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Items: 1 to 20 of 166

1.

6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists.

Saito T, Obitsu T, Kondo T, Matsui T, Nagao Y, Kusumi K, Matsumura N, Ueno S, Kishi A, Katsumata S, Kagamiishi Y, Nakai H, Toda M.

Bioorg Med Chem. 2011 Sep 15;19(18):5432-45. doi: 10.1016/j.bmc.2011.07.055. Epub 2011 Jul 31.

PMID:
21865047
2.

Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.

Huang CQ, Wilcoxen KM, Grigoriadis DE, McCarthy JR, Chen C.

Bioorg Med Chem Lett. 2004 Aug 2;14(15):3943-7.

PMID:
15225703
3.

Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF₁) receptor antagonists.

Saito T, Obitsu T, Minamoto C, Sugiura T, Matsumura N, Ueno S, Kishi A, Katsumata S, Nakai H, Toda M.

Bioorg Med Chem. 2011 Oct 15;19(20):5955-66. doi: 10.1016/j.bmc.2011.08.055. Epub 2011 Aug 27.

PMID:
21930387
4.

Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.

Wustrow DJ, Capiris T, Rubin R, Knobelsdorf JA, Akunne H, Davis MD, MacKenzie R, Pugsley TA, Zoski KT, Heffner TG, Wise LD.

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2067-70.

PMID:
9873487
5.

Cyclopenta[d]pyrimidines and dihydropyrrolo[2,3-d]pyrimidines as potent and selective corticotropin-releasing factor 1 receptor antagonists.

Arban R, Benedetti R, Bonanomi G, Capelli AM, Castiglioni E, Contini S, Degiorgis F, Di Felice P, Donati D, Fazzolari E, Gentile G, Marchionni C, Marchioro C, Messina F, Micheli F, Oliosi B, Pavone F, Pasquarello A, Perini B, Rinaldi M, Sabbatini FM, Vitulli G, Zarantonello P, Di Fabio R, St-Denis Y.

ChemMedChem. 2007 Apr;2(4):528-40.

PMID:
17335099
6.

Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.

Chen C, Wilcoxen KM, Huang CQ, McCarthy JR, Chen T, Grigoriadis DE.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3669-73.

PMID:
15203140
7.

Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.

Chen C, Wilcoxen KM, Huang CQ, Xie YF, McCarthy JR, Webb TR, Zhu YF, Saunders J, Liu XJ, Chen TK, Bozigian H, Grigoriadis DE.

J Med Chem. 2004 Sep 9;47(19):4787-98.

PMID:
15341493
8.

Design, synthesis, and SAR of 2-dialkylamino-4-arylpyrimidines as potent and selective corticotropin-releasing factor(1) (CRF(1)) receptor antagonists.

Huang CQ, Grigoriadis DE, Liu Z, McCarthy JR, Ramphal J, Webb T, Whitten JP, Xie MY, Chen C.

Bioorg Med Chem Lett. 2004 May 3;14(9):2083-6.

PMID:
15080983
9.

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
10.

Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.

Chen YL, Mansbach RS, Winter SM, Brooks E, Collins J, Corman ML, Dunaiskis AR, Faraci WS, Gallaschun RJ, Schmidt A, Schulz DW.

J Med Chem. 1997 May 23;40(11):1749-54.

PMID:
9171885
11.

Heteroaryl-substituted 4-(1H-pyrazol-1-yl)-5,6-dihydro-1H-pyrrolo[2,3-d]pyrimidine derivatives as potent and selective corticotropin-releasing factor receptor-1 antagonists.

Sabbatini FM, Di Fabio R, St-Denis Y, Capelli AM, Castiglioni E, Contini S, Donati D, Fazzolari E, Gentile G, Micheli F, Pavone F, Rinaldi M, Pasquarello A, Zampori MG, Di Felice P, Zarantonello P, Arban R, Perini B, Vitulli G, Benedetti R, Oliosi B, Worby A.

ChemMedChem. 2008 Feb;3(2):226-9. No abstract available.

PMID:
18000940
12.

Design, synthesis, and structure-activity relationships of novel pyrazolo[5,1-b]thiazole derivatives as potent and orally active corticotropin-releasing factor 1 receptor antagonists.

Takahashi Y, Hashizume M, Shin K, Terauchi T, Takeda K, Hibi S, Murata-Tai K, Fujisawa M, Shikata K, Taguchi R, Ino M, Shibata H, Yonaga M.

J Med Chem. 2012 Oct 11;55(19):8450-63. doi: 10.1021/jm300864p. Epub 2012 Oct 1.

PMID:
22971011
13.

Anxiolytic-like effects of the corticotropin-releasing factor1 (CRF1) antagonist DMP904 [4-(3-pentylamino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-pyrazolo-[1,5-a]-pyrimidine] administered acutely or chronically at doses occupying central CRF1 receptors in rats.

Lelas S, Wong H, Li YW, Heman KL, Ward KA, Zeller KL, Sieracki KK, Polino JL, Godonis HE, Ren SX, Yan XX, Arneric SP, Robertson DW, Hartig PR, Grossman S, Trainor GL, Taub RA, Zaczek R, Gilligan PJ, McElroy JF.

J Pharmacol Exp Ther. 2004 Apr;309(1):293-302. Epub 2004 Jan 23.

14.

Design and synthesis of tricyclic corticotropin-releasing factor-1 antagonists.

Gross RS, Guo Z, Dyck B, Coon T, Huang CQ, Lowe RF, Marinkovic D, Moorjani M, Nelson J, Zamani-Kord S, Grigoriadis DE, Hoare SR, Crowe PD, Bu JH, Haddach M, McCarthy J, Saunders J, Sullivan R, Chen T, Williams JP.

J Med Chem. 2005 Sep 8;48(18):5780-93.

PMID:
16134945
15.

Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.

Ducray R, Ballard P, Barlaam BC, Hickinson MD, Kettle JG, Ogilvie DJ, Trigwell CB.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):959-62. doi: 10.1016/j.bmcl.2007.12.035. Epub 2007 Dec 23.

PMID:
18182285
16.

Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.

Baraldi PG, Cacciari B, Romagnoli R, Spalluto G, Klotz KN, Leung E, Varani K, Gessi S, Merighi S, Borea PA.

J Med Chem. 1999 Nov 4;42(22):4473-8. No abstract available.

PMID:
10579811
17.

Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.

Baraldi PG, Cacciari B, Spalluto G, Bergonzoni M, Dionisotti S, Ongini E, Varani K, Borea PA.

J Med Chem. 1998 Jun 4;41(12):2126-33.

PMID:
9622554
18.

Antidepressant-like activity of corticotropin-releasing factor type-1 receptor antagonists in mice.

Nielsen DM, Carey GJ, Gold LH.

Eur J Pharmacol. 2004 Sep 19;499(1-2):135-46.

PMID:
15363960
19.

Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.

Baraldi PG, Fruttarolo F, Tabrizi MA, Preti D, Romagnoli R, El-Kashef H, Moorman A, Varani K, Gessi S, Merighi S, Borea PA.

J Med Chem. 2003 Mar 27;46(7):1229-41.

PMID:
12646033
20.

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

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