Page last updated: 2024-12-06
nafimidone
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
Nafimidone is a synthetic, non-narcotic analgesic. It is a selective inhibitor of the enzyme cyclooxygenase-2 (COX-2), which is responsible for the production of prostaglandins, inflammatory mediators involved in pain and inflammation. Nafimidone has been studied for its potential therapeutic effects in a variety of conditions, including pain, inflammation, and cancer. It has shown promising results in preclinical studies, but it has not yet been approved for use in humans. Nafimidone is a prodrug, meaning that it is converted to its active form in the body. The synthesis of Nafimidone involves several steps, including the reaction of a substituted aniline with a benzoyl chloride derivative. The resulting amide is then treated with a Grignard reagent to form the corresponding ketone. The final step in the synthesis is the reduction of the ketone to the desired alcohol. '
nafimidone: RN given refers to parent cpd [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 51200 |
| CHEMBL ID | 416801 |
| SCHEMBL ID | 1817018 |
| MeSH ID | M0116271 |
Synonyms (27)
| Synonym |
|---|
| 2-imidazol-1-yl-2'-acetonaphthone |
| 2-(1h-imidazol-1-yl)-1-(1-naphthalenyl)ethanone |
| nafimidonum [latin] |
| 1-(2-naphthoylmethyl)imidazole |
| nafimidone |
| brn 0523776 |
| ethanone, 2-(1h-imidazol-1-yl)-1-(1-naphthalenyl)- |
| nafimidone [inn] |
| nafimidona [spanish] |
| CHEMBL416801 |
| 2-imidazol-1-yl-1-naphthalen-2-ylethanone |
| hzu3iq1eww , |
| 64212-22-2 |
| nafimidonum |
| 5-23-04-00380 (beilstein handbook reference) |
| unii-hzu3iq1eww |
| nafimidona |
| nafimidone [mart.] |
| ITPVLJQRUQVNSD-UHFFFAOYSA-N |
| SCHEMBL1817018 |
| DTXSID80214426 |
| 1-(1-naphthyl)-2-(1h-imidazol-1-yl)ethanone |
| FT-0768480 |
| 1-(2-naphthyl)-2-(imidazol-1-yl)ethanone |
| Q6958175 |
| 2-(1h-imidazol-1-yl)-1-(naphthalen-2-yl)ethan-1-one |
| EN300-18563699 |
Research Excerpts
Overview
Nafimidone is a potential new antiepileptic drug with a therapeutic profile in experimental animal seizure models similar to that of phenytoin (PHT)
| Excerpt | Reference | Relevance |
|---|---|---|
| "Nafimidone is a new antiepileptic drug which may be effective in partial onset seizures. " | ( Pharmacokinetics of nafimidone in patients with chronic intractable epilepsy. Gunawan, S; Treiman, DM, 1987) | 2.04 |
| "Nafimidone is a potential new antiepileptic drug with a therapeutic profile in experimental animal seizure models similar to that of phenytoin (PHT). " | ( Efficacy of nafimidone in the treatment of intractable partial seizures: report of a two-center pilot study. Barber, KO; Ben-Menachem, E; Cereghino, JJ; McCormick, KB; Ojemann, L; Swisher, K; Treiman, DM; White, BG; Wilensky, AJ; Yerby, M, ) | 1.95 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " Systemic clearance of nafimidone from plasma after iv administration was approximately 2 times higher than hepatic blood flow in rats, and the oral bioavailability was 15%." | ( Disposition of nafimidone in rats. Chaplin, MD; Graham, DJ; Hall, DJ; Hama, KM; Kurz, L; Smith, SA, ) | 0.79 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| " within 30 min of dosing before electrical stimulation." | ( The anticonvulsant action of nafimidone on kindled amygdaloid seizures in rats. Albertson, TE; Walby, WF, ) | 0.42 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Bioassays (9)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID112801 | Effective dose in mice by horizontal screen assay (administered orally); No effect at highest dose of 400 mg/kg | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol. |
| AID40680 | In vitro displacement of [3H]flunitrazepam binding to cortical membranes at 5e-5M concentration | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol. |
| AID112168 | Effective dose to produce anticonvulsant activity using maximal electroshock assay (MES) evaluated in mice after oral administration | 1987 | Journal of medicinal chemistry, May, Volume: 30, Issue:5 | Imidazole anticonvulsants: structure-activity relationships of [(biphenylyloxy)alkyl]imidazoles. |
| AID112808 | Effective dose in mice by pentylenetetrazole assay (administered subcutaneously) | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol. |
| AID119413 | Potentiation of hexobarbital-induced sleeping time in mice | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol. |
| AID1312151 | Anticonvulsant activity in patient assessed as improvement in seizure control at 600 mg/day administered up to 1 year | 2016 | Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18 | Design and comparative anticonvulsant activity assessment of CNS-active alkyl-carbamoyl imidazole derivatives. |
| AID40681 | In vivo displacement of [3H]flunitrazepam binding to rat cortical membranes after 20 mg/kg ip dose | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol. |
| AID122339 | Compound was tested for time to peak anticonvulsant effect (TPE) | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol. |
| AID112804 | Effective dose in mice by maximal electroshock assay, administered orally | 1986 | Journal of medicinal chemistry, Sep, Volume: 29, Issue:9 | Structure-activity relationships of (arylalkyl)imidazole anticonvulsants: comparison of the (fluorenylalkyl)imidazoles with nafimidone and denzimol. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (16)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 8 (50.00) | 18.7374 |
| 1990's | 3 (18.75) | 18.2507 |
| 2000's | 1 (6.25) | 29.6817 |
| 2010's | 3 (18.75) | 24.3611 |
| 2020's | 1 (6.25) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 22.21
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.
| This Compound (22.21) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (4.35%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 22 (95.65%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||