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Items: 1 to 50 of 85

1.

Synthesis and evaluation of novel tricyclic benzo[4.5]cyclohepta[1.2]pyridine derivatives as NMDA/NR2B antagonists.

McIntyre CJ, McCauley JA, Bednar B, Bednar RA, Butcher JW, Claremon DA, Cunningham ME, Freidinger RM, Gaul SL, Homnick CF, Koblan KS, Mosser SD, Romano JJ, Liverton NJ.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):5132-5. doi: 10.1016/j.bmcl.2009.07.028. Epub 2009 Jul 10.

PMID:
19648007
2.

Using the ribosome to synthesize peptidomimetics.

Freidinger RM.

F1000 Biol Rep. 2009 Jul 8;1:53. doi: 10.3410/B1-53.

3.

2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Su DS, Lim JL, Tinney E, Wan BL, Murphy KL, Reiss DR, Harrell CM, O'Malley SS, Ransom RW, Chang RS, Pettibone DJ, Yu J, Tang C, Prueksaritanont T, Freidinger RM, Bock MG, Anthony NJ.

J Med Chem. 2008 Jul 10;51(13):3946-52. doi: 10.1021/jm800199h. Epub 2008 Jun 14.

PMID:
18553956
4.

Alpha-hydroxy amides as a novel class of bradykinin B1 selective antagonists.

Wood MR, Schirripa KM, Kim JJ, Kuduk SD, Chang RK, Di Marco CN, DiPardo RM, Wan BL, Murphy KL, Ransom RW, Chang RS, Holahan MA, Cook JJ, Lemaire W, Mosser SD, Bednar RA, Tang C, Prueksaritanont T, Wallace AA, Mei Q, Yu J, Bohn DL, Clayton FC, Adarayn ED, Sitko GR, Leonard YM, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):716-20. Epub 2007 Nov 19.

PMID:
18061443
5.

Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.

Su DS, Lim JL, Markowitz MK, Wan BL, Murphy KL, Reiss DR, Harrell CM, O'Malley SS, Ransom RW, Chang RS, Pettibone DJ, Tang C, Prueksaritanont T, Freidinger RM, Bock MG.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3006-9. Epub 2007 Mar 21.

PMID:
17428657
6.

Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.

Wood MR, Schirripa KM, Kim JJ, Wan BL, Murphy KL, Ransom RW, Chang RS, Tang C, Prueksaritanont T, Detwiler TJ, Hettrick LA, Landis ER, Leonard YM, Krueger JA, Lewis SD, Pettibone DJ, Freidinger RM, Bock MG.

J Med Chem. 2006 Feb 23;49(4):1231-4.

PMID:
16480259
7.

Bradykinin B1 antagonists: SAR studies in the 2,3-diaminopyridine series.

Kuduk SD, Chang RK, Ng C, Murphy KL, Ransom RW, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2005 Sep 1;15(17):3925-9.

PMID:
15993596
8.

Binding modes of dihydroquinoxalinones in a homology model of bradykinin receptor 1.

Ha SN, Hey PJ, Ransom RW, Harrell CM Jr, Murphy KL, Chang R, Chen TB, Su DS, Markowitz MK, Bock MG, Freidinger RM, Hess FJ.

Biochem Biophys Res Commun. 2005 May 27;331(1):159-66.

PMID:
15845373
9.

2,3-Diaminopyridine as a platform for designing structurally unique nonpeptide bradykinin B1 receptor antagonists.

Feng DM, Wai JM, Kuduk SD, Ng C, Murphy KL, Ransom RW, Reiss D, Chang RS, Harrell CM, MacNeil T, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.

Bioorg Med Chem Lett. 2005 May 2;15(9):2385-8.

PMID:
15837330
10.

2,3-diaminopyridine bradykinin B1 receptor antagonists.

Kuduk SD, Ng C, Feng DM, Wai JM, Chang RS, Harrell CM, Murphy KL, Ransom RW, Reiss D, Ivarsson M, Mason G, Boyce S, Tang C, Prueksaritanont T, Freidinger RM, Pettibone DJ, Bock MG.

J Med Chem. 2004 Dec 16;47(26):6439-42.

PMID:
15588075
11.

Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.

Su DS, Markowitz MK, Murphy KL, Wan BL, Zrada MM, Harrell CM, O'Malley SS, Hess JF, Ransom RW, Chang RS, Wallace MA, Raab CE, Dean DC, Pettibone DJ, Freidinger RM, Bock MG.

Bioorg Med Chem Lett. 2004 Dec 20;14(24):6045-8.

PMID:
15546726
12.

Pharmacological characterization and radioligand binding properties of a high-affinity, nonpeptide, bradykinin B1 receptor antagonist.

Ransom RW, Harrell CM, Reiss DR, Murphy KL, Chang RS, Hess JF, Miller PJ, O'Malley SS, Hey PJ, Kunapuli P, Su DS, Markowitz MK, Wallace MA, Raab CE, Jones AN, Dean DC, Pettibone DJ, Freidinger RM, Bock MG.

Eur J Pharmacol. 2004 Sep 19;499(1-2):77-84.

PMID:
15363953
13.

Progress towards the development of a HIV-1 gp41-directed vaccine.

McGaughey GB, Barbato G, Bianchi E, Freidinger RM, Garsky VM, Hurni WM, Joyce JG, Liang X, Miller MD, Pessi A, Shiver JW, Bogusky MJ.

Curr HIV Res. 2004 Apr;2(2):193-204. Review.

PMID:
15078183
14.

NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles.

McCauley JA, Theberge CR, Romano JJ, Billings SB, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Xia M, Cunningham ME, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ.

J Med Chem. 2004 Apr 8;47(8):2089-96.

PMID:
15056006
15.

Design and synthesis of novel bioactive peptides and peptidomimetics.

Freidinger RM.

J Med Chem. 2003 Dec 18;46(26):5553-66. No abstract available.

PMID:
14667208
16.

Discovery of a potent, non-peptide bradykinin B1 receptor antagonist.

Su DS, Markowitz MK, DiPardo RM, Murphy KL, Harrell CM, O'Malley SS, Ransom RW, Chang RS, Ha S, Hess FJ, Pettibone DJ, Mason GS, Boyce S, Freidinger RM, Bock MG.

J Am Chem Soc. 2003 Jun 25;125(25):7516-7.

PMID:
12812482
17.

Benzodiazepines as potent and selective bradykinin B1 antagonists.

Wood MR, Kim JJ, Han W, Dorsey BD, Homnick CF, DiPardo RM, Kuduk SD, MacNeil T, Murphy KL, Lis EV, Ransom RW, Stump GL, Lynch JJ, O'Malley SS, Miller PJ, Chen TB, Harrell CM, Chang RS, Sandhu P, Ellis JD, Bondiskey PJ, Pettibone DJ, Freidinger RM, Bock MG.

J Med Chem. 2003 May 8;46(10):1803-6.

PMID:
12723943
18.

Identification of a series of CCK-2 receptor nonpeptide agonists: sensitivity to stereochemistry and a receptor point mutation.

Kopin AS, McBride EW, Chen C, Freidinger RM, Chen D, Zhao CM, Beinborn M.

Proc Natl Acad Sci U S A. 2003 Apr 29;100(9):5525-30. Epub 2003 Apr 15.

19.

Novel 5-cyclopropyl-1,4-benzodiazepin-2-ones as potent and selective I(Ks)-blocking class III antiarrhythmic agents.

Butcher JW, Liverton NJ, Claremon DA, Freidinger RM, Jurkiewicz NK, Lynch JJ, Salata JJ, Wang J, Dieckhaus CM, Slaughter DE, Vyas K.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1165-8. Erratum in: Bioorg Med Chem Lett. 2003 Aug 4;13(15):2611.

PMID:
12643935
20.

HIV-1 vaccine development: constrained peptide immunogens show improved binding to the anti-HIV-1 gp41 MAb.

McGaughey GB, Citron M, Danzeisen RC, Freidinger RM, Garsky VM, Hurni WM, Joyce JG, Liang X, Miller M, Shiver J, Bogusky MJ.

Biochemistry. 2003 Mar 25;42(11):3214-23.

PMID:
12641452
21.

Orally efficacious NR2B-selective NMDA receptor antagonists.

Claiborne CF, McCauley JA, Libby BE, Curtis NR, Diggle HJ, Kulagowski JJ, Michelson SR, Anderson KD, Claremon DA, Freidinger RM, Bednar RA, Mosser SD, Gaul SL, Connolly TM, Condra CL, Bednar B, Stump GL, Lynch JJ, Macaulay A, Wafford KA, Koblan KS, Liverton NJ.

Bioorg Med Chem Lett. 2003 Feb 24;13(4):697-700.

PMID:
12639561
22.

A prostate-specific antigen (PSA)-activated vinblastine prodrug selectively kills PSA-secreting cells in vivo.

DeFeo-Jones D, Brady SF, Feng DM, Wong BK, Bolyar T, Haskell K, Kiefer DM, Leander K, McAvoy E, Lumma P, Pawluczyk JM, Wai J, Motzel SL, Keenan K, Van Zwieten M, Lin JH, Garsky VM, Freidinger R, Oliff A, Jones RE.

Mol Cancer Ther. 2002 May;1(7):451-9.

23.

Design and synthesis of a pro-drug of vinblastine targeted at treatment of prostate cancer with enhanced efficacy and reduced systemic toxicity.

Brady SF, Pawluczyk JM, Lumma PK, Feng DM, Wai JM, Jones R, DeFeo-Jones D, Wong BK, Miller-Stein C, Lin JH, Oliff A, Freidinger RM, Garsky VM.

J Med Chem. 2002 Oct 10;45(21):4706-15.

PMID:
12361397
24.

A nonpeptide oxytocin receptor antagonist radioligand highly selective for human receptors.

Lemaire W, O'Brien JA, Burno M, Chaudhary AG, Dean DC, Williams PD, Freidinger RM, Pettibone DJ, Williams DL Jr.

Eur J Pharmacol. 2002 Aug 16;450(1):19-28.

PMID:
12176104
25.

Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).

Nantermet PG, Barrow JC, Lundell GF, Pellicore JM, Rittle KE, Young M, Freidinger RM, Connolly TM, Condra C, Karczewski J, Bednar RA, Gaul SL, Gould RJ, Prendergast K, Selnick HG.

Bioorg Med Chem Lett. 2002 Feb 11;12(3):319-23.

PMID:
11814787
26.

The synthesis of a prodrug of doxorubicin designed to provide reduced systemic toxicity and greater target efficacy.

Garsky VM, Lumma PK, Feng DM, Wai J, Ramjit HG, Sardana MK, Oliff A, Jones RE, DeFeo-Jones D, Freidinger RM.

J Med Chem. 2001 Nov 22;44(24):4216-24.

PMID:
11708923
27.

Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.

Barrow JC, Nantermet PG, Selnick HG, Glass KL, Ngo PL, Young MB, Pellicore JM, Breslin MJ, Hutchinson JH, Freidinger RM, Condra C, Karczewski J, Bednar RA, Gaul SL, Stern A, Gould R, Connolly TM.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2691-6.

PMID:
11591503
28.

Cyclic imides as potent and selective alpha-1A adrenergic receptor antagonists.

DiPardo RM, Patane MA, Newton RC, Price R, Broten TP, Chang RS, Ransom RW, Di Salvo J, Freidinger RM, Bock MG.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1959-62.

PMID:
11459670
29.

In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist.

Chang RS, Chen TB, O'Malley SS, Pettibone DJ, DiSalvo J, Francis B, Bock MG, Freidinger R, Nagarathnam D, Miao SW, Shen Q, Lagu B, Murali Dhar TG, Tyagarajan S, Marzabadi MR, Wong WC, Gluchowski C, Forray C.

Eur J Pharmacol. 2000 Dec 15;409(3):301-12.

PMID:
11108825
30.

A peptide-doxorubicin 'prodrug' activated by prostate-specific antigen selectively kills prostate tumor cells positive for prostate-specific antigen in vivo.

DeFeo-Jones D, Garsky VM, Wong BK, Feng DM, Bolyar T, Haskell K, Kiefer DM, Leander K, McAvoy E, Lumma P, Wai J, Senderak ET, Motzel SL, Keenan K, Van Zwieten M, Lin JH, Freidinger R, Huff J, Oliff A, Jones RE.

Nat Med. 2000 Nov;6(11):1248-52.

PMID:
11062536
31.

Preparation and evaluation of 1,3-diaminocyclopentane-linked dihydropyrimidinone derivatives as selective alpha1a-receptor antagonists.

Barrow JC, Glass KL, Selnick HG, Freidinger RM, Chang RS, O'Malley SS, Woyden C.

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1917-20.

PMID:
10987417
32.

De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.

Lagu B, Tian D, Jeon Y, Li C, Wetzel JM, Nagarathnam D, Shen Q, Forray C, Chang RS, Broten TP, Ransom RW, Chan TB, O'Malley SS, Schorn TW, Rodrigues AD, Kassahun K, Pettibone DJ, Freidinger RO, Gluchowski C.

J Med Chem. 2000 Jul 27;43(15):2775-8. No abstract available.

PMID:
10956183
33.

Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.

Nantermet PG, Barrow JC, Selnick HG, Homnick CF, Freidinger RM, Chang RS, O'Malley SS, Reiss DR, Broten TP, Ransom RW, Pettibone DJ, Olah T, Forray C.

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1625-8.

PMID:
10937710
34.

In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.

Barrow JC, Nantermet PG, Selnick HG, Glass KL, Rittle KE, Gilbert KF, Steele TG, Homnick CF, Freidinger RM, Ransom RW, Kling P, Reiss D, Broten TP, Schorn TW, Chang RS, O'Malley SS, Olah TV, Ellis JD, Barrish A, Kassahun K, Leppert P, Nagarathnam D, Forray C.

J Med Chem. 2000 Jul 13;43(14):2703-18.

PMID:
10893308
35.

Nonpeptidic ligands for peptide and protein receptors.

Freidinger RM.

Curr Opin Chem Biol. 1999 Aug;3(4):395-406. Review.

PMID:
10419845
36.

Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

Williams PD, Bock MG, Evans BE, Freidinger RM, Gallicchio SN, Guidotti MT, Jacobson MA, Kuo MS, Levy MR, Lis EV, Michelson SR, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Salvatore C, Stauffer KJ, Woyden CJ.

Bioorg Med Chem Lett. 1999 May 3;9(9):1311-6.

PMID:
10340620
37.

Progress in the development of oxytocin antagonists for use in preterm labor.

Williams PD, Bock MG, Evans BE, Freidinger RM, Pettibone DJ.

Adv Exp Med Biol. 1998;449:473-9.

PMID:
10026841
38.

Nonpeptide oxytocin antagonists: potent, orally bioavailable analogs of L-371,257 containing a 1-R-(pyridyl)ethyl ether terminus.

Kuo MS, Bock MG, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Perlow DS, Pettibone DJ, Quigley AG, Reiss DR, Williams PD, Woyden CJ.

Bioorg Med Chem Lett. 1998 Nov 3;8(21):3081-6.

PMID:
9873680
39.

Synthesis of protected lactam-bridged dipeptides.

Perlow DS, Freidinger RM.

Methods Mol Med. 1999;23:209-25. doi: 10.1385/0-89603-517-4:209.

PMID:
21380900
40.

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.

41.

Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.

Bell IM, Erb JM, Freidinger RM, Gallicchio SN, Guare JP, Guidotti MT, Halpin RA, Hobbs DW, Homnick CF, Kuo MS, Lis EV, Mathre DJ, Michelson SR, Pawluczyk JM, Pettibone DJ, Reiss DR, Vickers S, Williams PD, Woyden CJ.

J Med Chem. 1998 Jun 4;41(12):2146-63.

PMID:
9622556
42.

Characterization of the two-step pathway for inhibition of thrombin by alpha-ketoamide transition state analogs.

Lewis SD, Lucas BJ, Brady SF, Sisko JT, Cutrona KJ, Sanderson PE, Freidinger RM, Mao SS, Gardell SJ, Shafer JA.

J Biol Chem. 1998 Feb 27;273(9):4843-54.

43.

Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]acetamide.

Selnick HG, Liverton NJ, Baldwin JJ, Butcher JW, Claremon DA, Elliott JM, Freidinger RM, King SA, Libby BE, McIntyre CJ, Pribush DA, Remy DC, Smith GR, Tebben AJ, Jurkiewicz NK, Lynch JJ, Salata JJ, Sanguinetti MC, Siegl PK, Slaughter DE, Vyas K.

J Med Chem. 1997 Nov 21;40(24):3865-8. No abstract available.

PMID:
9397166
44.

Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position.

Feng DM, Gardell SJ, Lewis SD, Bock MG, Chen Z, Freidinger RM, Naylor-Olsen AM, Ramjit HG, Woltmann R, Baskin EP, Lynch JJ, Lucas R, Shafer JA, Dancheck KB, Chen IW, Mao SS, Krueger JA, Hare TR, Mulichak AM, Vacca JP.

J Med Chem. 1997 Nov 7;40(23):3726-33.

PMID:
9371237
45.

Discovery and development of non-peptide antagonists of peptide hormone receptors.

Pettibone DJ, Freidinger RM.

Biochem Soc Trans. 1997 Aug;25(3):1051-7. Review. No abstract available.

PMID:
9388600
46.

Design of highly potent noncovalent thrombin inhibitors that utilize a novel lipophilic binding pocket in the thrombin active site.

Tucker TJ, Lumma WC, Mulichak AM, Chen Z, Naylor-Olsen AM, Lewis SD, Lucas R, Freidinger RM, Kuo LC.

J Med Chem. 1997 Mar 14;40(6):830-2. No abstract available.

PMID:
9083470
47.

Small molecule ligands for oxytocin and vasopressin receptors.

Freidinger RM, Pettibone DJ.

Med Res Rev. 1997 Jan;17(1):1-16. Review. No abstract available.

PMID:
8979247
48.

1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.

Williams PD, Clineschmidt BV, Erb JM, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Pettibone DJ, Reiss DR, Veber DF, et al.

J Med Chem. 1995 Nov 10;38(23):4634-6. No abstract available.

PMID:
7473590
49.

Conformationally constrained o-tolylpiperazine camphorsulfonamide oxytocin antagonists. Structural modifications that provide high receptor affinity and suggest a bioactive conformation.

Williams PD, Ball RG, Clineschmidt BV, Culberson JC, Erb JM, Freidinger RM, Pawluczyk JM, Perlow DS, Pettibone DJ, Veber DF.

Bioorg Med Chem. 1994 Sep;2(9):971-85.

PMID:
7712132
50.

Development and pharmacological assessment of novel peptide and nonpeptide oxytocin antagonists.

Pettibone DJ, Clineschmidt BV, Bock MG, Evans BE, Freidinger RM, Veber DF, Williams PD.

Regul Pept. 1993 Apr 29;45(1-2):289-93. Review. No abstract available.

PMID:
8511358

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