Anti-Human immunodeficiency virus

Chen CH, Vazquez-Padua M et al (1991) Effect of anti-human immunodeficiency virus nucleoside analogs on mitochondrial DNA and its implication for delayed toxicity. Mol Pharmacol 39(5) 625-628... 

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. Anti-microb Agents Chemother 2005 49(l 1 ) 4721 —4732. 

Nakashima H, Masuda M, Murakami T, Koyanagi Y, Matsumoto A, Fujii N, Yamamoto N. Anti-human immunodeficiency virus activity of a novel synthetic peptide, T22 ([Tyr-5,12,Lys-7]polyphemusin II) a possible inhibitor of virus-cell fusion. Antimicrob Agents Chemother 1992 36 1249 — 1255. 

Jansen RW, Molema G, Pauwels R, Schols D, De Clercq E, Meijer DKF. Potent in vitro anti-human immunodeficiency virus-1 activity of modified human serum albumins. Mol Pharmacol 1991 39 818-823. 

Balzarini J, Hao Z, Herdewijn P, Johns DG, De Clercq E. Intracellular metabolism and mechanism of anti-retrovirus action of 9-(2-phosphonylme-thoxyethyl)adenine, a potent anti-human immunodeficiency virus compound. Proc Natl Acad Sci USA 1991 88 1499-1503. 

In addition, new some epoxide hydrolases have also shown a great utility for the desymmetrization of meso-epoxides. An interesting example is the synthesis of nelfinavir-the active pharmaceutical ingredient (API) of the anti-human immunodeficiency virus drug Viracept-where the (R,R)-diol obtained by opening the meso-epoxide is a suitable starting material. Scheme 10.6 shows a synthetic route to nehinavir [14]. 

An efficient synthesis of the l-aUyl-6-(l, 2, 3 -triazolyl) analogue 170 of 1-[2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (KEPT), an anti-human immunodeficiency virus (HIV) reverse transcriptase inhibitor, was reported using an intermolecular 1,3-dipolar cycloaddition of the azide 169 with acetylenes (35) (Scheme 9.35). Azidouracil (169), when refluxed with an acetylene in equimolar proportions in toluene, gave the corresponding triazoles (170) in excellent yield. 

Pontzer CH, Yamamoto JK, Bazer FW, Ott TL, Johnson HM. Potent anti-feline immunodificiency virus and anti-human immunodeficiency virus effect of interferon tau. J Immunol 1995 (in press). 

Domsife RE, St. Clair MH, Huang AT, Panella TJ, Koszalka GW, Burns CL, et al. Anti-human immunodeficiency virus synergism by zidovudine (3 -azidothymi... 

Future Anti-Human Immunodeficiency Virus Drugs Under Development... 

Fujihashi T, Hara H, Sakata T, Mori K, Higuchi H, Tanaka A, Kaji H, Kaji A (1995) Anti-Human Immunodeficiency Virus (HIV) Activities of Halogenated Gomisin J Derivatives, New Nonnucleoside Inhibitors of HIV Type 1 Reverse Transcriptase. Antimicrob Agents Chemother 39 2000... 

Giordano, V., Jin, D.Y., Rekosh, D. and Jeang, K.T. (2000) Intravirion targeting of a functional anti-human immunodeficiency virus ribozyme directed to pol. Virology, 267, 174-184. 

R. W. Jansen, D. Schols, R. Pauwels, E. De Clercq, and D. K. F. Meijer, Novel, negatively charged, human serum albumins display potent and selective in vitro anti-human immunodeficiency virus type 1 activity, Mol. Pharmacol. 44 1003-1007 (1993). 

This methodology has been applied to the synthesis of the dihydropyran portion 32 of tipranavir (33), an anti-human immunodeficiency virus compound (Scheme 28.23).56-70 The dihydropyran 32 can be accessed from the cyclopentene 34 by what is formally a tandem AROM/RCM reaction. 

Huang, L. Yuan, X. Aiken, C. Chen, C. H. Bifunctional anti-human immunodeficiency virus t3fpe 1 small molecules with two novel mechanisms of action. Antimicrob. Agents Chemother, 2004, 48 663—665. 

Dalod M, Dupuis M, Deschemin JC, Sicard D, Salmon D, Delfraissy JF, Venet A, Sinet M, Guillet JG (1999) Broad, intense anti-human immunodeficiency virus (HIV) ex vivo CD8(-i-) responses in HIV type 1-infected patients Comparison with anti-Epstein-Barr virus responses and changes during antiretroviral therapy. J Virol 73 7108-7116. 

Zink MC, Uhrlaub J, De Witt J, VoeUcer T, Bullock B, Mankowski J, TArwater P, Clements J, Barber S (2005) Neuroprotective and anti-human immunodeficiency virus activity of minocycline. JAMA 293 2003-2011. 

Curdlan, which is a linear (1—> 3)-/3-D-glucan (O Scheme i), also suppresses the proliferation of subcutaneously implanted sarcoma 180 markedly [7]. Curdlan sulfate with a high degree of suhstitution (O Scheme 4) is reported to exert strong anti-human immunodeficiency virus (anti-HIV) activity [8,9]. 

Sato, Y., Utsumi, K., Maruyama, T., et al. (1994) Synthesis and hypnotic and anti-human immunodeficiency virus-1 activities of -Substituted 2 -Deoxy-2 -fluorouridines. Chem. Pharm. Bull., 42, 595-598. 

Soudeyns, H., Yao, X.-J., Gao, Q., Belleau, B., Kraus, J.-L., Nguyen-Ba, N., Spira, B., and Wainberg, M. A. (1991) Anti-human immunodeficiency virus type 1 activity and in vitro toxicity of 2 -deoxy-3 -thiacytidine (BCH-189), a novel heterocyclic nucleoside analog. Antimicrob. Agents Chemother. 35, 1386-1390. 

Pincus, S. H. and Tolstikov, V. V. (1995) Anti-human immunodeficiency virus immunoconjugates. Adv. Pharmacol. 32, 205-242. 

Erice, A., Balfour, H. H., Jr., Myers, D. E., Leske, V. L., Sannerud, K. J., Kuebelbeck, V., Irvin, J. D., and Uckun, F. M. (1993) Anti-human immunodeficiency virus type 1 activity of an anti-CD4 immunoconjugate containing pokeweeci antiviral protein. Antimicrob. Agents Chemother. 37, 835-338. 

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