| Name | CCR5 |
|---|---|
| Synonyms | C C CKR 5; ChemR13; C C chemokine receptor type 5; CC chemokine receptor 5; CC CKR 5; CCCKR 5; CCCKR5; CCR 5… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18019544 | Feng DZ, Song YL, Jiang XH, Chen L, Long YQ: Forward- and reverse-synthesis of piperazinopiperidine amide analogs: a general access to structurally diverse 4-piperazinopiperidine-based CCR5 antagonists. Org Biomol Chem. 2007 Aug 21;5(16):2690-7. The S-configuration of the benzylic-substituent is vital for the CCR5 binding, and the bulky or aryl substituent on the 2-position in the piperazine ring is detrimental to the activity. |
145(1,3,3,5) | Details |
| 11585438 | Tagat JR, Steensma RW, McCombie SW, Nazareno DV, Lin SI, Neustadt BR, Cox K, Xu S, Wojcik L, Murray MG, Vantuno N, Baroudy BM, Strizki JM: Piperazine-based CCR5 antagonists as HIV-1 inhibitors. J Med Chem. 2001 Oct 11;44(21):3343-6. Truncation of the original piperidino-2 (S)-methyl piperazine lead structure 2, from a family of muscarinic antagonists, gave compound 8 which has improved selectivity for the HIV-1 co-receptor CCR5 over muscarinic receptors. |
144(1,3,3,4) | Details |
| 14521412 | Debnath AK: Generation of predictive pharmacophore models for CCR5 antagonists: study with piperidine- and piperazine-based compounds as a new class of HIV-1 entry inhibitors. J Med Chem. 2003 Oct 9;46(21):4501-15. |
64(0,2,2,4) | Details |
| 11514156 | Tagat JR, McCombie SW, Steensma RW, Lin S, Nazareno DV, Baroudy B, Vantuno N, Xu S, Liu J: Piperazine-based CCR5 antagonists as HIV-1 inhibitors. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2143-6. |
63(0,2,2,3) | Details |
| 15115380 | Tagat JR, McCombie SW, Nazareno D, Labroli MA, Xiao Y, Steensma RW, Strizki JM, Baroudy BM, Cox K, Lachowicz J, Varty G, Watkins R: Piperazine-based CCR5 antagonists as HIV-1 inhibitors. J Med Chem. 2004 May 6;47(10):2405-8. |
33(0,1,1,3) | Details |
| 15203141 | Jiang XH, Song YL, Long YQ: Facile synthesis of 4-substituted-4-aminopiperidine derivatives, the key building block of piperazine-based CCR5 antagonists. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3675-8. |
33(0,1,1,3) | Details |
| 20347189 | Fan X, Zhang HS, Chen L, Long YQ: Efficient synthesis and identification of novel propane-1,3-diamino bridged CCR5 antagonists with variation on the basic center carrier. Eur J Med Chem. 2010 Mar 7. By employing pharmacophore-based design and the privileged fragments reassembly, a series of piperidine-/tropane-/piperazine-bridged CCR5 antagonists were designed and synthesized via an efficient convergent synthesis strategy, with focus on the optimal choice of the basic center carrier structure. |
33(0,1,1,3) | Details |
| 12769714 | Boyle CD, Palani A: Structure-activity relationship studies: M2 and CCR5 receptor antagonists. . Curr Top Med Chem. 2003;3(10):1155-69. |
3(0,0,0,3) | Details |
| 12565973 | McCombie SW, Tagat JR, Vice SF, Lin SI, Steensma R, Palani A, Neustadt BR, Baroudy BM, Strizki JM, Endres M, Cox K, Dan N, Chou CC: Piperazine-based CCR5 antagonists as HIV-1 inhibitors. Bioorg Med Chem Lett. 2003 Feb 10;13(3):567-71. |
31(0,1,1,1) | Details |