New Advances in the Pharmacological Treatment of Human Immunodeficiency Virus (HIV) Infection: Focus on Protease Inhibitors

1997 ◽  
Vol 10 (1) ◽  
pp. 20-51 ◽  
Author(s):  
Catherine M. Oliphant ◽  
Scott M. Bonnema
Keyword(s):  
Hiv Infection ◽  
Protease Inhibitors ◽  
Factors Affecting ◽  
Hiv Therapy ◽  
New Class ◽  
Complete Knowledge ◽  
Immunodeficiency Virus ◽  
Infection Focus ◽  
Anti Hiv Agents ◽  
Anti Hiv

The introduction of a new class of anti-HIV agents, the protease inhibitors, has given new hope to patients with HIV infection. Use of these agents requires the pharmacist to have a complete knowledge of phar macokinetics, adverse reactions, drug-drug interactions, and resistance profiles. Patient compliance is one of the most important factors affecting the success and failure of protease inhibitor therapy. Pharma cists have the opportunity to positively influence outcomes of HIV therapy.

scholarly journals 3,4-Dihydro-2-Alkoxy-6-Benzyl-4-Oxopyrimidines (DABOs): A New Class of Specific Inhibitors of Human Immunodeficiency Virus Type 1

1993 ◽  
Vol 4 (6) ◽  
pp. 361-368 ◽  
Author(s):  
M. Artico ◽  
S. Massa ◽  
A. Mai ◽  
M. E. Marongiu ◽  
G. Piras ◽  
...  
Keyword(s):  
Methoxy Group ◽  
New Class ◽  
Immunodeficiency Virus ◽  
Alkoxy Groups ◽  
Anti Hiv Agents ◽  
Hydrolysis Of ◽  
Anti Hiv ◽  
Hiv 1 ◽  
Specific Inhibitors

A series of novel 3,4-dihydro-6-benzyl-4-oxopyrimidines substituted at both the C-5 and the C-2 positions were synthesized as potential anti-HIV agents. Preparation of the title compounds was achieved by condensation of O-methylisourea with methyl 2-alkyl-4-phenylacetylacetate and subsequent displacement of the methoxy group by reaction with a series of linear, ramified and cyclic alkoxy groups containing from three to six carbon units. Methyl 2-alkyl-4-phenylacetylacetates were prepared by alkylation of methyl 4-phenylacetylacetate, which was obtained starting from Meldrum's acid and phenacetyl chloride. Acid hydrolysis of 3,4-dihydro-6-benzyl-2-methoxy-4-oxopyrimidines furnished the corresponding 1,2,3,4-tetrahydro-6-benzyl-2,4-dioxopyrimidines. In acutely infected MT-4 cells, compounds 3e, 3o, 3q and 3r showed an anti-HIV-1 activity as potent and/or selective as HEPT and ddl. Unlike HEPT, the replacement of a methyl for an hydrogen atom at position C-5 of 3,4-dihydro-2-alkoxy-6-benzyl-4-oxopyrimidines (DABOs) did not abolish the antiviral activity, as well as the substitution of the C-5 methyl for an ethyl group did not increase the potency. However, similarly to HEPT and its derivatives, DABOs targeted the HIV-1 reverse transcriptase and neither inhibited the multiplication of HIV-2 in acutely infected MT-4 cells, nor that of HIV-1 in chronically infected H9/IIIB cells.

Lazarus and Group Psychotherapy: AIDS in the Era of Protease Inhibitors

2003 ◽  
Vol 31 (3) ◽  
pp. 314-342 ◽  
Author(s):  
George V. Gushue ◽  
Sarah J. Brazaitis
Keyword(s):  
Protease Inhibitors ◽  
Group Process ◽  
Therapy Group ◽  
Immune Deficiency Syndrome ◽  
Deficiency Syndrome ◽  
Hiv And Aids ◽  
Medical Treatments ◽  
New Class ◽  
Immunodeficiency Virus ◽  
Acquired Immune Deficiency

A new class of medications, protease inhibitors, has dramatically improved the health of many people with Human Immunodeficiency Virus (HIV) and Acquired Immune Deficiency Syndrome (AIDS). This development has had a major impact on the lives of those affected by HIV/AIDS. This article considers how a group is affected by the larger systems of which it is a part. The article examines changes in the content, process, and salient leadership tasks of an ongoing therapy group for people with HIV and AIDS before and following the initial introduction of new medical treatments. It also considers how the group process continues to be affected by the more recent failure of these medications for many patients. Implications for research, practice, and training are discussed.

Antimicrobial Peptide, LL-37, And Its Potential As An Anti-HIV Agent

2021 ◽  
Vol 44 (3) ◽  
pp. E64-71
Author(s):  
Ana Vera-Cruz ◽  
Nongnuj Tanphaichitr ◽  
Jonathan B. Angel
Keyword(s):  
Health Impact ◽  
High Rate ◽  
Limited Data ◽  
Inhibitory Effects ◽  
Hiv Replication ◽  
Sexually Transmitted ◽  
Immunodeficiency Virus ◽  
Immunomodulatory Properties ◽  
Anti Hiv Agents ◽  
Anti Hiv

Human immunodeficiency virus (HIV) continues to have a profound global health impact. New infections continue at a high rate despite the development of prophylactic therapies, prompting the need for development of novel preventative approaches. Antimicrobial peptides (AMPs), such as LL-37, display broad microbicidal properties and have potential as anti-HIV agents. LL-37 has been studied for its anti-HIV activity and the limited data available suggest it can inhibit HIV infection in primary T cells as well as exert inhibitory effects on key HIV enzymes. Its immunomodulatory properties may both enhance and inhibit HIV replication. In addition, LL-37 has both 1) the ability to kill other sexually-transmitted pathogens and 2) spermicidal activity; thus, it is a good candidate for multipurpose prevention technology. Further investigation of its anti-HIV activity is warranted.

scholarly journals Potent activity of 2'-beta-fluoro-2',3'-dideoxyadenosine against human immunodeficiency virus type 1 infection in hu-PBL-SCID mice.

1996 ◽  
Vol 40 (10) ◽  
pp. 2369-2374 ◽  
Author(s):  
K Ruxrungtham ◽  
E Boone ◽  
H Ford ◽  
J S Driscoll ◽  
R T Davey ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
T Cells ◽  
Hiv Infection ◽  
Infection Rate ◽  
Cd4 T Cells ◽  
Scid Mice ◽  
Immunodeficiency Virus ◽  
Anti Hiv

A new antiretroviral agent, 2'-beta-fluoro-2',3'-dideoxyadenosine (FddA), is an acid-stable compound whose triphosphate form is a potent reverse transcriptase inhibitor with in vitro anti-human immunodeficiency virus (HIV) activity and a favorable pharmacokinetic profile. Severe combined immunodeficiency (SCID) mice reconstituted with human peripheral blood leukocytes (hu-PBL-SCID mice) provide a useful small-animal model for HIV research. In the present study we utilized this experimental system for the in vivo evaluation of the anti-HIV activity of this new compound when administered prior to infection. Initial studies revealed that, following a challenge with 50 100% tissue culture infective doses of HIV type 1 lymphadenopathy-associated virus, 39 of 42 (93%) control mice developed HIV infection, as evidenced by positive coculture or positive PCR. Administration of zidovudine decreased the infection rate to 5 of 16 (31%), while administration of FddA decreased the infection rate to 0 of 44 (0%). In follow-up controlled studies, the anti-HIV activity of FddA was confirmed, with 18 of 20 control mice showing evidence of HIV infection, compared with 4 of 20 FddA-treated mice. In addition to having direct anti-HIV effects, FddA was found to have a protective effect on human CD4+ T cells in the face of HIV infection. Mice treated with FddA were found to have a significantly higher percentage of CD4+ T cells than controls (10.3% +/- 3.4% versus 0.27% +/- 0.21%; P = 0.01). Thus, FddA, with its potent anti-HIV activity in vivo, high oral bioavailability, long intracellular half-life, and ability to preserve CD4+ cells in the presence of HIV, appears to be a promising agent for clinical investigation.

Synthesis and Antiviral Activity of 1,3-Disubstituted Uracils against HIV-1 and HCMV

2003 ◽  
Vol 14 (5) ◽  
pp. 271-279 ◽  
Author(s):  
Tokumi Maruyama ◽  
Shigetada Kozai ◽  
Tetsuo Yamasaki ◽  
Myriam Witvrouw ◽  
Christophe Pannecouque ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Antiviral Activity ◽  
Human Cytomegalovirus ◽  
Therapeutic Agents ◽  
Reverse Transcriptase Inhibitors ◽  
Uracil Derivatives ◽  
Immunodeficiency Virus ◽  
Anti Hiv Agents ◽  
Anti Hiv ◽  
Hiv 1

The development of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) is an efficient strategy for finding new therapeutic agents against human immunodeficiency virus (HIV). A large number of 6-substituted uracil derivatives have been prepared in order to explore new NNRTIs. However, there are few approaches to anti-HIV agents from 1,3-disubstituted uracil derivatives. Therefore, we tried to prepare several 1,3-disubstituted uracils, which were easily obtainable from uracil by preparation under alkali and Mitsunobu conditions, and examined their antiviral activity against HIV-1 and human cytomegalovirus (HCMV). We found that 1-benzyl-3-(3,5-dimethylbenzyl)uracil and 1-cyanomethyl-3-(3,5-dimethylbenzyl)-4-thiouracil showed powerful inhibition against HCMV and HIV-1, respectively.

Dendronized PLGA nanoparticles with anionic carbosilane dendrons as antiviral agents against HIV infection

RSC Advances ◽  
2016 ◽  
Vol 6 (77) ◽  
pp. 73817-73826 ◽  
Author(s):  
Marta Galán ◽  
Cristina Fornaguera ◽  
Paula Ortega ◽  
Gabriela Calderó ◽  
Raquel Lorente ◽  
...  
Keyword(s):  
Hiv Infection ◽  
Antiviral Agents ◽  
Plga Nanoparticles ◽  
Anti Hiv Agents ◽  
Anti Hiv

PLGA nanoparticles functionalized with carbosilane anionic dendrons have been prepared. The biocompatibility and HIV activity have been explored in PBMC and HEC-1A cells. The results indicate that these systems are powerful anti-HIV agents.

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