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�й�ҩѧ��־ 2012, Vol. 47 Issue (14) :1097-1100    DOI:
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CHEN Wen-Wen, LIU Xin-Yong-* .[J]  Chinese Pharmaceutical Journal, 2012,V47(14): 1097-1100
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[1] UAIDS report�� 2010. http�� //www. unaids. org/ documents/ 20101123_Global Report_em. pdf
[2] BARBARO G�� SCOZZAFAVA A�� MASTROLORENZO A�� et al. Highly active antiretroviral therapy�� current state of the art�� new agents and their pharmacological interactions useful for improving therapeutic outcome [J]. Curr Pharm Des�� 2005�� 11(14)�� 1805-1843.
[3] BODEN D�� HURLEY A�� ZHANG L�� et al. HIV-1 drug resistance in newly infected individuals [J]. JAMA�� 1999�� 282(12)�� 1135-1141.
[4] WERB D�� MILLS E J�� MONTANER J S�� et al. Risk of resistance to highly active antiretroviral therapy among HIV-positive injecting drug users�� a meta-analysis [J]. Lancet Infect Dis�� 2010�� 10(7)�� 464-469.
[5] INTROCASO C E�� HINES J M�� AND KOVARIK C L. Cutaneous toxicities of antiretroviral therapy for HIV�� part I. Lipodystrophy syndrome�� nucleoside reverse transcriptase inhibitors�� and protease inhibitors [J]. J Am Acad Dermatol�� 2010�� 63(4)�� 549-561.
[6] SAMSON M�� LIBERT F�� DORANZ B J�� et al. Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene [J]. Nature�� 1996�� 382(6593)�� 722-725.
[7] DORR P�� WESTBY M�� DOBBS S�� et al. Maraviroc (UK-427��857)�� a potent�� orally bioavailable�� and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity [J]. Antimicrob Agents Chemother�� 2005�� 49(11)�� 4721-4732.
[8] GILLIAM B L�� RIEDEL D J�� REDFIELD R R. Clinical use of CCR5 inhibitors in HIV and beyond [J]. J Transl Med�� 2011�� 9��suppl 1���� 9.
[9] ABEL S�� RUSSELL D�� WHITLOCK L A�� et al. Assessment of the absorption�� metabolism and absolute bioavailability of maraviroc in healthy male subjects [J]. Br J Clin Pharmacol�� 2008�� 65��suppl 1����60-67.
[10] NOZZA S�� GALLI L�� VISCO F�� et al. Raltegravir�� maraviroc�� etravirine�� an effective protease inhibitor and nucleoside reverse transcriptase inhibitor-sparing regimen for salvage therapy in HIV-infected patients with triple-class experience [J]. AIDS�� 2010�� 24(6)�� 924-928.
[11] TILTON J C�� WILEN C B�� DIDIGU C A�� et al. A maraviroc-resistant HIV-1 with narrow cross-resistance to other CCR5 antagonists depends on both N-terminal and extracellular loop domains of drug-bound CCR5 [J]. J Virol�� 2010�� 84(20)�� 10863-10876.
[12] TAGAT J R�� MCCOMBIE S W�� NAZARENO D�� et al. Piperazine-based CCR5 antagonists as HIV-1 inhibitors. IV. Discovery of 1-[(4��6-dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-[2-methoxy-1(R)-4-(trifluoromethyl)phenyl]ethyl-3(S)-methyl-1-piperaz inyl]- 4-methylpiperidine (Sch-417690/Sch-D)�� a potent�� highly selective�� and orally bioavailable CCR5 antagonist [J]. J Med Chem�� 2004�� 47(10)�� 2405-2408.
[13] SCHURMANN D�� FATKENHEUER G�� REYNES J�� et al. Antiviral activity�� pharmacokinetics and safety of vicriviroc�� an oral CCR5 antagonist�� during 14-day monotherapy in HIV-infected adults [J]. AIDS�� 2007�� 21(10)�� 1293-1299.
[14] GULICK R M�� SU Z�� FLEXNER C�� et al. Phase 2 study of the safety and efficacy of vicriviroc�� a CCR5 inhibitor�� in HIV-1-Infected�� treatment-experienced patients�� AIDS clinical trials group 5211[J]. J Infect Dis�� 2007�� 196(2)�� 304-312.
[15] SULEIMAN J�� ZINGMAN B S�� DIAZ R S�� et al. Vicriviroc in combination therapy with an optimized regimen for treatment-experienced subjects�� 48-week results of the VICTOR-E1 phase 2 trial [J]. J Infect Dis�� 2010�� 201(4)�� 590-599.
[16] ZINGMAN B�� SULEIMAN J�� DEJESUS E�� et al. Vicriviroc�� a next generation CCR5 antagonist�� exhibits potent�� sustained suppression of viral replication in treatment-experienced adults�� VICTOR-E1 48-week results[C]. 15th Conference on Retroviruses and Opportunistic Infections Boston�� MA�� USA�� February 3-6�� 2008�� 39LB.
[17] LENZ J C�� ROCKSTROH J K. Vicriviroc�� a new CC-chemokine receptor 5 inhibitor for treatment of HIV�� properties�� promises and challenges [J]. Expert Opin Drug Metab Toxicol�� 2010�� 6(9)�� 1139-1150.
[18] SETO M�� AIKAWA K�� MIYAMOTO N�� et al. Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents�� synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety [J]. J Med Chem�� 2006�� 49(6)�� 2037-2048.
[19] BABA M�� TAKASHIMA K�� MIYAKE H�� et al. TAK-652 inhibits CCR5-mediated human immunodeficiency virus type 1 infection in vitro and has favorable pharmacokinetics in humans [J]. Antimicrob Agents Chemother�� 2005�� 49(11)�� 4584-4591.
[20] LALEZARI J�� GATHE J�� BRINSON C�� et al. Safety�� efficacy�� and pharmacokinetics of TBR-652�� a CCR5/CCR2 antagonist�� in HIV-1-infected�� treatment-experienced�� CCR5 antagonist-naive subjects [J]. J Acquir Immune Defic Syndr�� 2011�� 57(2)�� 118-125.
[21] STUPPLE P A�� BATCHELOR D V�� CORLESS M�� et al. An imidazopiperidine series of CCR5 antagonists for the treatment of HIV�� The discovery of N-{(1S)-1-(3-fluorophenyl)-3-[(3-endo)-3-(5-isobutyryl-2-methyl-4��5��6��7-tetrahydr o-1H-imidazo[4��5-c]pyridin-1-yl)-8-azabicyclo[3. 2. 1]oct-8-yl]propyl}acetamide (PF-232798) [J]. J Med Chem�� 2011�� 54��1����67-77.
[22] Anti-HIV agents. Is PF-232798 a possible successor to maraviroc? [J]. Treatment Update�� 2008�� 20(2)�� 8.
[23] XUE C-B�� CHEN L�� CAO G�� et al. Discovery of INCB9471�� a potent�� selective�� and orally bioavailable CCR5 antagonist with potent anti-HIV-1 activity [J]. ACS Med Chem Lett�� 2010�� 1(9)�� 483-487.
[24] SHIN N�� SOLOMON K�� ZHOU N�� et al. Identification and characterization of INCB9471�� an allosteric noncompetitive small-molecule antagonist of C-C chemokine receptor 5 with potent inhibitory activity against monocyte migration and HIV-1 infection [J]. J Pharmacol Exp Ther�� 2011�� 338(1)�� 228-239.
[25] MA D�� YU S�� LI B�� et al. Synthesis and biological evaluation of 1��3��3��4-tetrasubstituted pyrrolidine CCR5 receptor antagonists. Discovery of a potent and orally bioavailable anti-HIV agent [J]. Chem Med Chem�� 2007�� 2(2)�� 187-193.
[26] WU W�� XIE D�� CHENG Z�� et al. Determination of nifeviroc�� a novel CCR5 antagonist�� Application to a pharmacokinetic study [J]. J Pharm Biomed Anal�� 2011�� 56(3)�� 637-640.
[27] PETT S L�� MCCARTHY M C�� COOPER D A�� et al. A phase I study to explore the activity and safety of SCH532706�� a small molecule chemokine receptor-5 antagonist in HIV type-1-infected patients [J]. Antivir Ther�� 2009�� 14(1)�� 111-115.
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