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Advances in novel anti-HIV-1 drugs and drug candidates: 2005-2008

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Author:: No author available

Journal Title:: ACTA PHARMACEUTICA SINICA

Issue:: 2

DOI:: No doi available

Key Word:: 艾滋病;HIV-1;药物发现,研究进展;AIDS;HIV-1;drug discovery;review

Abstract： HIV and AIDS remain as the crucial global health concern, therefore, research and development of novel anti-HIV-1 chemical therapeutics is still of paramount significance, which may be illuminated by cases of successful marketed drugs. Herein, we document the discovery and biological profile of new anti-HIV-1 drugs approved by FDA between 2005 and 2008 and some drug candidates are also discussed.

Reference

[1]周春梅,王琳,张铭龙,等.抗人免疫缺陷病毒（HIV）天然产物Calanolide A及其类似物的合成[J].1999,(9).
[2]彭宗根,陈鸿珊,王琳,等.HIV-1逆转录酶抑制剂消旋11-去甲胡桐素A的抗HIV-1活性研究[J].2008,(5).
[3]J Ding,K Das,C Tantillo,etc.Structure of HIV-1 reverse transcriptase in a complex with the non-nucleoside inhibitor α-APA R 95845 at 2.8 å resolution[J].1995,3(4).
[4]Suvit Thaisrivongs,Keith D. Watenpaugh,W. Jeffrey Howe,etc.Structure-Based Design of Novel HIV Protease Inhibitors: Carboxamide-Containing 4-Hydroxycoumarins and 4-Hydroxy-2-pyrones as Potent Nonpeptidic Inhibitors[J].1995,38(18).
[5]Mori J,Rickett G,Armour D,etc.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].2005,49(11).
[6]S M, Poppe,D E, Slade,K T, Chong,etc.Antiviral activity of the dihydropyrone PNU-140690, a new nonpeptidic human immunodeficiency virus protease inhibitor.[J].1997,41.
[7]Duncan Armour,Martin Edwards,Marcel J.de Groot.The Discovery of CCR5 Receptor Antagonists for the Treatment of HIV Infection; Hit-to-Lead Studies[J].2006,1(7).
[8]Cox K,Tagat JR,Nazareno DV,etc.Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-((2,4-dimethyl-3-pyridinyl)carbonyl)-4- methyl-4-(3(S)-methyl-4-(1(S)-(4-(trifluoromethyl)phenyl)ethyl)-1-piperazi nyl)- piperidine N1-oxide (Sch-350634), an orally bioavailabl[J].2001,44(21).
[9]Ghosh AK,Mitsuya H,Chapsal BD,etc.Design of HIV protease inhibitors targeting protein backbone: An effective strategy for combating drug resistance[J].2008,41(1).
[10]A K, Ghosh,W J, Thompson,P M, Fitzgerald,etc.Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran.[J].1994,37(16).
[11]Pacini B,De Francesco R,Nizi E,etc.The monoethyl ester of meconic acid is an active site inhibitor of HCV NS5B RNA-dependent RNA polymerase.[J].2004,14(12).
[12]Rudi Pauwels,Koen Andries,Zeger Debyser,etc.Potent and Highly Selective Human Immunodeficiency Virus Type 1 (HIV-1) Inhibition by a Series of α-Anilinophenylacetamide Derivatives Targeted at HIV-1 Reverse Transcriptase[J].1993,90(5).
[13]A K, Ghosh,J F, Kincaid,D E, Walters,etc.Nonpeptidal P2 ligands for HIV protease inhibitors: structure-based design, synthesis, and biological evaluation.[J].1996,39.
[14]Petrocchi A,Rowley M,Summa V,etc.4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species[J].2006,49(23).
[15].Total Synthesis of (±)-Calanolide a and Its Anti-Hiv Activity[J].1998,(5).
[16]Flexner C.HIV drug development: the next 25 years.[J].2007,6(12).
[17]Kincaid JF,Mitsuya H,Maeda K,etc.Novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI) UIC-94017 (TMC114) with potent activity against multi-PI-resistant human immunodeficiency virus in vitro.[J].2003,47(10).
[18]Greenough TC,Desrosiers RC,Sullivan JL.Declining CD4 T-cell counts in a person infected with nef-deleted HIV-1 (letter)[J].1999,340(3).
[19]Andrea Savarino.A historical sketch of the discovery and development of HIV-1 integrase inhibitors[J].2006,15(12).
[20]Paz OG,Hazuda DJ,Summa V,etc.Discovery of Raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infection[J].2008,51(18).
[21]M A, Navia,P M, Fitzgerald,B M, McKeever,etc.Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1.[J].1989,337(6208).
[22]Tachibana, Kazunobu,Hirota, Seiichi,Iizasa, Hisashi,etc.The chemokine receptor CXCR4 is essential for vascularization of the gastrointestinal tract.[J].1998,393(6685).
[23]Y R, Zou,A H, Kottmann,M, Kuroda,etc.Function of the chemokine receptor CXCR4 in haematopoiesis and in cerebellar development.[J].1998,393(6685).
[24]Frangoise Barre-Sinoussi.HIV: A Discovery Opening the Road to Novel Scientific Knowledge and Global Health Improvement (Nobel Lecture)[J].2009,48(32).
[25]S, Thaisrivongs,H I, Skulnick,S R, Turner,etc.Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.[J].1996,39.
[26]Wai JS,Grobler JA,Felock P,etc.Diketo acid inhibitor mechanism and HIV-1 integrase: Implications for metal binding in the active site of phosphotransferase enzymes.[J].2002,99(10).
[27]J F, Mayaux,A, Bousseau,R, Pauwels,etc.Triterpene derivatives that block entry of human immunodeficiency virus type 1 into cells.[J].1994,91.
[28]M, Samson,F, Libert,B J, Doranz,etc.Resistance to HIV-1 infection in caucasian individuals bearing mutant alleles of the CCR-5 chemokine receptor gene.[J].1996,382.
[29]Wang YF,Amano M,Leschenko S,etc.A novel bis-tetrahydrofuranylurethane-containing nonpeptidic protease inhibitor (PI), GRL-98065, is potent against multiple-PI-resistant human immunodeficiency virus in vitro.[J].2007,51(6).
[30]S, Thaisrivongs,D L, Romero,R A, Tommasi,etc.Structure-based design of HIV protease inhibitors: 5,6-dihydro-4-hydroxy-2-pyrones as effective, nonpeptidic inhibitors.[J].1996,39.
[31]Nguyen BY,Grinsztejn B,Gonzalez CJ,etc.Safety and efficacy of the HIV-1 integrase inhibitor raltegravir (MK-0518) in treatment-experienced patients with multidrug-resistant virus: a phase II randomised controlled trial.[J].2007,369(9569).
[32]Karl, Salzwedel,David E, Martin,Michael, Sakalian.Maturation inhibitors: a new therapeutic class targets the virus structure.[J].1900,9.
[33]Steven Gubernick,lima Yasothan Peter Kirkpatrick,Richard Haubrich.Etravirine[J].2008,7(4).
[34].Randomised trial of addition of lamivudine or lamivudine plus loviride to zidovudine-containing regimens for patients with HIV-1 infection: the CAESAR trial[J].1997,349(9063).
[35]Vincenzo Summa,Licia Tomei,Paola Pace,etc.Discovery of α,γ-Diketo Acids as Potent Selective and Reversible Inhibitors of Hepatitis C Virus NS5b RNA-Dependent RNA Polymerase[J].2004,47(1).
[36]Lee KH,Morris Natschke SL,Qian K.HIV entry inhibitors and their potential in HIV therapy.[J].2009,29(2 TN.7).
[37]YOULA S. TSANTRIZOS.Peptidomimetic Therapeutic Agents Targeting the Protease Enzyme of the Human Immunodeficiency Virus and Hepatitis C Virus[J].2008,41(10).
[38]Napier C,Wood A,Price DA,etc.Overcoming HERG affinity in the discovery of the CCR5 antagonist maraviroc.[J].2006,16(17).
[39]Allaway GP,Smith PF,Forrest A,etc.Phase I and II study of the safety, virologic effect, and pharmacokinetics/pharmacodynamics of single-dose 3-o-(3',3'-dimethylsuccinyl)betulinic acid (bevirimat) against human immunodeficiency virus infection.[J].2007,51(10).
[40]Tie Y,Boross PI,Leshchenko S,etc.High Resolution Crystal Structures of HIV-1 Protease with a Potent Non-peptide Inhibitor (UIC-94017) Active Against Multi-drug-resistant Clinical Strains.[J].2004,338(2).
[41]Toshihiro Fujioka,Yoshiki Kashiwada,Robert E. Kilkuskie,etc.Anti-AIDS Agents, 11. Betulinic Acid and Platanic Acid as Anti-HIV Principles from Syzigium claviflorum, and the Anti-HIV Activity of Structurally Related Triterpenoids[J].1994,57(2).
[42]Li CB.,Fridell R.,Meanwell N.,etc.A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding[J].2003,100(19).
[43]Muzammil S,Armstrong AA,Kang LW,etc.Unique thermodynamic response of tipranavir to human immunodeficiency virus type 1 protease drug resistance mutations[J].2007,81(10).
[44]Clader JW,Endres M,Palani A,etc.Discovery of 4-((Z)-(4-bromophenyl)- (ethoxyimino)methyl)-1'-((2,4-dimethyl-3- pyridinyl)carbonyl)-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.[J].2001,44(21).
[45]Yoel Kashman,Kirk R. Gustafson,Richard W. Fuller,etc.HIV inhibitory natural products. Part 7. The calanolides, a novel HIV-inhibitory class of coumarin derivatives from the tropical rainforest tree, Calophyllum lanigerum[J].1992,35(15).
[46]S, Thaisrivongs,P K, Tomich,K D, Watenpaugh,etc.Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors.[J].1994,37(20).
[47]Reyes GR,Xu S,Baroudy BM,etc.Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1.[J].2005,49(12).
[48]H I, Skulnick,P D, Johnson,W J, Howe,etc.Structure-based design of sulfonamide-substituted non-peptidic HIV protease inhibitors.[J].1995,38(26).
[49]Rudi Pauwels,Marie-Pierre de Béthune,Koen Andries,etc.Discovery, Development and Characterization of Agents Active Against the Aids Virus[J].1995,15(1-4).
[50]F, Soler,C, Poujade,M, Evers,etc.Betulinic acid derivatives: a new class of specific inhibitors of human immunodeficiency virus type 1 entry.[J].1996,39.
[51]Turner SR,Strohbach JW,Tommasi RA,etc.Tipranavir (PNU-140690): a potent, orally bioavailable nonpeptidic HIV protease inhibitor of the 5,6-dihydro-4-hydroxy-2-pyrone sulfonamide class.[J].1998,41(18).
[52]Al-Mawsawi LQ,Neamati N,Gundla R,etc.HIV-1 integrase inhibitors: 2005-2006 update.[J].2008,28(1).
[53]A. Castillo,J. M. Orenstein,R. Goila-Gaur,etc.PA-457: A potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing[J].2003,100(23).
[54]Sepkowitz KA.AIDS--the first 20 years.[J].2001,344(23).
[55]M T, Flavin,J D, Rizzo,A, Khilevich,etc.Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers.[J].1996,39.