Thiated Analogues of 2′,3′-Dideoxy-3′-fluorothymidine and Their Phosphorylated and Phosphonylated Derivatives: Synthesis, Interaction with HIV Reverse Transcriptase, and in vitro anti-HIV Activity

ChemInform ◽  
2004 ◽  
Vol 35 (5) ◽  
Author(s):  
A. Miazga ◽  
K. Felczak ◽  
M. Bretner ◽  
M. A. Siwecka ◽  
A. Piasek ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Hiv Reverse Transcriptase ◽  
Anti Hiv

scholarly journals EFFECT OF FREE ALKALOID AND NON-FREE ALKALOID ETHANOL 70% EXTRACT OF JUSTICIA GENDARUSSA BURM F. LEAVES AGAINST REVERSE TRANSCRIPTASE HIV ENZYME IN VITRO AND CHEMICAL COMPOUND ANALYSIS

2016 ◽  
Vol 6 (1) ◽  
pp. 1
Author(s):  
Bambang Prajogo ◽  
Prihartini Widiyanti ◽  
Hafrizal Riza
Keyword(s):  
High Performance Liquid Chromatography ◽  
Liquid Chromatography ◽  
Reverse Transcriptase ◽  
Retention Time ◽  
High Performance ◽  
Hiv Reverse Transcriptase ◽  
Reverse Transcriptase Enzyme ◽  
Anti Hiv ◽  
Hiv Aids

HIV-AIDS is a global problem and the deadliest disease in the world. One of HIV and AIDS prevention strategy can be done with traditional medicine research program from natural resource that has anti-HIV AIDS activity. It has been found that 70% ethanol extract of Justicia gendarussa Burm.f leaves, alkaloid free and alkaloid non-free, has a strong inhibitory activity against HIV reverse transcriptase enzyme, as an effort to find a solution in the face of HIV AIDS prevalence that is still high with problem of HIV-AIDS treatment such as side effects and resistances. Justicia gendarussa had already known for having an effect anti-HIV and therefore we were looking at the mechanism of inhibition of HIV Reverse Transcriptase enzyme. Both types of extracts were tested in vitro using ELISA technique and analysed chemical content of Gendarusin A as anti-HIV using high performance liquid chromatography. ELISA test results obtained percent inhibition, respectively for 254.2, 254.2, 235.6, and 279.7 for the concentration of 5 ppm, 10 ppm, 15 ppm and 20 ppm of free alkaloid extract and 169.0, 164.0, 130.5 and 369.5 for the concentration of 5 ppm, 10 ppm, 15 ppm and 20 ppm of non-free-alkaloid extract. The results of high performance liquid chromatography obtained Gendarusin A in the free-alkaloid extract at retention time 8.402 minutes and non-free alkaloid extract at retention time 8.381. Therefore, these results concluded that the Justicia gendarussa Burm.f can be a useful resource for the isolation and development of new anti-HIV.

scholarly journals Fullerene Derivatives of Nucleoside HIV Reverse Transcriptase Inhibitors—In Silico Activity Prediction

2018 ◽  
Vol 19 (10) ◽  
pp. 3231 ◽  
Author(s):  
Aleksandra Dąbrowska ◽  
Tomasz Pieńko ◽  
Przemysław Taciak ◽  
Katarzyna Wiktorska ◽  
Zdzisław Chilmonczyk ◽  
...  
Keyword(s):  
Reverse Transcriptase ◽  
Hiv Reverse Transcriptase ◽  
Reverse Transcriptase Inhibitors ◽  
Activity Prediction ◽  
Hiv Therapy ◽  
C20 Fullerene ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Similar Affinity ◽  
Hiv 1

Here we present new derivatives of nucleoside reverse transcriptase inhibitors with a C20 fullerene. The computational chemistry methods used in this study evaluate affinity of designed compounds towards the HIV-1 reverse transcriptase (RT) binding site and select the most active ones. The best of the designed compounds have superior or similar affinity to RT active site in comparison to most active test compounds, including drugs used in anti-HIV therapy.

An Approach towards the Synthesis of Potential Metal-Chelating TSAO-T Derivatives as Bidentate Inhibitors of Human Immunodeficiency virus Type 1 Reverse Transcriptase

1998 ◽  
Vol 9 (5) ◽  
pp. 412-421 ◽  
Author(s):  
C Chamorro ◽  
M-J Camarasa ◽  
M-J Pérez-Pérez ◽  
E de Clercq ◽  
J Balzarini ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Reverse Transcriptase ◽  
Human Immunodeficiency Virus Type ◽  
Virus Type ◽  
Parent Compound ◽  
Immunodeficiency Virus ◽  
Anti Hiv ◽  
Hiv 1

Novel derivatives of the potent human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) inhibitor TSAO-T have been designed, synthesized and tested for their in vitro antiretro-viral activity against HIV. These TSAO-T derivatives have been designed as potential bidentate inhibitors of HIV-1 RT, which combine in their structure the functionality of a non-nucleoside RT inhibitor (TSAO-T) and a bivalent ion-chelating moiety (a β-diketone moiety) linked through an appropriate spacer to the N-3 of thymine of TSAO-T . Some of the new compounds have an anti-HIV-1 activity comparable to that of the parent compound TSAO-T, but display a markedly increased antiviral selectivity. There was a clear relationship between antiviral activity and the length of the spacer group that links the TSAO molecule with the chelating moiety. A shorter spacer invariably resulted in increased antiviral potency. None of the TSAO-T derivatives were endowed with anti-HIV-2 activity.

EVALUATION OF SOME MEDICINAL PLANTS AS PUTATIVE HIV-PROTEASE INHIBITORS

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (06) ◽  
pp. 24-28
Author(s):  
A.A Rege ◽  
◽  
A. S Chowdhary
Keyword(s):  
Inhibitory Activity ◽  
In Vitro Study ◽  
Hiv Protease ◽  
Tinospora Cordifolia ◽  
Ocimum Sanctum ◽  
Hiv Protease Inhibitors ◽  
Hiv Reverse Transcriptase ◽  
Anti Hiv ◽  
Potent Inhibitory Activity

Aqueous extracts of Ocimum sanctum Linn., Tinospora cordifolia (Willd.) Miers ex Hook. f. & Thoms, Withania somnifera Dunal, Avicennia officinalis Linn. and Rhizophora mucronata Lam. were included for the present in vitro study. Pepsin was used as a substitute for HIV-protease to evaluate inhibitory activity of these extracts, as pepsin has close resemblance with HIV-protease in proteolytic activity. O. sanctum revealed the highest inhibitory activity followed by R. mucronata. In our earlier study, O. sanctum and R. mucronata exerted anti-HIV activity via multiple mechanisms of action; viz., interference with the gp120 / CD4 interaction and inhibition of HIV-reverse transcriptase. In the present study, they also showed potent inhibitory activity against pepsin enzyme (indirectly against HIV-protease) which may be due their flavonoids content.

Sensitivity of V75I HIV-1 reverse transcriptase mutant selected in vitro by acyclovir to anti-HIV drugs

AIDS ◽  
2010 ◽  
Vol 24 (2) ◽  
pp. 319-323 ◽  
Author(s):  
Moira A McMahon ◽  
Janet D Siliciano ◽  
Rahul M Kohli ◽  
Robert F Siliciano
Keyword(s):  
Reverse Transcriptase ◽  
Hiv Drugs ◽  
Anti Hiv ◽  
Hiv 1

scholarly journals In Vitro Antiviral Activity of the Novel, Tyrosyl-Based Human Immunodeficiency Virus (HIV) Type 1 Protease Inhibitor Brecanavir (GW640385) in Combination with Other Antiretrovirals and against a Panel of Protease Inhibitor-Resistant HIV

2007 ◽  
Vol 51 (9) ◽  
pp. 3147-3154 ◽  
Author(s):  
Richard Hazen ◽  
Robert Harvey ◽  
Robert Ferris ◽  
Charles Craig ◽  
Phillip Yates ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Antiviral Activity ◽  
Protease Inhibitor ◽  
Reverse Transcriptase ◽  
In Vitro Assays ◽  
Immunodeficiency Virus ◽  
Anti Hiv ◽  
Hiv 1

ABSTRACT Brecanavir, a novel tyrosyl-based arylsulfonamide, high-affinity, human immunodeficiency virus type 1 (HIV-1) protease inhibitor (PI), has been evaluated for anti-HIV activity in several in vitro assays. Preclinical assessment of brecanavir indicated that this compound potently inhibited HIV-1 in cell culture assays with 50% effective concentrations (EC50s) of 0.2 to 0.53 nM and was equally active against HIV strains utilizing either the CXCR4 or CCR5 coreceptor, as was found with other PIs. The presence of up to 40% human serum decreased the anti-HIV-1 activity of brecanavir by 5.2-fold, but under these conditions the compound retained single-digit nanomolar EC50s. When brecanavir was tested in combination with nucleoside reverse transcriptase inhibitors, the antiviral activity of brecanavir was synergistic with the effects of stavudine and additive to the effects of zidovudine, tenofovir, dideoxycytidine, didanosine, adefovir, abacavir, lamivudine, and emtricitabine. Brecanavir was synergistic with the nonnucleoside reverse transcriptase inhibitor nevirapine or delavirdine and was additive to the effects of efavirenz. In combination with other PIs, brecanavir was additive to the activities of indinavir, lopinavir, nelfinavir, ritonavir, amprenavir, saquinavir, and atazanavir. Clinical HIV isolates from PI-experienced patients were evaluated for sensitivity to brecanavir and other PIs in a recombinant virus assay. Brecanavir had a <5-fold increase in EC50s against 80% of patient isolates tested and had a greater mean in vitro potency than amprenavir, indinavir, lopinavir, atazanavir, tipranavir, and darunavir. Brecanavir is by a substantial margin the most potent and broadly active antiviral agent among the PIs tested in vitro.

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