Compounds > pms 601
Page last updated: 2024-11-08

pms 601

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

Description

PMS 601: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID462383
CHEMBL ID6322
SCHEMBL ID7243345
MeSH IDM0365363

Synonyms (16)

Synonym
diethyl-carbamic acid 1,4-bis-(3,4,5-trimethoxy-benzoyl)-piperazin-2-ylmethyl ester(pms 601)
diethyl-carbamic acid 1,4-bis-(3,4,5-trimethoxy-benzoyl)-piperazin-2-ylmethyl ester
bdbm50046993
pms-601
158978-98-4
pms 601
[1,4-bis(3,4,5-trimethoxybenzoyl)piperazin-2-yl]methyl n,n-diethylcarbamate
carbamic acid, n,n-diethyl-, [1,4-bis(3,4,5-trimethoxybenzoyl)-2-piperazinyl]methyl ester
CHEMBL6322 ,
ZINC04394014
carbamic acid, n,n-diethyl-, (1,4-bis(3,4,5-trimethoxybenzoyl)-2-piperazinyl)methyl ester
1,4-bis(3',4',5'-trimethoxybenzoyl)-2-(n,n-diethylaminocarbonyloxymethyl)piperazine
QKSXEJNMSRTCRE-UHFFFAOYSA-N
SCHEMBL7243345
DTXSID30936025
[1,4-bis(3,4,5-trimethoxybenzoyl)piperazin-2-yl]methyl diethylcarbamate

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" The transport parameter measured (K(in)) proves that 1a is able to cross this biological barrier, but a pharmacokinetic study reveals its weak bioavailability in rats."( Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
Bensaid, O; Cisternino, S; Clayette, P; Dereuddre-Bosquet, N; Dong, CZ; Dormont, D; Heymans, F; Huet, J; Lamouri, A; Martin, M; Redeuilh, C; Rousselle, C; Scherrmann, JM; Serradji, N, 2004)		0.32
[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)
Platelet-activating factor receptorCavia porcellus (domestic guinea pig)IC50 (µMol)25.80000.00430.75777.8000AID167654
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (16)

Assay IDTitleYearJournalArticle
AID281895AUC in Sprague-Dawley rat at 500 mg/kg, po normalized to 1 mg/kg2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID157040Inhibition of PAF-induced platelet aggregation was determined using platelet rich plasma (PRP) of New Zealand rabbits.2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Structure-activity relationships in platelet-activating factor (PAF). 10. From PAF antagonism to inhibition of HIV-1 replication.
AID281890Cmax in Sprague-Dawley rat at 100 mg/kg, iv normalized to 1 mg/kg2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID281883Antiviral activity against HIV1 BAL in human MDM cells2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID281893Cmax in Sprague-Dawley rat at 500 mg/kg, po normalized to 1 mg/kg2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID167654Inhibition of PAF-induced rabbit platelet aggregation1993Journal of medicinal chemistry, Apr-16, Volume: 36, Issue:8
Design and modeling of new platelet-activating factor antagonists. 1. Synthesis and biological activity of 1,4-bis(3',4',5'-trimethoxybenzoyl)-2-[[(substituted carbonyl and carbamoyl)oxy]methyl]piperazines.
AID281889Inhibition of PAF-induced platelet aggregation in rabbit platelet-rich plasma2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID83105Antiviral activity towards inhibition of HIV-1 replication using monocyte-derived macrophage infected by the HIV-1/Ba-L strain.2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Structure-activity relationships in platelet-activating factor (PAF). 10. From PAF antagonism to inhibition of HIV-1 replication.
AID83104Cytotoxic concentration against monocyte-derived macrophage infected by the HIV-1/Ba-L strain using neutral red staining assay.2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Structure-activity relationships in platelet-activating factor (PAF). 10. From PAF antagonism to inhibition of HIV-1 replication.
AID281885Cytotoxicity against human MDM cells by neutral red staining2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID83107Percent inhibition at 100 uM dose of HIV-1 replication using monocyte-derived macrophages infected by the HIV-1/Ba-L strain.2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Structure-activity relationships in platelet-activating factor (PAF). 10. From PAF antagonism to inhibition of HIV-1 replication.
AID281898Partition coefficient, log P of the compound2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID281891Half life in Sprague-Dawley rat at 100 mg/kg, iv normalized to 1 mg/kg2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID281892AUC in Sprague-Dawley rat at 100 mg/kg, iv normalized to 1 mg/kg2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID281894Half life in Sprague-Dawley rat at 500 mg/kg, po normalized to 1 mg/kg2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
AID281896Bioavailability in Sprague-Dawley rat at 500 mg/kg, po normalized to 1 mg/kg2004Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25
Structure-activity relationships in platelet-activating factor. 12. Synthesis and biological evaluation of platelet-activating factor antagonists with anti-HIV-1 activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's1 (16.67)18.2507
2000's5 (83.33)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.95

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.95 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.95)

All Compounds (24.57)

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%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
carbamates
[no description available]		2.0210amino-acid anion
thiazoles
[no description available]		2101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
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.		210azide;
pyrimidine 2',3'-dideoxyribonucleoside		antimetabolite;
antiviral drug;
HIV-1 reverse transcriptase inhibitor
1-hexadecyl-2-acetyl-glycero-3-phosphocholine
Platelet Activating Factor: A phospholipid derivative formed by PLATELETS; BASOPHILS; NEUTROPHILS; MONOCYTES; and MACROPHAGES. It is a potent platelet aggregating agent and inducer of systemic anaphylactic symptoms, including HYPOTENSION; THROMBOCYTOPENIA; NEUTROPENIA; and BRONCHOCONSTRICTION.. 2-O-acetyl-1-O-hexadecyl-sn-glycero-3-phosphocholine : A 2-acetyl-1-alkyl-sn-glycero-3-phosphocholine betaine which has hexadecyl as the alkyl group. PAF is a potent phospholipid activator and mediator of many leukocyte functions, including platelet aggregation, inflammation, and anaphylaxis.		2.93402-acetyl-1-alkyl-sn-glycero-3-phosphocholineantihypertensive agent;
beta-adrenergic antagonist;
bronchoconstrictor agent;
hematologic agent;
vasodilator agent
rp 48740
3-(3-pyridinyl)-1H,3H-pyrrolo(1,2-c)thiazole-7-carboxamide: platelet activating factor antagonist		210
ginkgolide b
[no description available]		1.9810
ConditionIndicatedRelationship StrengthStudiesTrials
HIV
Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.		02.4120
Cognition Disorders
Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.		02.0510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.0510
Astrocytosis
[description not available]		02.0510
Acquired-Immune Deficiency Syndrome Dementia Complex
[description not available]		02.0510
AIDS Dementia Complex
A neurologic condition associated with the ACQUIRED IMMUNODEFICIENCY SYNDROME and characterized by impaired concentration and memory, slowness of hand movements, ATAXIA, incontinence, apathy, and gait difficulties associated with HIV-1 viral infection of the central nervous system. Pathologic examination of the brain reveals white matter rarefaction, perivascular infiltrates of lymphocytes, foamy macrophages, and multinucleated giant cells. (From Adams et al., Principles of Neurology, 6th ed, pp760-1; N Engl J Med, 1995 Apr 6;332(14):934-40)		02.0510