Abstract:
BACKGROUND:The emergence of drug-resistant viral strains has created the need for the development of novel anti-HIV agents with a diverse structure that targets key enzymes in the HIV lifecycle. OBJECTIVE:Considering the pharmacophore of integrase inhibitors, one of the validated targets for anti-HIV therapy, we designed a quinazolinone incorporated coumarin scaffold to affect HIV. METHODS:Coumarin is a beta enol ester and also a well-known drug scaffold. Designed structures were prepared using a one-pot three-component reaction from 3-amino-4-hydroxycoumarin, isatoic anhydride and benzaldehyde derivatives. RESULTS:In vitro anti-HIV and cytotoxicity assay indicated that more than half of the compounds had EC50 values lower than 50 µM. Unsubstituted phenyl derivative showed the highest activity and selectivity with an EC50 value of 5 µM and a therapeutic index of 7. Compounds were docked into the integrase active site to investigate the probable mechanism of action. Accordingly, the hydroxyl moiety of coumarin along with the carbonyl of the quinazolinone ring could function as the metal chelating group. Quinazolinone and phenyl groups interact with side chains of IN residues, as well. CONCLUSION:Here, a novel anti-HIV scaffold is represented for further modification and in-vivo studies.
journal_name
Curr HIV Resjournal_title
Current HIV researchauthors
Safakish M,Hajimahdi Z,Aghasadeghi MR,Vahabpour R,Zarghi Adoi
10.2174/1570162X17666191210105809subject
Has Abstractpub_date
2020-01-01 00:00:00pages
41-51issue
1eissn
1570-162Xissn
1873-4251pii
CHR-EPUB-102870journal_volume
18pub_type
杂志文章abstract:PURPOSE:Switch to unboosted atazanavir (ATV) is an attractive option due to convenience and tolerability in HIV-positive patients. With limited available data we investigated the determinants of long-term efficacy and the consequences of virological failure of unboosted atazanavir-based regimens. METHODS:Retrospective...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162x12666140807151616
更新日期:2014-01-01 00:00:00
abstract::Most of the HIV-infected long term survivors show strong CD8+ cell noncytotoxic antiviral response (CNAR) that plays as an important factor for maintaining the relative healthy state of infected individuals. HIV infected former blood donors (FBDs) in Anhui, China are the unique population that considered infected by t...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016209788680561
更新日期:2009-07-01 00:00:00
abstract::It has been known for decades that exogenous RNAs are able to induce cytotoxic T lymphocytes (CTLs) and immunological reactivity to a wide variety of antigens. The molecular events responsible for these effects remain unclear for more than two decades. It has been decided to revisit this phenomenon in the light of new...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016205774370447
更新日期:2005-10-01 00:00:00
abstract:BACKGROUND:Suboptimal adherence to antiretroviral therapy (ART) is a strong predictor of virologic failure (VF) among people with HIV. Various methods such as patient self-report, pill counts and pharmacy refills have been utilized to monitor adherence. However, there are limited data on the accuracy of combining metho...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162x1205141121102501
更新日期:2014-01-01 00:00:00
abstract::The aim of the study was to report the epidemiological profile of HIV-1 positive patients from, Istanbul, Turkey, which has one of the lowest HIV-1/AIDS prevalences in Europe. The patients were followed by ACTHIV-IST group which was established by the Infectious Diseases Departments of five teaching hospitals (three u...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162x12666140411111803
更新日期:2014-01-01 00:00:00
abstract::Opioid use in HIV infection has been associated with an increased frequency of neurological disease and cognitive impairment and vitamin A deficiency has been linked to progressive HIV disease in drug users. In this report the potential effects of these factors, alone and in combination, on gamma amino butyric acid (G...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016212802138715
更新日期:2012-07-01 00:00:00
abstract::An estimated 800,000 children acquired HIV-infection in 2002, most as a result of mother-to-child transmission (MTCT), and vertically-acquired HIV infection continues to be of major public health importance. Prevention of MTCT is possible with a combination of interventions including antiretroviral therapy (ART) (usua...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162033485140
更新日期:2003-10-01 00:00:00
abstract::Antigenic variation, which is the result of amino acid substitution and genetic evolution, poses a major challenge in the development of vaccines against pathogens with unstable genomes, such as HIV-1 and Influenza. Thus, it is highly important to characterize the relationship of genetic evolution, antigenic variation...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016207779316305
更新日期:2007-01-01 00:00:00
abstract::To assess the correlation between HIV-1 RNA load in blood and semen by antiretroviral therapy status and the relative penetration of antiretroviral drugs in seminal plasma. We performed a cross-sectional cohort study of 119 HIV-1 subjects divided into three groups according to treatment status. Blood and semen were co...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016208785861177
更新日期:2008-09-01 00:00:00
abstract:BACKGROUND:Over the years, numerous studies have been carried out demonstrating the role of antibodies in HIV control leading to the development of antibody-based therapeutic and prophylactic strategies. OBJECTIVE:The objective of this review is to provide updated information on the role of antibodies in the preventio...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162x14999160224103320
更新日期:2016-01-01 00:00:00
abstract:BACKGROUND:Human milk banking has been promoted to provide donated breast milk for at-risk children whose mothers cannot breastfeed them but this effort was hindered by the advent of HIV epidemic. OBJECTIVE:To estimate the seroprevalence of HIV, syphilis and hepatitis B in the blood of human milk donors registered in ...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X15666170707143541
更新日期:2017-01-01 00:00:00
abstract::Passive immunization studies in non-human primates have established unequivocally that virus neutralization can prevent infection, providing the impetus for current intense efforts to identify immunogens that elicit broadly neutralizing antibodies in humans. Although Fc-mediated effector function may also contribute t...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162x113116660060
更新日期:2013-07-01 00:00:00
abstract::Enteroaggregative Escherichia coli (EAEC) have been isolated from both HIV-positive and non-HIV diarrheal samples. In this study a collection of 18 isolates from these two groups were compared for biofilm formation and antibiotic resistance and for the presence of 14 virulence-related genes. All the HIV-positive and o...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162x12666140207161000
更新日期:2013-12-01 00:00:00
abstract:BACKGROUND:Cytokines have been widely demonstrated to involve in the pathogenesis of AIDS and the mechanisms of antiretroviral therapy. Interleukin 27 (IL-27) is a new member of the IL-12 cytokine family and has been shown to interfere HIV-1 virus replication with controversial findings. This study is to investigate th...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X15666170517130339
更新日期:2017-01-01 00:00:00
abstract::After the infusion of HIV-1 virus into a host cell, RNA is reverse transcribed to dsDNA, which persists intracellular to the infected cell in a variety of forms. Numerous in-house assays have been developed for the quantification of the different cellular HIV-1 DNA forms; these implement conventional or real-time PCR ...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016209788348001
更新日期:2009-05-01 00:00:00
abstract:BACKGROUND:Although HIV and injury contribute substantially to disease burdens in lowand middle-income countries (LMIC), their intersection is poorly characterized. OBJECTIVE:This systematic review assessed the prevalence and associated mortality impact of HIVseropositivity among injured patients in LMIC. METHODS:A s...
journal_title:Current HIV research
pub_type: 杂志文章,meta分析,评审
doi:10.2174/1570162X15666170920112743
更新日期:2017-11-23 00:00:00
abstract::Recently, a mechanism of negative regulation of immune responses by a specialized population of so-called regulatory T cells (Tregs) has become a focus of intense investigation. Through the discovery of transcription factor Foxp3 as a central molecular determinant of Tregs differentiation and function, the complex bio...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016210791208613
更新日期:2010-06-01 00:00:00
abstract:BACKGROUND:China has implemented a nation-wide policy to control mother-to-child transmission (MTCT) of the human immunodeficiency virus (HIV) since 2011, yet the efficacy of the control policy is less studied. The aim of the present study was to report the data in the prevention of MTCT of HIV in Nantong city, China. ...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X18666200810134025
更新日期:2020-01-01 00:00:00
abstract:OBJECTIVE:There is scarce information about the molecular epidemiology of HIV-infection in Armenia (former USSR). The objective of this work was to estimate the distribution of HIV-1 subtypes in this country and get any information about HIV drug resistance in naÏve patients. DESIGN:A joint study involving 78 patients...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162x13666150407142834
更新日期:2015-01-01 00:00:00
abstract::The development of pre-exposure prophylactics or microbicide products for the reduction or elimination of the sexual transmission of HIV has numerous challenges or barriers to success. Historically traditional dosage forms such as gels have been developed in the field but more recently controlled release dosage forms ...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016212799304599
更新日期:2012-01-01 00:00:00
abstract::A current debate in the HIV-1 vaccine field concerns the ability of an immunodeficiency virus to elicit a protective response. One argument is that HIV-1 superinfections are frequent in healthy individuals, because virus evades conventional immune surveillance, a serious obstacle to vaccine design. The opposing argume...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016209789346255
更新日期:2009-09-01 00:00:00
abstract::Beta defensins are antimicrobial peptides that serve to protect the host from microbial invasion at skin and mucosal surfaces. Here we explore the relationships among beta defensin levels, total bacterial colonization, and colonization by bacterial vaginosis (BV)-related bacteria and lactobacilli in the female genital...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016212802429848
更新日期:2012-09-01 00:00:00
abstract::In HIV-1, tRNA(Lys3) serves as the primer for reverse transcriptase, and during viral assembly, the tRNA(Lys) isoacceptors, tRNA(Lys1,2) and tRNA(Lys3), are selectively packaged into the virion. In this review, we shall first discuss the evidence for the formation of a tRNA(Lys) packaging complex, whose components inc...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162043484988
更新日期:2004-04-01 00:00:00
abstract::According to the World Health Organization's 2007 estimates, close to 33 million people worldwide are living with HIV/AIDS. Over the past two decades, significant progress has been made in understanding HIV pathogenesis and disease progression, which has allowed the identification of a multitude of drug and vaccine ta...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016208785861159
更新日期:2008-09-01 00:00:00
abstract::Neisseria gonorrhoeae (GC), a major cause of pelvic inflammatory disease, can facilitate HIV transmission. In response to GC infection, genital epithelial cells can produce cytokines, chemokines and defensins to modulate HIV infection and infectivity. GC can also induce the production of cytokines and chemokines in mo...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/157016212800618138
更新日期:2012-04-01 00:00:00
abstract:BACKGROUND:HIV-1+ long-term nonprogressors (LTNPs) maintain natural control of viral infection. This study sought to identify and characterize HIV- LTNPs series case, regarding the presence of possible host factors that may be associated with this status. METHODS:We evaluated the plasma levels of IP-10/IL-8 chemokines...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X16666171206120024
更新日期:2017-01-01 00:00:00
abstract::The human immunodeficiency virus (HIV) is unique in its capacity to produce chronic disease in almost all infected hosts. To accomplish this, it has evolved multiple mechanisms to effectively evade the immune response. HIV encodes at least one protein that makes infected cells resistant to CTL killing by downmodulatin...
journal_title:Current HIV research
pub_type: 杂志文章,评审
doi:10.2174/1570162033352138
更新日期:2003-01-01 00:00:00
abstract:BACKGROUND:Vitamin D deficiency is common in HIV population and has been associated with increased comorbidity risk and poor immunologic status. OBJECTIVE:To evaluate the effect of protease inhibitor lopinavir/ritonavir monotherapy on changes in serum 25-hydroxyvitamin D [25(OH)D] over 48 weeks. METHODS:Thirty-four t...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X18666200827115615
更新日期:2020-08-27 00:00:00
abstract:INTRODUCTION:Tuberculosis (TB) is a pandemic infectious disease especially frequent in HIV-infected patients. Toll-like receptor (TLR) 4 has been described to play a main role in the innate immunity against TB. In fact, single nucleotide polymorphisms (SNPs) in TLRs may influence AIDS disease progression. The associati...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/157016210791111052
更新日期:2010-04-01 00:00:00
abstract:BACKGROUND:HIV-1 CRF55_01B was first reported in 2013. At present, no report is available regarding this new clade's polymorphisms in its functionally critical regions protease and reverse transcriptase. OBJECTIVE:To identify the diversity difference in protease and reverse transcriptase between CRF55_01B and its pare...
journal_title:Current HIV research
pub_type: 杂志文章
doi:10.2174/1570162X18666200415140652
更新日期:2020-01-01 00:00:00