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Results: 1 to 20 of 93

1.

CCR2 receptor antagonists: optimization of biaryl sulfonamides to increase activity in whole blood.

Wang GZ, Haile PA, Daniel T, Belot B, Viet AQ, Goodman KB, Sha D, Dowdell SE, Varga N, Hong X, Chakravorty S, Webb C, Cornejo C, Olzinski A, Bernard R, Evans C, Emmons A, Briand J, Chung CW, Quek R, Lee D, Gough PJ, Sehon CA.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7291-4. doi: 10.1016/j.bmcl.2011.10.038. Epub 2011 Oct 19.

PMID:
22047688
[PubMed - indexed for MEDLINE]
2.

In vivo activity of an azole series of CCR2 antagonists.

Smethurst CA, Bevan N, Brooks C, Emmons A, Gough PJ, Mookherjee C, Moores K, Peace S, Philp J, Piercy V, Watson SP, Zippoli M.

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7252-5. doi: 10.1016/j.bmcl.2012.09.020. Epub 2012 Sep 23. Erratum in: Bioorg Med Chem Lett. 2013 Jan 1;23(1):382.

PMID:
23079519
[PubMed - indexed for MEDLINE]
3.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13.

PMID:
21036044
[PubMed - indexed for MEDLINE]
4.

Pharmacological profile of JNJ-27141491 [(S)-3-[3,4-difluorophenyl)-propyl]-5-isoxazol-5-yl-2-thioxo-2,3-dihydro-1H-imidazole-4-carboxyl acid methyl ester], as a noncompetitive and orally active antagonist of the human chemokine receptor CCR2.

Buntinx M, Hermans B, Goossens J, Moechars D, Gilissen RA, Doyon J, Boeckx S, Coesemans E, Van Lommen G, Van Wauwe JP.

J Pharmacol Exp Ther. 2008 Oct;327(1):1-9. doi: 10.1124/jpet.108.140723. Epub 2008 Jul 3.

PMID:
18599682
[PubMed - indexed for MEDLINE]
Free Article
5.

Identification of a sulfonamide series of CCR2 antagonists.

Peace S, Philp J, Brooks C, Piercy V, Moores K, Smethurst C, Watson S, Gaines S, Zippoli M, Mookherjee C, Ife R.

Bioorg Med Chem Lett. 2010 Jul 1;20(13):3961-4. doi: 10.1016/j.bmcl.2010.04.142. Epub 2010 May 7.

PMID:
20627722
[PubMed - indexed for MEDLINE]
6.

CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human CCR2 knockin mice.

Sullivan T, Miao Z, Dairaghi DJ, Krasinski A, Wang Y, Zhao BN, Baumgart T, Ertl LS, Pennell A, Seitz L, Powers J, Zhao R, Ungashe S, Wei Z, Boring L, Tsou CL, Charo I, Berahovich RD, Schall TJ, Jaen JC.

Am J Physiol Renal Physiol. 2013 Nov 1;305(9):F1288-97. doi: 10.1152/ajprenal.00316.2013. Epub 2013 Aug 28.

PMID:
23986513
[PubMed - indexed for MEDLINE]
Free PMC Article
7.

Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists.

Cai C, Kang FA, Hou C, O'Neill JC, Opas E, McKenney S, Johnson D, Sui Z.

Bioorg Med Chem Lett. 2013 Jan 1;23(1):351-4. doi: 10.1016/j.bmcl.2012.10.069. Epub 2012 Oct 24.

PMID:
23182090
[PubMed - indexed for MEDLINE]
8.

Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.

Lim JW, Oh Y, Kim JH, Oak MH, Na Y, Lee JO, Lee SW, Cho H, Park WK, Choi G, Kang J.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2099-102. doi: 10.1016/j.bmcl.2010.02.072. Epub 2010 Feb 20.

PMID:
20223662
[PubMed - indexed for MEDLINE]
9.

Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs.

Trujillo JI, Huang W, Hughes RO, Rogier DJ, Turner SR, Devraj R, Morton PA, Xue CB, Chao G, Covington MB, Newton RC, Metcalf B.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1827-31. doi: 10.1016/j.bmcl.2011.01.052. Epub 2011 Jan 21.

PMID:
21316220
[PubMed - indexed for MEDLINE]
10.

Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.

Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N, Xi N, Xu S, Bannon AW, Baumgartner JW.

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7.

PMID:
15745810
[PubMed - indexed for MEDLINE]
11.

Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2.

Shin N, Baribaud F, Wang K, Yang G, Wynn R, Covington MB, Feldman P, Gallagher KB, Leffet LM, Lo YY, Wang A, Xue CB, Newton RC, Scherle PA.

Biochem Biophys Res Commun. 2009 Sep 18;387(2):251-5. doi: 10.1016/j.bbrc.2009.06.135. Epub 2009 Jul 1.

PMID:
19576173
[PubMed - indexed for MEDLINE]
12.

Dopamine D2 receptor-mediated G protein activation assessed by agonist-stimulated [35S]guanosine 5'-O-(gamma-thiotriphosphate) binding in rat striatal membranes.

Odagaki Y, Toyoshima R.

Prog Neuropsychopharmacol Biol Psychiatry. 2006 Sep 30;30(7):1304-12. Epub 2006 Jul 7.

PMID:
16824659
[PubMed - indexed for MEDLINE]
13.

Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.

Koller M, Lingenhoehl K, Schmutz M, Vranesic IT, Kallen J, Auberson YP, Carcache DA, Mattes H, Ofner S, Orain D, Urwyler S.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3358-61. doi: 10.1016/j.bmcl.2011.04.017. Epub 2011 Apr 8.

PMID:
21531559
[PubMed - indexed for MEDLINE]
14.

Discovery and mapping of an intracellular antagonist binding site at the chemokine receptor CCR2.

Zweemer AJ, Bunnik J, Veenhuizen M, Miraglia F, Lenselink EB, Vilums M, de Vries H, Gibert A, Thiele S, Rosenkilde MM, IJzerman AP, Heitman LH.

Mol Pharmacol. 2014 Oct;86(4):358-68. doi: 10.1124/mol.114.093328. Epub 2014 Jul 14.

PMID:
25024169
[PubMed - indexed for MEDLINE]
15.

An orally active chemokine receptor CCR2 antagonist prevents glomerulosclerosis and renal failure in type 2 diabetes.

Sayyed SG, Ryu M, Kulkarni OP, Schmid H, Lichtnekert J, GrĂ¼ner S, Green L, Mattei P, Hartmann G, Anders HJ.

Kidney Int. 2011 Jul;80(1):68-78. doi: 10.1038/ki.2011.102. Epub 2011 Apr 20.

PMID:
21508925
[PubMed - indexed for MEDLINE]
16.

Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists.

Nirogi RV, Deshpande AD, Kambhampati R, Badange RK, Kota L, Daulatabad AV, Shinde AK, Ahmad I, Kandikere V, Jayarajan P, Dubey PK.

Bioorg Med Chem Lett. 2011 Jan 1;21(1):346-9. doi: 10.1016/j.bmcl.2010.11.001. Epub 2010 Nov 5.

PMID:
21134749
[PubMed - indexed for MEDLINE]
17.

5-HT-stimulated [35S]guanosine-5'-O-(3-thio)triphosphate binding as an assay for functional activation of G proteins coupled with 5-HT1B receptors in rat striatal membranes.

Odagaki Y, Toyoshima R.

Naunyn Schmiedebergs Arch Pharmacol. 2006 Feb;372(5):335-45. Epub 2006 Feb 21.

PMID:
16491386
[PubMed - indexed for MEDLINE]
18.

Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.

Sheppard GS, Wang J, Kawai M, Fidanze SD, BaMaung NY, Erickson SA, Barnes DM, Tedrow JS, Kolaczkowski L, Vasudevan A, Park DC, Wang GT, Sanders WJ, Mantei RA, Palazzo F, Tucker-Garcia L, Lou P, Zhang Q, Park CH, Kim KH, Petros A, Olejniczak E, Nettesheim D, Hajduk P, Henkin J, Lesniewski R, Davidsen SK, Bell RL.

J Med Chem. 2006 Jun 29;49(13):3832-49.

PMID:
16789740
[PubMed - indexed for MEDLINE]
19.

Development of displacement binding and GTPgammaS scintillation proximity assays for the identification of antagonists of the micro-opioid receptor.

Rodgers G, Hubert C, McKinzie J, Suter T, Statnick M, Emmerson P, Stancato L.

Assay Drug Dev Technol. 2003 Oct;1(5):627-36.

PMID:
15090235
[PubMed - indexed for MEDLINE]
20.

Tetrahydroquinoline sulfonamides as vasopressin 1b receptor antagonists.

Scott JD, Miller MW, Li SW, Lin SI, Vaccaro HA, Hong L, Mullins DE, Guzzi M, Weinstein J, Hodgson RA, Varty GB, Stamford AW, Chan TY, McKittrick BA, Greenlee WJ, Priestley T, Parker EM.

Bioorg Med Chem Lett. 2009 Nov 1;19(21):6018-22. doi: 10.1016/j.bmcl.2009.09.050. Epub 2009 Sep 17.

PMID:
19800231
[PubMed - indexed for MEDLINE]
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