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Items: 37

1.

Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors.

Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Stein AJ, Holt M, Valentine J, Zavadoski W.

Bioorg Med Chem Lett. 2017 Feb 1;27(3):413-419. doi: 10.1016/j.bmcl.2016.12.053. Epub 2016 Dec 23.

PMID:
28041831
2.

Tryptophan hydroxylase 1 Inhibition Impacts Pulmonary Vascular Remodeling in Two Rat Models of Pulmonary Hypertension.

Aiello RJ, Bourassa PA, Zhang Q, Dubins J, Goldberg DR, De Lombaert S, Humbert M, Guignabert C, Cavasin MA, McKinsey TA, Paralkar V.

J Pharmacol Exp Ther. 2017 Feb;360(2):267-279. doi: 10.1124/jpet.116.237933. Epub 2016 Dec 7.

PMID:
27927914
3.

Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors.

Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Stein AJ, Valentine J, Zavadoski W.

Bioorg Med Chem Lett. 2016 Jun 15;26(12):2855-2860. doi: 10.1016/j.bmcl.2016.04.057. Epub 2016 Apr 21.

PMID:
27146606
4.

Discovery of spirocyclic proline tryptophan hydroxylase-1 inhibitors.

Goldberg DR, De Lombaert S, Aiello R, Bourassa P, Barucci N, Zhang Q, Paralkar V, Valentine J, Zavadoski W.

Bioorg Med Chem Lett. 2016 Feb 15;26(4):1124-9. doi: 10.1016/j.bmcl.2016.01.064. Epub 2016 Jan 22.

PMID:
26821821
5.

Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915).

Takahashi H, Riether D, Bartolozzi A, Bosanac T, Berger V, Binetti R, Broadwater J, Chen Z, Crux R, De Lombaert S, Dave R, Dines JA, Fadra-Khan T, Flegg A, Garrigou M, Hao MH, Huber J, Hutzler JM, Kerr S, Kotey A, Liu W, Lo HY, Loke PL, Mahaney PE, Morwick TM, Napier S, Olague A, Pack E, Padyana AK, Thomson DS, Tye H, Wu L, Zindell RM, Abeywardane A, Simpson T.

J Med Chem. 2015 Feb 26;58(4):1669-90. doi: 10.1021/jm501185j. Epub 2015 Feb 11.

PMID:
25671290
6.

Discovery of potent, selective chymase inhibitors via fragment linking strategies.

Taylor SJ, Padyana AK, Abeywardane A, Liang S, Hao MH, De Lombaert S, Proudfoot J, Farmer BS 3rd, Li X, Collins B, Martin L, Albaugh DR, Hill-Drzewi M, Pullen SS, Takahashi H.

J Med Chem. 2013 Jun 13;56(11):4465-81. doi: 10.1021/jm400138z. Epub 2013 Jun 4.

PMID:
23659209
7.

Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.

Huber JD, Bentzien J, Boyer SJ, Burke J, De Lombaert S, Eickmeier C, Guo X, Haist JV, Hickey ER, Kaplita P, Karmazyn M, Kemper R, Kennedy CA, Kirrane T, Madwed JB, Mainolfi E, Nagaraja N, Soleymanzadeh F, Swinamer A, Eldrup AB.

J Med Chem. 2012 Aug 23;55(16):7114-40. doi: 10.1021/jm300601d. Epub 2012 Aug 6.

PMID:
22803959
8.

Benzimidazolone as potent chymase inhibitor: modulation of reactive metabolite formation in the hydrophobic (P1) region.

Lo HY, Nemoto PA, Kim JM, Hao MH, Qian KC, Farrow NA, Albaugh DR, Fowler DM, Schneiderman RD, Michael August E, Martin L, Hill-Drzewi M, Pullen SS, Takahashi H, De Lombaert S.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4533-9. doi: 10.1016/j.bmcl.2011.05.126. Epub 2011 Jun 17.

PMID:
21733690
9.

Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.

Hodgetts KJ, Ge P, Yoon T, De Lombaert S, Brodbeck R, Gulianello M, Kieltyka A, Horvath RF, Kehne JH, Krause JE, Maynard GD, Hoffman D, Lee Y, Fung L, Doller D.

J Med Chem. 2011 Jun 23;54(12):4187-206. doi: 10.1021/jm200365y. Epub 2011 May 27.

PMID:
21618986
10.

Discovery and evaluation of pyrazolo[1,5-a]pyrimidines as neuropeptide Y1 receptor antagonists.

Griffith DA, Hargrove DM, Maurer TS, Blum CA, De Lombaert S, Inthavongsay JK, Klade LE, Mack CM, Rose CR, Sanders MJ, Carpino PA.

Bioorg Med Chem Lett. 2011 May 1;21(9):2641-5. doi: 10.1016/j.bmcl.2010.12.116. Epub 2011 Jan 7.

PMID:
21295475
11.

Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method.

Kowalski JA, Swinamer AD, Muegge I, Eldrup AB, Kukulka A, Cywin CL, De Lombaert S.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3703-7. doi: 10.1016/j.bmcl.2010.04.078. Epub 2010 Apr 22.

PMID:
20472432
12.

Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.

Blum CA, Caldwell T, Zheng X, Bakthavatchalam R, Capitosti S, Brielmann H, De Lombaert S, Kershaw MT, Matson D, Krause JE, Cortright D, Crandall M, Martin WJ, Murphy BA, Boyce S, Jones AB, Mason G, Rycroft W, Perrett H, Conley R, Burnaby-Davies N, Chenard BL, Hodgetts KJ.

J Med Chem. 2010 Apr 22;53(8):3330-48. doi: 10.1021/jm100051g.

PMID:
20307063
13.

Optimization of piperidyl-ureas as inhibitors of soluble epoxide hydrolase.

Eldrup AB, Soleymanzadeh F, Farrow NA, Kukulka A, De Lombaert S.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):571-5. doi: 10.1016/j.bmcl.2009.11.091. Epub 2009 Nov 22.

PMID:
19969453
14.

Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase.

Taylor SJ, Soleymanzadeh F, Eldrup AB, Farrow NA, Muegge I, Kukulka A, Kabcenell AK, De Lombaert S.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5864-8. doi: 10.1016/j.bmcl.2009.08.074. Epub 2009 Aug 26.

PMID:
19758802
15.

Structure-based optimization of arylamides as inhibitors of soluble epoxide hydrolase.

Eldrup AB, Soleymanzadeh F, Taylor SJ, Muegge I, Farrow NA, Joseph D, McKellop K, Man CC, Kukulka A, De Lombaert S.

J Med Chem. 2009 Oct 8;52(19):5880-95. doi: 10.1021/jm9005302.

PMID:
19746975
16.

Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design.

Cook BN, Bentzien J, White A, Nemoto PA, Wang J, Man CC, Soleymanzadeh F, Khine HH, Kashem MA, Kugler SZ Jr, Wolak JP, Roth GP, De Lombaert S, Pullen SS, Takahashi H.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):773-7. doi: 10.1016/j.bmcl.2008.12.028. Epub 2008 Dec 10.

PMID:
19111460
17.

2-Arylpyrimidines: novel CRF-1 receptor antagonists.

Yoon T, De Lombaert S, Brodbeck R, Gulianello M, Krause JE, Hutchison A, Horvath RF, Ge P, Kehne J, Hoffman D, Chandrasekhar J, Doller D, Hodgetts KJ.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4486-90. doi: 10.1016/j.bmcl.2008.07.063. Epub 2008 Jul 18.

PMID:
18672365
18.

Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.

Blum CA, Zheng X, Brielmann H, Hodgetts KJ, Bakthavatchalam R, Chandrasekhar J, Krause JE, Cortright D, Matson D, Crandall M, Ngo CK, Fung L, Day M, Kershaw M, De Lombaert S, Chenard BL.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4573-7. doi: 10.1016/j.bmcl.2008.07.036. Epub 2008 Jul 15.

PMID:
18662872
19.

The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists.

Yoon T, De Lombaert S, Brodbeck R, Gulianello M, Chandrasekhar J, Horvath RF, Ge P, Kershaw MT, Krause JE, Kehne J, Hoffman D, Doller D, Hodgetts KJ.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):891-6. doi: 10.1016/j.bmcl.2007.12.050. Epub 2008 Jan 3.

PMID:
18180159
20.

From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.

Zheng X, Hodgetts KJ, Brielmann H, Hutchison A, Burkamp F, Brian Jones A, Blurton P, Clarkson R, Chandrasekhar J, Bakthavatchalam R, De Lombaert S, Crandall M, Cortright D, Blum CA.

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. Epub 2006 Jul 25.

PMID:
16870426
22.

2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists.

Hodgetts KJ, Yoon T, Huang J, Gulianello M, Kieltyka A, Primus R, Brodbeck R, De Lombaert S, Doller D.

Bioorg Med Chem Lett. 2003 Aug 4;13(15):2497-500.

PMID:
12852951
23.

Non-peptidic CRF1 receptor antagonists for the treatment of anxiety, depression and stress disorders.

Kehne J, De Lombaert S.

Curr Drug Targets CNS Neurol Disord. 2002 Oct;1(5):467-93. Review.

PMID:
12769601
24.

3-Aryl pyrazolo[4,3-d]pyrimidine derivatives: Nonpeptide CRF-1 antagonists.

Yuan J, Gulianello M, De Lombaert S, Brodbeck R, Kieltyka A, Hodgetts KJ.

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2133-6.

PMID:
12127521
25.

Pharmacological properties of CGS 35066, a potent and selective endothelin-converting enzyme inhibitor, in conscious rats.

Trapani AJ, Beil ME, Bruseo CW, De Lombaert S, Jeng AY.

J Cardiovasc Pharmacol. 2000 Nov;36(5 Suppl 1):S40-3.

PMID:
11078331
26.

Design and synthesis of a potent and selective endothelin-converting enzyme inhibitor, CGS 35066.

Jeng AY, De Lombaert S, Beil ME, Bruseo CW, Savage P, Chou M, Trapani AJ.

J Cardiovasc Pharmacol. 2000 Nov;36(5 Suppl 1):S36-9.

PMID:
11078330
27.

CGS 34043: a non-peptidic, potent and long-acting dual inhibitor of endothelin converting enzyme-1 and neutral endopeptidase 24.11.

Trapani AJ, De Lombaert S, Beil ME, Bruseo CW, Savage P, Chou M, Jeng AY.

Life Sci. 2000;67(9):1025-33.

PMID:
10954036
28.

Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.

De Lombaert S, Blanchard L, Stamford LB, Tan J, Wallace EM, Satoh Y, Fitt J, Hoyer D, Simonsbergen D, Moliterni J, Marcopoulos N, Savage P, Chou M, Trapani AJ, Jeng AY.

J Med Chem. 2000 Feb 10;43(3):488-504.

PMID:
10669576
29.

Characterization of CGS 31447, a potent and nonpeptidic endothelin-converting enzyme inhibitor.

Shetty SS, Savage P, DelGrande D, De Lombaert S, Jeng AY.

J Cardiovasc Pharmacol. 1998;31 Suppl 1:S68-70.

PMID:
9595403
30.

Differential inhibition of wild-type endothelin-converting enzyme-1 and its mutants.

Savage P, De Lombaert S, Shimada K, Tanzawa K, Jeng AY.

J Cardiovasc Pharmacol. 1998;31 Suppl 1:S16-8.

PMID:
9595388
31.

Antihypertensive and natriuretic effects of CGS 30440, a dual inhibitor of angiotensin-converting enzyme and neutral endopeptidase 24.11.

Chatelain RE, Ghai RD, Trapani AJ, Odorico LM, Dardik BN, De Lombaert S, Lappe RW, Fink CA.

J Pharmacol Exp Ther. 1998 Mar;284(3):974-82.

PMID:
9495857
32.

A rapid indirect method to determine the plasma concentrations of neutral endopeptidase inhibitors.

Ghai RD, De Lombaert S, Ksander GM, Berry C, Sakane Y, Trapani AJ.

Res Commun Mol Pathol Pharmacol. 1995 Feb;87(2):211-20.

PMID:
7749658
33.
34.

Pharmacological profile of a non-peptidic dual inhibitor of neutral endopeptidase 24.11 and endothelin-converting enzyme.

De Lombaert S, Ghai RD, Jeng AY, Trapani AJ, Webb RL.

Biochem Biophys Res Commun. 1994 Oct 14;204(1):407-12.

PMID:
7945387
35.

Pharmacologic profile of CGS 24128, a potent, long-acting inhibitor of neutral endopeptidase 24.11.

Trapani AJ, Beil ME, Coté DT, de Lombaert S, Erion MD, Gerlock TE, Ghai RD, Hopkins MF, Peppard JV, Webb RL, et al.

J Cardiovasc Pharmacol. 1994 Mar;23(3):358-64.

PMID:
7515977
36.

N-Phosphonomethyl dipeptides and their phosphonate prodrugs, a new generation of neutral endopeptidase (NEP, EC 3.4.24.11) inhibitors.

De Lombaert S, Erion MD, Tan J, Blanchard L, el-Chehabi L, Ghai RD, Sakane Y, Berry C, Trapani AJ.

J Med Chem. 1994 Feb 18;37(4):498-511.

PMID:
8120868
37.

The pharmacology of CGS 25462: a potent, orally bioavailable, long-acting inhibitor of neutral endopeptidase 24.11.

Trapani AJ, De Lombaert S, Erion MD, Ghai RD, Peppard JV, Lappe RW, Worcel M.

J Hypertens Suppl. 1993 Dec;11(5):S220-1. No abstract available.

PMID:
8158354

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