| Name | VR1 |
|---|---|
| Synonyms | HVG 1; VR1; HVG1; VAULTRC 1; VAULTRC1; vRNA; vault RNA component 1; vRNAs… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 14505681 | Sun Q, Tafesse L, Islam K, Zhou X, Victory SF, Zhang C, Hachicha M, Schmid LA, Patel A, Rotshteyn Y, Valenzano KJ, Kyle DJ: 4-(2-pyridyl) piperazine-1-carboxamides: potent vanilloid receptor 1 antagonists. Bioorg Med Chem Lett. 2003 Oct 20;13(20):3611-6. A series of 4-(2-pyridyl) piperazine-1-carboxamide analogues based on the lead compound 1 was synthesized and evaluated for VR1 antagonist activity in -induced (CAP) and pH (5.5)-induced (pH) FLIPR assays in a rat VR1-expressing HEK293 cell line. |
82(1,1,1,2) | Details |
| 15771431 | Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI: Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl) piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl) amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J Med Chem. 2005 Mar 24;48(6):1857-72. |
81(1,1,1,1) | Details |
| 16870426 | 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: From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5217-21. Epub 2006 Jul 25. Bioisosteric replacement of piperazine with an aryl ring in lead VR1 antagonist 1 led to the biarylamide series. |
32(0,1,1,2) | Details |
| 15664827 | Park HG, Choi JY, Kim MH, Choi SH, Park MK, Lee J, Suh YG, Cho H, Oh U, Kim HD, Joo YH, Shin SS, Kim JK, Jeong YS, Koh HJ, Park YH, Jew SS: Biarylcarboxybenzamide derivatives as potent vanilloid receptor (VR1) antagonistic ligands. Bioorg Med Chem Lett. 2005 Feb 1;15(3):631-4. The replacement of the piperazine moiety of the lead compound 1 with phenyl ring showed quite enhanced antagonistic activity. |
2(0,0,0,2) | Details |
| 14723956 | Lee J, Kang SU, Lim JO, Choi HK, Jin MK, Toth A, Pearce LV, Tran R, Wang Y, Szabo T, Blumberg PM: N-[4-(methylsulfonylamino) benzyl] thiourea analogues as vanilloid receptor antagonists: analysis of structure-activity relationships for the "C-Region". Bioorg Med Chem. 2004 Jan 15;12(2):371-85. We recently reported that N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino) benzyl] thiourea (2) was a high affinity antagonist of the vanilloid receptor with a binding affinity of K (i)=63 nM and an antagonism of K (i)=53.9 nM in rat VR1 heterologously expressed in Chinese hamster ovary (CHO) cells (Mol. In an effort to further improve binding affinity and antagonistic potency, we have modified the C-region of the lead 4-t-butylbenzyl group with diverse surrogates, such as araalkyl, alkyl, 4-alkynylbenzyl, indanyl, 3,3-diarylpropyl, 4-alkoxybenzyl, 4-substituted piperazine and piperidine. |
2(0,0,0,2) | Details |