Anti-human immunodeficiency virus agent

Balzarini J, Naesens L, Herdewijn P, Rosenberg I, Holy A, Pauwels R, Baba M, Johns DG, De Clercq E. Marked in vivo antiretrovirus activity of 9-(2-phosphonylmcthoxycthyljadcninc, a selective anti-human immunodeficiency virus agent. Proc Natl Acad Sci USA 1989 86 332-336. 

Ray AS, Vela JE, Boojamra CG, Zhang L, Hui H, Callebaut C, Stray K, Lin KY, Gao Y, Mackman RL et ai (2008) Intracellular metabolism of the nucleotide prodrug GS-9131, a potent anti-human immunodeficiency virus agent. Antimicrob Agents Chemother 52 648-654... 

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. 

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... 

Hydrolysis of the diastereoisomerically pure Strecker product under racemization-free acidic conditions, followed by hydrogenolysis of the benzylic C-N bond, results in a 73% overall yield of (S)-tert-leucine (11). The amino acid 11 is an interesting, sterically constrained amino acid that is applied in various new antiviral and anti-HIV (human immunodeficiency virus) agents. 

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. 

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. 

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. 

Further, the research and development of anticancer drug 335, anti-human immunodeficiency virus (anti-HIV) agent 336 (Figure 21) <2004SOS(17)357>, and antibacterial sulfonamides <2005EJM377> have been reported. 

Datema, R., Rabin, L., Hincenbergs, M., Moreno, M. B., Warren, S., Linquist, V., Rosenwirth, B., Seifert, J., and McCune, J. M. (1996) Antiviral efficacy in vivo of the anti-human immunodeficiency virus bicyclam SDZ SID 791 (JM 3100), an inhibitor of infectious cell entry. Antimicrobial Agents and Chemotherapy 40,750-754. 

Soudeyns H, Yao Xj, Gao Q, Belleau B, Kraus JL, Nguyen-Ba N, Spira B. Wainberg M. Anti-human immunodeficiency virus Type 1 activity and m vitro toxicity of 2 -deoxy-3 -thiacyti dine (BCHI89), a novel heterocyclic nucleoside analogue. Antimicrob Agents Chemocher 1991 35 1386-1390. 

Shah V, Doncel GF, SeyoumT, Eaton KM, Zalenskaya 1, Hagver R, et al. Sophorolipids, microbial gly-cohpids with anti-human immunodeficiency virus and sperm-immobilizing activities. Antimicrob Agents Chemother 2005 49 4093-100. 

Gosselin G, Schinazi RE, Sommadossi JP, Mathi C, Bergogne MC, Aubertin AM, Kim A, Imbach JL (1994) Anti-human immunodeficiency virus activities of the 1-1 enantiomer of 2, 3 -dideoxycytidine and its 5-fluoro derivative in vitro. Antimicrob Agents Chemother... 

Daluge, S.M. Good, S.S. Paletto, M.B. Miller, W.H. St.Clair, M.H. Boone, L.R. Tisdale, M. Parry, N.R. Reardon, J.E. Domsife, R.E. Averett, D.R. Krenitsky, T.A. 1592U89, a novel carbocyclic nucleoside analog with potent, selective anti-human immunodeficiency virus activity, Antimicrob.Agents Chemother., 1997,41, 1082-1093. 

Cundy, K.C. Sueoka, C. Lynch, G.R. Griffin, L. Lee, WJl. Shaw, J.-P. Pharmacokinetics and bioavailability of the anti-human immunodeficiency virus nucleotide analog 9-[(R)-2-(phosphonomethoxy)-propyl]adenine (PMPA) in dogs, Antimicrob.Agents Chemother., 1998, 42, 687-690. [derivatization adefovir is internal standard fluorescence detection LOQ 25 ng/mL tenofovir only]... 

The rapid spread of acquired immune deficiency syndrome (AIDS) has prompted numerous efforts to develop therapeutic agents against the human immunodeficiency virus type 1 (HIV-1) [2351. Efforts have focused on inhibition of the virally encoded reverse transcriptase (RT) enzyme, which is responsible for the conversion of retroviral RNA to proviral DNA. The nucleoside RT inhibitors 3 -azidothymidine (AZT) and dideoxyinosine (ddl) have proven to be clinically useful anti HIV-1 agents [236], but due to their lack of selectivity versus other DNA polymerases, these compounds are flawed by their inherent toxi-... 

Furoannelated analogs of uracil acyclic nucleosides were prepared as compounds with potential as anti-HIV agents (HIV = human immunodeficiency virus). Hence, 6-benzyluracil 320 is converted to the precursor 321 first by hydroxymethylation, silylation in situ with bis(trimethylsilyl)acetamide (BSA), then by alkylation (Scheme 28) <2001S559>. Ring closure to 322 was effected by treatment with lead tetraacetate and calcium carbonate <2004AP148>. 

A group of substituted pyrrole derivatives, in particular compounds 34 and 35, are of considerable interest as novel human immunodeficiency virus (HIV) type 1 entry inhibitors that interfere with the gp41 stK-helix bundle formation and block virus fusion. They are under scrutiny as novel anti-HIV agents <2004AAC4349>. 

Thiazolidines are also known to selectively intercept the biochemical processes of the pathogenic organisms such as bacteria, virus, and fungi, in the host species. Thiazolidines introduction into the HIV/AIDS (Human Immunodeficiency Virus/Acquired Immune Deficiency Syndrome) therapy is due to l-aryl-lff,3ff-thiazolo[3,4-a]benzimidazole (TBZ) analogues (Fig. 26). Barreca et al. have modified the TBZ by opening its B ring to explore the thiazolidines namely 2-(2,6-dihalo phenyl)-3-(substituted pyridin-2-yl)-thiazolidin-4-ones (Table 16) as potential anti-HIV-1 RT agents [173]. 

Another therapeutic application of polyhydroxylated alkaloids is as anti-viral agents. Inhibitors of processing a-glucosidases, such as castanospermine and DNJ, have been shown to decrease the infectivity of human immunodeficiency virus (HIV) in vitro at concentrations which are not cytotoxic to lymphocytes, whereas specific inhibitors of processing a-mannosidases (swainsonine and 1-deoxymannojirimycin) have no effect on Castanospermine and DNJ also reduce the infectivity of other retroviruses... 

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