Compounds > iqp-0528
Page last updated: 2024-12-08

iqp-0528

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth

Cross-References

ID SourceID
PubMed CID483499
CHEMBL ID556417
SCHEMBL ID674037
MeSH IDM0574835

Synonyms (24)

Synonym
iqp-0528
6-[(3,5-dimethylphenyl)carbonyl]-1-(cyclopropylmethyl)-5-(methylethyl)-1,3-dihydropyrimidine-2,4-dione
1-(cyclopropylmethyl)-6-(3,5-dimethylbenzoyl)-5-isopropyl-pyrimidine-2,4-dione
2,4(1h,3h)-pyrimidinedione, 1-(cyclopropylmethyl)-6-(3,5-dimethylbenzoyl)-5-isopropyl-
1-(cyclopropylmethyl)-6-(3,5-dimethylbenzoyl)-5-propan-2-ylpyrimidine-2,4-dione
CHEMBL556417 ,
1367755-87-0
SCHEMBL674037
2,4(1h,3h)-pyrimidinedione, 1-(cyclopropylmethyl)-6-(3,5-dimethylbenzoyl)-5-(1-methylethyl)-
unii-1y42tzl33o
301297-45-0
1y42tzl33o ,
iqp-528
1-(cyclopropyl)methyl-5-isopropyl-6-(3,5-dimethylbenzoyl)-2,4-pyrimidinedione
UCOAKFIVSAVHLC-UHFFFAOYSA-N ,
bdbm50480660
1-(3-cyclopropyl)methyl-6-(3,5-dimethylbenzoyl)-5-isopropyl-2,4(1h,3h)-pyrimidinedione
DB14888
SB17098
Q27253135
1-(cyclopropylmethyl)-6-(3,5-dimethylbenzoyl)-5-isopropylpyrimidine-2,4(1h,3h)-dione
CS-0015606
HY-19509
AKOS040748591

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" With the increased realization of receptive anal intercourse among heterosexual couples often in conjunction with vaginal intercourse, having a safe and effective microbicide for both mucosal sites is critical."( Safety and efficacy of tenofovir/IQP-0528 combination gels - a dual compartment microbicide for HIV-1 prevention.
Buckheit, KW; Buckheit, RW; Dezzutti, CS; Gwozdz, G; Mahalingam, A; Shetler, C; Ugaonkar, SR, 2012)		0.66

Dosage Studied

Polymeric quick-dissolving films were developed as a solid dosage topical microbicide formulation for the vaginal delivery of HIV nonnucleoside reverse transcriptase inhibitor (NNRTI) pyrimidinedione.

ExcerptRelevanceReference
"Polymeric quick-dissolving films were developed as a solid dosage topical microbicide formulation for the vaginal delivery of the highly potent and non-toxic, dual-acting HIV nonnucleoside reverse transcriptase inhibitor (NNRTI) pyrimidinedione, IQP-0528."( Vaginal film drug delivery of the pyrimidinedione IQP-0528 for the prevention of HIV infection.
Boczar, A; Buckheit, RW; Ham, AS; Rohan, LC; W Buckheit, K; Yang, L, 2012)		0.81
"Based on the above evaluations, a vaginal film formulation has been identified as a potential solid dosage form for the vaginal delivery of the topical microbicide candidate IQP-0528."( Vaginal film drug delivery of the pyrimidinedione IQP-0528 for the prevention of HIV infection.
Boczar, A; Buckheit, RW; Ham, AS; Rohan, LC; W Buckheit, K; Yang, L, 2012)		0.83
" Low adherence linked with frequent dosing and short therapeutic duration has emerged as the major reason for inconsistent efficacy outcomes with gels in clinical trials."( Osmotic pump tablets for delivery of antiretrovirals to the vaginal mucosa.
Herold, BC; Kiser, PF; Mesquita, PM; Rastogi, R; Teller, RS, 2013)		0.39
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Reverse transcriptase/RNaseH Human immunodeficiency virus 1IC50 (µMol)2.33350.00011.076810.0000AID427965; AID427966
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (18)

Assay IDTitleYearJournalArticle
AID427961Cytotoxicity against human CEM-SS cells by XTT assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427963Therapeutic index, ratio of TC50 for human CEM-SS cells to EC50 for HIV1 RF infected in human CEM-SS cells2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427972Antiviral activity against HIV1 infected in human CEM-SS cells assessed as inhibition of viral replication and virus-induced cytopathic effect by dose-response curve analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427962Antiviral activity against HIV2 ROD infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427982Antiviral activity against SIV MAC251 infected in human 174xCEM cells assessed as inhibition of virus-induced cytopathic effect2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427977Inhibition of HIV2 reverse transcriptase2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427967Antiviral activity against HIV1 infected in human HeLa cells expressing CD4-LTR assessed as inhibition of viral entry-related beta galactosidase expression treated for 2 hrs followed by drug wash out measured after 48 hrs by MAGI assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427960Antiviral activity against HIV1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427965Inhibition of wild type HIV1 reverse transcriptase assessed as 32P-labeled GMP incorporation into nascent DNA strand2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427980Inhibition of HIV2 reverse transcriptase assessed as 32P-labeled GMP incorporation into nascent DNA strand at highest concentration2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427966Inhibition of HIV1 reverse transcriptase K103N mutant assessed as 32P-labeled GMP incorporation into nascent DNA strand2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427981Inhibition of HIV1 gp120/CD4 interaction assessed as inhibition of gp120 and gp41 coexpressing human HL2/3 cell fusion to CD4 expressing human HeLa cells treated for 2 hrs measured after 48 hrs by chemiluminescence assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427978Antiviral activity against HIV2 assessed as inhibition of viral single round replication at early time point2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427968Cytotoxicity against human HeLa cells expressing CD4-LTR by XTT assay2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427964Therapeutic index, ratio of TC50 for human CEM-SS cells to EC50 for HIV2 ROD infected in human CEM-SS cells2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427983Antiviral activity against HIV2 infected in human CEM-SS cells assessed as inhibition of viral replication and virus-induced cytopathic effect by dose-response curve analysis2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427969Therapeutic index, ratio of TC50 human HeLa cells expressing CD4-LTR to EC50 for HIV1 entry inhibition in human HeLa cells expressing CD4-LTR2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
AID427979Antiviral activity against HIV2 assessed as inhibition of viral replication treated at time points after viral entry into host cells2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Comparative evaluation of the inhibitory activities of a series of pyrimidinedione congeners that inhibit human immunodeficiency virus types 1 and 2.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (10.00)29.6817
2010's9 (90.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other10 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
adenine
[no description available]		2.48206-aminopurines;
purine nucleobase		Daphnia magna metabolite;
Escherichia coli metabolite;
human metabolite;
mouse metabolite;
Saccharomyces cerevisiae metabolite
lactic acid
Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.		2.13102-hydroxy monocarboxylic acidalgal metabolite;
Daphnia magna metabolite
pontamine sky blue
[no description available]		2.0410
zidovudine
Zidovudine: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by an azido group. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication, acting as a chain-terminator of viral DNA during reverse transcription. It improves immunologic function, partially reverses the HIV-induced neurological dysfunction, and improves certain other clinical abnormalities associated with AIDS. Its principal toxic effect is dose-dependent suppression of bone marrow, resulting in anemia and leukopenia.. zidovudine : A pyrimidine 2',3'-dideoxyribonucleoside compound having a 3'-azido substituent and thymine as the nucleobase.		2.0410azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
efavirenz
efavirenz: HIV-1 reverse transcriptase inhibitor. efavirenz : 1,4-Dihydro-2H-3,1-benzoxazin-2-one substituted at the 4 position by cyclopropylethynyl and trifluoromethyl groups (S configuration) and at the 6 position by chlorine. A non-nucleoside reverse transcriptase inhibitor with activity against HIV, it is used with other antiretrovirals for combination therapy of HIV infection.		2.0410acetylenic compound;
benzoxazine;
cyclopropanes;
organochlorine compound;
organofluorine compound		antiviral drug;
HIV-1 reverse transcriptase inhibitor
organophosphonates
hydrogenphosphite : A divalent inorganic anion resulting from the removal of a proton from two of the hydroxy groups of phosphorous acid.		2.4820divalent inorganic anion;
phosphite ion
tenofovir
tenofovir (anhydrous) : A member of the class of phosphonic acids that is methylphosphonic acid in which one of the methyl hydrogens is replaced by a [(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy group. An inhibitor of HIV-1 reverse transcriptase, the bis(isopropyloxycarbonyloxymethyl) ester (disoproxil ester) prodrug is used as the fumaric acid salt in combination therapy for the treatment of HIV infection.		2.4820nucleoside analogue;
phosphonic acids		antiviral drug;
drug metabolite;
HIV-1 reverse transcriptase inhibitor
piperidines
Piperidines: A family of hexahydropyridines.		2.1110
pyrimidinones
Pyrimidinones: Heterocyclic compounds known as 2-pyrimidones (or 2-hydroxypyrimidines) and 4-pyrimidones (or 4-hydroxypyrimidines) with the general formula C4H4N2O.		3.7190
ConditionIndicatedRelationship StrengthStudiesTrials
HIV Coinfection
[description not available]		03.4870
HIV Infections
Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).		03.4870
AIDS, Simian
[description not available]		02.1110
Acquired Immune Deficiency Syndrome
[description not available]		02.0710
Acquired Immunodeficiency Syndrome
An acquired defect of cellular immunity associated with infection by the human immunodeficiency virus (HIV), a CD4-positive T-lymphocyte count under 200 cells/microliter or less than 14% of total lymphocytes, and increased susceptibility to opportunistic infections and malignant neoplasms. Clinical manifestations also include emaciation (wasting) and dementia. These elements reflect criteria for AIDS as defined by the CDC in 1993.		02.0710