A5016741562- HIV/AIDS drug development and treatment
- HIV Research and Treatment
- Click Chemistry and Applications
- Pneumocystis jirovecii pneumonia detection and treatment
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and biological activity
- Biochemical and Molecular Research
- Synthesis and Biological Evaluation
- Quinazolinone synthesis and applications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- HIV/AIDS Research and Interventions
- Hepatitis C virus research
- Chemical Synthesis and Analysis
- DNA and Nucleic Acid Chemistry
- Cytomegalovirus and herpesvirus research
- Carbohydrate Chemistry and Synthesis
- Computational Drug Discovery Methods
- Herpesvirus Infections and Treatments
- Advanced biosensing and bioanalysis techniques
- Synthesis of Organic Compounds
- Synthesis of heterocyclic compounds
- RNA Interference and Gene Delivery
- Crystallography and molecular interactions
- T-cell and Retrovirus Studies
Rega Institute for Medical Research
2016-2025
KU Leuven
2016-2025
Yale University
2022
Fudan University
2003-2022
Shandong University
2008-2020
Duke University
2020
University of North Carolina at Chapel Hill
2020
University of Rostock
2013-2016
University of Perugia
2004-2016
University of Basrah
2011-2013
The interest in the synthesis of Se-containing compounds is growing with discovery derivatives exhibiting various biological activities. In this manuscript, we have identified a series 2,2′-diselenobisbenzamides (DISeBAs) as novel HIV retroviral nucleocapsid protein 7 (NCp7) inhibitors. Because its pleiotropic functions whole viral life cycle and mutation intolerant nature, NCp7 represents target great which not reached by any anti-HIV agent clinical use. Using diselenobisbenzoic scaffold,...
Limited information is available on the activity of anti-retroviral drugs against human immunodeficiency virus type 2 (HIV-2) and simian (SIV) strains to guide their use in treatment or prophylaxis. We evaluated antiviral 16 approved one experimental drug, AMD3100, two wild-type HIV-2 (ROD EHO) isolates, SIV (mac251 B670), simian–human (SHIV) that contain reverse transcriptase (RTSHIV) envelope glycoprotein (SHIV89.6) 1 (HIV-1) a SIV(mac239) background. Drug susceptibility was measured...
New indolylarylsulfone derivatives bearing cyclic substituents at indole-2-carboxamide linked through a methylene/ethylene spacer were potent inhibitors of the WT HIV-1 replication in CEM and PBMC cells with inhibitory concentrations low nanomolar range. Against mutant L100I K103N RT strains MT-4 cells, compounds 20, 24−26, 36, 40 showed antiviral potency superior to that NVP EFV. these strains, equipotent ETV. Molecular docking experiments on this novel series IAS analogues have also...
Natural products represent an inexhaustible source of novel therapeutic agents. Their complex and constrained three-dimensional structures endow these molecules with exceptional biological properties, thereby giving them a major role in drug discovery programs. However, the search for new bioactive metabolites is hampered by chemical complexity matrices which they are found. The purification single constituents from such requires significant amount work that it should be ideally performed...
The emergence of multidrug resistant HIV-1 strains and the inability HAART to eradicate virus from infected patients demand new drugs able interfere with an alternative step replicative cycle. naphthyridone 3 (HM13N), described in present study, is a promising anti-HIV agent due its ability inhibit Tat-mediated transcription potent antiviral activity observed acutely, chronically, latently cells. absence any tendency select for resistance mutations vitro adds potential clinical value this...
Graphene quantum dots (GQD) are the next generation of nanomaterials with great potential in drug delivery and target-specific HIV inhibition. In this study we investigated antiviral activity graphene based by using water-soluble GQD synthesized from multiwalled carbon nanotubes (MWCNT) through prolonged acidic oxidation exfoliation compared their anti-HIV that exerted reverse transcriptase inhibitors (RTI) conjugated same nanomaterial. The antiretroviral agents chosen study, CHI499 CDF119,...
A dynamic G-quadruplex region has been previously shown to form in the long terminal repeat (LTR) promoter of HIV-1 integrated DNA genome. Inhibition activity and antiviral effects have observed when this was stabilized by BRACO-19, a trisubstituted acridine derivative that binds G-quadruplexes. Here, we aimed at characterizing mechanism action BRACO-19 analysing its towards broad range strains, host cells infection modes.The cell lines primary infected or persistently strains evaluated...
We designed and synthesized a series of human immunodeficiency virus type 1 (HIV-1) non-nucleoside reverse transcriptase inhibitors (NNRTIs) with piperidine-substituted thiophene[3,2-d]pyrimidine scaffold, employing strategy structure-based molecular hybridization substituent decorating. Most the compounds exhibited broad-spectrum activity low (single-digit) nanomolar EC50 values toward panel wild-type (WT), single-mutant, double-mutant HIV-1 strains. Compound 27 was most potent; compared...
To address drug resistance to HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel diarylpyrimidine (DAPY) derivatives targeting "tolerant region I" and II" the NNRTIs binding pocket (NNIBP) were designed utilizing structure-guided scaffold-hopping strategy. The dihydrofuro[3,4-d]pyrimidine 13c2 13c4 proved be exceptionally potent against wide range strains carrying single NNRTI-resistant mutations (EC50 = 0.9–8.4 nM), which remarkably superior that etravirine...
Currently, HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a major component of the highly active anti-retroviral therapy (HAART) regimen. However, occurrence drug-resistant strains and adverse reactions after long-term usage have inevitably compromised clinical application NNRTIs. Therefore, development novel with distinct anti-resistance profiles better pharmacological properties is still an enormous challenge. Herein, we summarize state-of-the-art medicinal chemistry...
Ethiopian medicinal plants used for the treatment of a variety ailments including infectious diseases were screened activity against human immunodeficiency virus type 1 (HIV-1) and 2 (HIV-2). Seventy-one polar nonpolar extracts derived from 21 belonging to 14 families tested inhibition viral replication using HIV-1 (IIIB) HIV-2 (ROD) strains. Selective growth was assessed by simultaneous determination in vitro cytotoxicity each MT-4 cells. Six made root bark Bersama abyssinica Fresen, leaves...
Polyanionic dendrimers were synthesized and evaluated for their antiviral effects. Phenyldicarboxylic acid (BRI6195) naphthyldisulfonic (BRI2923) found to inhibit the replication of human immunodeficiency virus type 1 (HIV-1; strain III<sub>B</sub>) in MT-4 cells at a EC<sub>50</sub> 0.1 0.3 μg/ml, respectively. The not toxic up highest concentrations tested (250 μg/ml). These compounds also effective against various other HIV-1 strains, including clinical isolates, HIV-2 simian (SIV,...
Starting from 1H,3H-thiazolo[3,4-a]benzimidazoles (TBZs), we performed the design, synthesis, and structure-activity relationship studies of a series 2,3-diaryl-1,3-thiazolidin-4-ones. Some derivatives proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentrations with minimal cytotoxicity, thereby acting as nonnucleoside RT inhibitors (NNRTIs). Computational were used delineate ligand-RT interactions probe binding ligands RT.