Endocrinol. 2000 Jan;14(1):160-9.

PMID:
10628755
22.

Growth hormone releasing substances: types and their receptors.

Smith RG, Palyha OC, Feighner SD, Tan CP, McKee KK, Hreniuk DL, Yang L, Morriello G, Nargund R, Patchett AA, Howard AD.

Horm Res. 1999;51 Suppl 3:1-8. Review.

PMID:
10592437
23.

Thiazole-derived potent, highly bioavailable short duration growth hormone secretagogues.

Yang L, Morriello G, Leung K, Jacks T, Cheng K, Schleim KD, Smith R, Patchett AA.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1761-6.

PMID:
10406638
24.

Receptor for motilin identified in the human gastrointestinal system.

Feighner SD, Tan CP, McKee KK, Palyha OC, Hreniuk DL, Pong SS, Austin CP, Figueroa D, MacNeil D, Cascieri MA, Nargund R, Bakshi R, Abramovitz M, Stocco R, Kargman S, O'Neill G, Van Der Ploeg LH, Evans J, Patchett AA, Smith RG, Howard AD.

Science. 1999 Jun 25;284(5423):2184-8.

25.

Synthesis and biological activities of spiroheterocyclic growth hormone secretagogues.

Chen MH, Pollard PP, Patchett AA, Cheng K, Wei L, Chan WW, Butler B, Jacks TM, Smith RG.

Bioorg Med Chem Lett. 1999 May 3;9(9):1261-6.

PMID:
10340611
26.

Potent, orally bioavailable somatostatin agonists: good absorption achieved by urea backbone cyclization.

Pasternak A, Pan Y, Marino D, Sanderson PE, Mosley R, Rohrer SP, Birzin ET, Huskey SE, Jacks T, Schleim KD, Cheng K, Schaeffer JM, Patchett AA, Yang L.

Bioorg Med Chem Lett. 1999 Feb 8;9(3):491-6.

PMID:
10091708
27.

Carbohydroxamido-oxazolidines: antibacterial agents that target lipid A biosynthesis.

Chen MH, Steiner MG, de Laszlo SE, Patchett AA, Anderson MS, Hyland SA, Onishi HR, Silver LL, Raetz CR.

Bioorg Med Chem Lett. 1999 Feb 8;9(3):313-8.

PMID:
10091675
28.

Potent 3-spiropiperidine growth hormone secretagogues.

Yang L, Morriello G, Prendergast K, Cheng K, Jacks T, Chan WW, Schleim KD, Smith RG, Patchett AA.

Bioorg Med Chem Lett. 1998 Jan 6;8(1):107-12.

PMID:
9925440
29.

Synthesis and biological activities of phenyl piperazine-based peptidomimetic growth hormone secretagogues.

Barakat KJ, Cheng K, Chan WW, Butler BS, Jacks TM, Schleim KD, Hora DF Jr, Hickey GJ, Smith RG, Patchett AA, Nargund RP.

Bioorg Med Chem Lett. 1998 Jun 2;8(11):1431-6.

PMID:
9871779
30.

Tripeptide growth hormone secretagogues.

Yang L, Morriello G, Pan Y, Nargund RP, Barakat K, Prendergast K, Cheng K, Chan WW, Smith RG, Patchett AA.

Bioorg Med Chem Lett. 1998 Apr 7;8(7):759-64.

PMID:
9871537
31.

Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry.

Rohrer SP, Birzin ET, Mosley RT, Berk SC, Hutchins SM, Shen DM, Xiong Y, Hayes EC, Parmar RM, Foor F, Mitra SW, Degrado SJ, Shu M, Klopp JM, Cai SJ, Blake A, Chan WW, Pasternak A, Yang L, Patchett AA, Smith RG, Chapman KT, Schaeffer JM.

Science. 1998 Oct 23;282(5389):737-40. Erratum in: Science 1998 Nov 27;282(5394):1646.

32.

Orally active growth hormone secretagogues.

Patchett AA, Smith RG, Wyvratt MJ.

Pharm Biotechnol. 1998;11:525-54. Review. No abstract available.

PMID:
9760695
33.

Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2.

Yang L, Berk SC, Rohrer SP, Mosley RT, Guo L, Underwood DJ, Arison BH, Birzin ET, Hayes EC, Mitra SW, Parmar RM, Cheng K, Wu TJ, Butler BS, Foor F, Pasternak A, Pan Y, Silva M, Freidinger RM, Smith RG, Chapman K, Schaeffer JM, Patchett AA.

Proc Natl Acad Sci U S A. 1998 Sep 1;95(18):10836-41.

34.

Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.

Nargund RP, Patchett AA, Bach MA, Murphy MG, Smith RG.

J Med Chem. 1998 Aug 13;41(17):3103-27. Review. No abstract available.

PMID:
9703459
35.

1-[2(R)-(2-amino-2-methylpropionylamino)-3-(1H-indol-3-yl)propionyl]- 3-benzylpiperidine-3(S)-carboxylic acid ethyl ester (L-163,540): a potent, orally bioavailable, and short-duration growth hormone secretagogue.

Yang L, Morriello G, Patchett AA, Leung K, Jacks T, Cheng K, Schleim KD, Feeney W, Chan WW, Chiu SH, Smith RG.

J Med Chem. 1998 Jul 2;41(14):2439-41. No abstract available.

PMID:
9651148
36.

Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.

Yang L, Guo L, Pasternak A, Mosley R, Rohrer S, Birzin E, Foor F, Cheng K, Schaeffer J, Patchett AA.

J Med Chem. 1998 Jun 18;41(13):2175-9. No abstract available.

PMID:
9632348
37.

Structural requirements for the activation of the human growth hormone secretagogue receptor by peptide and nonpeptide secretagogues.

Feighner SD, Howard AD, Prendergast K, Palyha OC, Hreniuk DL, Nargund R, Underwood D, Tata JR, Dean DC, Tan CP, McKee KK, Woods JW, Patchett AA, Smith RG, Van der Ploeg LH.

Mol Endocrinol. 1998 Jan;12(1):137-45.

PMID:
9440817
38.

Peptidomimetic regulation of growth hormone secretion.

Smith RG, Van der Ploeg LH, Howard AD, Feighner SD, Cheng K, Hickey GJ, Wyvratt MJ Jr, Fisher MH, Nargund RP, Patchett AA.

Endocr Rev. 1997 Oct;18(5):621-45. Review. No abstract available.

PMID:
9331545
39.

Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles.

Hickey GJ, Jacks TM, Schleim KD, Frazier E, Chen HY, Krupa D, Feeney W, Nargund RP, Patchett AA, Smith RG.

J Endocrinol. 1997 Feb;152(2):183-92.

PMID:
9071975
40.

Antibacterial agents that inhibit lipid A biosynthesis.

Onishi HR, Pelak BA, Gerckens LS, Silver LL, Kahan FM, Chen MH, Patchett AA, Galloway SM, Hyland SA, Anderson MS, Raetz CR.

Science. 1996 Nov 8;274(5289):980-2.

PMID:
8875939
41.

A receptor in pituitary and hypothalamus that functions in growth hormone release.

Howard AD, Feighner SD, Cully DF, Arena JP, Liberator PA, Rosenblum CI, Hamelin M, Hreniuk DL, Palyha OC, Anderson J, Paress PS, Diaz C, Chou M, Liu KK, McKee KK, Pong SS, Chaung LY, Elbrecht A, Dashkevicz M, Heavens R, Rigby M, Sirinathsinghji DJ, Dean DC, Melillo DG, Patchett AA, Nargund R, Griffin PR, DeMartino JA, Gupta SK, Schaeffer JM, Smith RG, Van der Ploeg LH.

Science. 1996 Aug 16;273(5277):974-7.

PMID:
8688086
42.

Development of a high specific activity sulfur-35-labeled sulfonamide radioligand that allowed the identification of a new growth hormone secretagogue receptor.

Dean DC, Nargund RP, Pong SS, Chaung LY, Griffin P, Melillo DG, Ellsworth RL, Van der Ploeg LH, Patchett AA, Smith RG.

J Med Chem. 1996 Apr 26;39(9):1767-70. No abstract available.

PMID:
8627599
43.

Identification of a new G-protein-linked receptor for growth hormone secretagogues.

Pong SS, Chaung LY, Dean DC, Nargund RP, Patchett AA, Smith RG.

Mol Endocrinol. 1996 Jan;10(1):57-61.

PMID:
8838145
44.

Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.

Patchett AA, Nargund RP, Tata JR, Chen MH, Barakat KJ, Johnston DB, Cheng K, Chan WW, Butler B, Hickey G, et al.

Proc Natl Acad Sci U S A. 1995 Jul 18;92(15):7001-5.

45.

In vivo pharmacology of a novel AT1 selective angiotensin II receptor antagonist, MK-996.

Kivlighn SD, Zingaro GJ, Gabel RA, Broten TP, Schorn TW, Schaffer LW, Naylor EM, Chakravarty PK, Patchett AA, Greenlee WJ, et al.

Am J Hypertens. 1995 Jan;8(1):58-66.

PMID:
7734099
46.

Structural model of antagonist and agonist binding to the angiotensin II, AT1 subtype, G protein coupled receptor.

Underwood DJ, Strader CD, Rivero R, Patchett AA, Greenlee W, Prendergast K.

Chem Biol. 1994 Dec;1(4):211-21.

PMID:
9383393
47.

Synthesis and structure-activity relationships of peptidyl alpha-keto heterocycles as novel inhibitors of prolyl endopeptidase.

Tsutsumi S, Okonogi T, Shibahara S, Ohuchi S, Hatsushiba E, Patchett AA, Christensen BG.

J Med Chem. 1994 Oct 14;37(21):3492-502.

PMID:
7932578
48.

Derivation of a 3D pharmacophore model for the angiotensin-II site one receptor.

Prendergast K, Adams K, Greenlee WJ, Nachbar RB, Patchett AA, Underwood DJ.

J Comput Aided Mol Des. 1994 Oct;8(5):491-512.

PMID:
7876897
49.

Triazolinone biphenylsulfonamide derivatives as orally active angiotensin II antagonists with potent AT1 receptor affinity and enhanced AT2 affinity.

Ashton WT, Chang LL, Flanagan KL, Hutchins SM, Naylor EM, Chakravarty PK, Patchett AA, Greenlee WJ, Chen TB, Faust KA, et al.

J Med Chem. 1994 Aug 19;37(17):2808-24.

PMID:
8064808
50.

Non-peptide angiotensin II receptor antagonists. 2. Design, synthesis, and biological activity of N-substituted (phenylamino)phenylacetic acids and acyl sulfonamides.

Dhanoa DS, Bagley SW, Chang RS, Lotti VJ, Chen TB, Kivlighn SD, Zingaro GJ, Siegl PK, Patchett AA, Greenlee WJ.

J Med Chem. 1993 Dec 24;36(26):4239-49. Erratum in: J Med Chem 1994 Apr 1;37(7):1034.

PMID:
8277506

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