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 Source | ID |
|---|---|
| PubMed CID | 483499 |
| CHEMBL ID | 556417 |
| SCHEMBL ID | 674037 |
| MeSH ID | M0574835 |
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
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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.
| Excerpt | Relevance | Reference |
|---|---|---|
| "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
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC50 (µMol) | 2.3335 | 0.0001 | 1.0768 | 10.0000 | AID427965; AID427966 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Bioassays (18)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID427961 | Cytotoxicity against human CEM-SS cells by XTT assay | 2008 | Antimicrobial 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. |
| AID427963 | Therapeutic index, ratio of TC50 for human CEM-SS cells to EC50 for HIV1 RF infected in human CEM-SS cells | 2008 | Antimicrobial 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. |
| AID427972 | Antiviral activity against HIV1 infected in human CEM-SS cells assessed as inhibition of viral replication and virus-induced cytopathic effect by dose-response curve analysis | 2008 | Antimicrobial 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. |
| AID427962 | Antiviral activity against HIV2 ROD infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay | 2008 | Antimicrobial 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. |
| AID427982 | Antiviral activity against SIV MAC251 infected in human 174xCEM cells assessed as inhibition of virus-induced cytopathic effect | 2008 | Antimicrobial 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. |
| AID427977 | Inhibition of HIV2 reverse transcriptase | 2008 | Antimicrobial 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. |
| AID427967 | Antiviral 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 assay | 2008 | Antimicrobial 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. |
| AID427960 | Antiviral activity against HIV1 RF infected in human CEM-SS cells assessed as inhibition of virus-induced cytopathic effect by XTT assay | 2008 | Antimicrobial 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. |
| AID427965 | Inhibition of wild type HIV1 reverse transcriptase assessed as 32P-labeled GMP incorporation into nascent DNA strand | 2008 | Antimicrobial 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. |
| AID427980 | Inhibition of HIV2 reverse transcriptase assessed as 32P-labeled GMP incorporation into nascent DNA strand at highest concentration | 2008 | Antimicrobial 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. |
| AID427966 | Inhibition of HIV1 reverse transcriptase K103N mutant assessed as 32P-labeled GMP incorporation into nascent DNA strand | 2008 | Antimicrobial 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. |
| AID427981 | Inhibition 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 assay | 2008 | Antimicrobial 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. |
| AID427978 | Antiviral activity against HIV2 assessed as inhibition of viral single round replication at early time point | 2008 | Antimicrobial 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. |
| AID427968 | Cytotoxicity against human HeLa cells expressing CD4-LTR by XTT assay | 2008 | Antimicrobial 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. |
| AID427964 | Therapeutic index, ratio of TC50 for human CEM-SS cells to EC50 for HIV2 ROD infected in human CEM-SS cells | 2008 | Antimicrobial 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. |
| AID427983 | Antiviral activity against HIV2 infected in human CEM-SS cells assessed as inhibition of viral replication and virus-induced cytopathic effect by dose-response curve analysis | 2008 | Antimicrobial 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. |
| AID427969 | Therapeutic index, ratio of TC50 human HeLa cells expressing CD4-LTR to EC50 for HIV1 entry inhibition in human HeLa cells expressing CD4-LTR | 2008 | Antimicrobial 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. |
| AID427979 | Antiviral activity against HIV2 assessed as inhibition of viral replication treated at time points after viral entry into host cells | 2008 | Antimicrobial 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)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 1 (10.00) | 29.6817 |
| 2010's | 9 (90.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 10 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||