Page last updated: 2024-12-08
albaconazole
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
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Protein Interactions
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Description
albaconazole: UR-9825 is the (1R,2R)-isomer; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
ID Source | ID |
---|---|
PubMed CID | 208952 |
CHEMBL ID | 298817 |
SCHEMBL ID | 1262830 |
MeSH ID | M0290738 |
Synonyms (37)
Synonym |
---|
7-chloro-3-((1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl)quinazolin-4(3h)-one |
ur-9825 |
w-0027 |
albaconazole |
7-chloro-3-[(1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1,2,4-triazol-1-yl)propyl]quinazolin-4-one |
CHEMBL298817 |
w0027 , |
187949-02-6 |
7-chloro-3-[(2r,3r)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1,2,4-triazol-1-yl)butan-2-yl]quinazolin-4-one |
albaconazol |
4(3h)-quinazolinone, 7-chloro-3-((1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl)- |
ur 9825 |
7-chloro-3-(2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl)quinazolin-4(3h)-one |
albaconazole [usan:inn] |
unii-ydw24y8iab |
ydw24y8iab , |
albaconazol [inn-spanish] |
albaconazole (usan/inn) |
D09702 |
(1r,2r)-7-chloro-3-[2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2, 4-triazol-1-yl)propyl]quinazolin-4(3h)-one |
(1r,2r)-7-chloro-3-[2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl]quinazolin-4(3h)-one |
UHIXWHUVLCAJQL-MPBGBICISA-N |
albaconazole [usan] |
7-chloro-3-[(1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl]quinazolin-4(3h)-one |
albaconazole [inn] |
SCHEMBL1262830 |
DTXSID3058244 |
bdbm50011477 |
AKOS027327579 |
J-012103 |
DB12073 |
Q4708967 |
7-chloro-3-((2r,3r)-3-(2,4-difluorophenyl)-3-hydroxy-4-(1h-1,2,4-triazol-1-yl)butan-2-yl)quinazolin-4(3h)-one |
ur 9625; ur 9825 |
ur9825 |
w 0027 |
4(3h)-quinazolinone, 7-chloro-3-[(1r,2r)-2-(2,4-difluorophenyl)-2-hydroxy-1-methyl-3-(1h-1,2,4-triazol-1-yl)propyl]- |
Research Excerpts
Overview
Albaconazole is an experimental triazole derivative with potent and broad-spectrum antifungal activity. It has a remarkably long half-life in dogs, monkeys, and humans.
Excerpt | Reference | Relevance |
---|---|---|
"Albaconazole is an experimental triazole derivative with potent and broad-spectrum antifungal activity and a remarkably long half-life in dogs, monkeys, and humans. " | ( Activity of the new triazole derivative albaconazole against Trypanosoma (Schizotrypanum) cruzi in dog hosts. Afonso, LC; Bahia, MT; Chiari, E; de Lana, M; Guedes, PM; Machado-Coelho, GL; Tafuri, WL; Urbina, JA; Veloso, VM, 2004) | 2.03 |
Effects
Excerpt | Reference | Relevance |
---|---|---|
"Albaconazole has also shown very potent activity against species of Candida, Cryptococcus and Aspergillus." | ( New and emerging treatments for fungal infections. Denning, DW; Pasqualotto, AC, 2008) | 1.07 |
Toxicity
Excerpt | Reference | Relevance |
---|---|---|
" However, frequent repeated dosing is required, and hepatic and cardiac adverse events may occur." | ( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis. Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013) | 0.59 |
" Most adverse events were mild or moderate, and treatment-related adverse events were all ≤3%." | ( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis. Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013) | 0.59 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
" Reduced toxicity, enhancement of bioavailability and counteraction of resistance are features desired by clinicians." | ( Newer antifungal agents. Türel, O, 2011) | 0.37 |
Dosage Studied
Excerpt | Relevance | Reference |
---|---|---|
" Its extended half-life probably permits dosing less frequently than once a day." | ( New and emerging treatments for fungal infections. Denning, DW; Pasqualotto, AC, 2008) | 0.35 |
" However, frequent repeated dosing is required, and hepatic and cardiac adverse events may occur." | ( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis. Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013) | 0.59 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Protein Targets (2)
Inhibition Measurements
Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
---|---|---|---|---|---|---|---|
Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 (µMol) | 34.8600 | 0.0009 | 1.9014 | 10.0000 | AID1138338 |
Sterol 14-alpha demethylase | Trypanosoma cruzi strain CL Brener | IC50 (µMol) | 0.0010 | 0.0010 | 1.7070 | 10.0000 | AID1915709 |
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] |
Biological Processes (22)
Molecular Functions (12)
Ceullar Components (5)
Process | via Protein(s) | Taxonomy |
---|---|---|
plasma membrane | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
cell surface | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
perinuclear region of cytoplasm | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
voltage-gated potassium channel complex | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
inward rectifier potassium channel complex | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
plasma membrane | Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) |
[Information is prepared from geneontology information from the June-17-2024 release] |
Bioassays (110)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID167736 | In vivo antifungal activity against systemic candidosis in rabbit kidney at a dose of 12.5 mg/kg, qd, po. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID1651348 | Antifungal activity against fluconazole-resistant Candida albicans isolate 100 by NCCLS protocol based broth microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID562993 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID432803 | Antifungal activity against Sporothrix albicans after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
AID725869 | Antifungal activity against Rhizomucor pusillus RHMI1 after 48 hrs by broth microdilution test | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID165452 | In vivo antifungal activity against systemic candidosis in rabbit lung at a dose of 2.5 mg/kg, qd, po. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID123517 | The compound was tested in vivo for anti-candida activity in mice model 1 (dose :0.5 mg/kg,fluconazole-treated group) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID562989 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID1247371 | Antifungal activity against Candida parapsilosis 22019 after 24 hrs by serial dilution method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates. |
AID307397 | Antifungal activity against Candida lusitaniae ATCC 42720 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID307400 | Antifungal activity against Aspergillus fumigatus ATCC 16424 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID118766 | In vivo antifungal activity against murine candidosis model after peroral administration with 0.5 mg/kg at various time intervals. (percent protection for 100% mortality with untreated group) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID307398 | Antifungal activity against Candida tropicalis ATCC 750 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID307394 | Antifungal activity against Candida glabrata ATCC 34138 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID725871 | Antifungal activity against Scedosporium sp. SCSP1 after 48 hrs by broth microdilution test | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID1651344 | Antifungal activity against Candida albicans Y0109 by NCCLS protocol based broth microdilution assay | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID167735 | In vivo antifungal activity against systemic candidosis in rabbit kidney at a dose of 0.5 mg/kg, qd, po. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID525140 | Antifungal activity against Fusarium moniliforme clade 2 by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
AID725874 | Antifungal activity against Aspergillus fumigatus ASFU20 after 48 hrs by M38 method | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID1138333 | Antimicrobial activity against fluconazole-resistant Candida albicans 100 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID1247369 | Antifungal activity against Candida albicans SC5314 after 24 hrs by serial dilution method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates. |
AID220226 | In vitro for antifungal activity against 10 yeasts | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID562994 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID562990 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID1247374 | Antifungal activity against Aspergillus fumigatus 7544 after 48 hrs by serial dilution method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates. |
AID1138335 | Antimicrobial activity against fluconazole-resistant Candida albicans J18 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID725882 | Antifungal activity against Candida krusei CAKR7 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID563001 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID562987 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID307403 | Antifungal activity against Aspergillus niger ATCC 9042 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID1651345 | Antifungal activity against Candida parapsilosis 22019 by NCCLS protocol based broth microdilution assay | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID26407 | Half-life in rats after iv administration | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID432799 | Antifungal activity against Sporothrix brasiliensis after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
AID562998 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID725881 | Antifungal activity against Candida krusei CAKR8 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID307399 | Antifungal activity against Candida parapsilosis ATCC 21019 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID432801 | Antifungal activity against Sporothrix globosa after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
AID195068 | In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 1 mg/kg, bid, po | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID73614 | In vitro antifungal activity against 6 filamentous fungi | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID562996 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID563000 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage twice daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID118757 | In vivo antifungal activity against murine candidosis model after peroral administration with 0.25 mg/kg at various time intervals. (percent protection for 100% mortality with untreated group); not tested | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID1138336 | Antimicrobial activity against fluconazole-resistant Candida albicans J28 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID725877 | Antifungal activity against Aspergillus fumigatus ASFU13 after 48 hrs by M38 method | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID1651343 | Antifungal activity against Aspergillus fumigatus 7544 by NCCLS protocol based broth microdilution assay | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID1138338 | Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID118756 | In vivo antifungal activity against murine candidosis model after peroral administration with 0.25 mg/kg at various time intervals. (percent protection for 100% mortality with fluconazole-treated group.); not tested | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID432800 | Antifungal activity against Sporothrix schenckii after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
AID118758 | In vivo antifungal activity against murine candidosis model after peroral administration with 0.5 mg/Kg at various time intervals. (percent protection for 100% mortality with fluconazole-treated group.) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID562995 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID307401 | Antifungal activity against Aspergillus flavus ATCC MYA-1004 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID1247373 | Antifungal activity against Candida glabrata 537 after 24 hrs by serial dilution method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates. |
AID562988 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID118893 | In vivo antifungal activity against murine candidosis model after peroral administration with 1 mg/kg at various time intervals. (percent protection for 100% mortality with untreated group) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID123519 | The compound was tested in vivo for anti-candida activity in mice model 2(dose: 5 mg/kg, untreated group). | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID525139 | Antifungal activity against Fusarium moniliforme clade 1 by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
AID1138337 | Antimicrobial activity against fluconazole-resistant Candida albicans J38 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID1651341 | Antifungal activity against Candida albicans SC5314 by NCCLS protocol based broth microdilution assay | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID525141 | Antifungal activity against Fusarium moniliforme clade 3 by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
AID562992 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 5 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID525142 | Antifungal activity against Fusarium thapsinum by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6 | In vitro antifungal susceptibility and molecular characterization of clinical isolates of Fusarium verticillioides (F. moniliforme) and Fusarium thapsinum. |
AID1138330 | Antimicrobial activity against Cryptococcus neoformans 32609 after 72 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID195069 | In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 25 mg/kg, bid, po | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID725880 | Antifungal activity against Candida glabrata CAGL2 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID1247372 | Antifungal activity against Cryptococcus neoformans 32609 after 72 hrs by serial dilution method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates. |
AID123520 | The compound was tested in vivo for anti-candida activity in mice model 2(dose :5 mg/kg,fluconazole-treated group) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID123518 | The compound was tested in vivo for anti-candida activity in mice model 1(dose: 0.5 mg/kg, untreated group). | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID725886 | Antifungal activity against fluconazole-resistant Candida albicans DSY735 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID432802 | Antifungal activity against Sporothrix mexicana after 72 hrs by microdilution method | 2008 | Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2 | In vitro antifungal susceptibilities of five species of sporothrix. |
AID1138331 | Antimicrobial activity against Candida glabrata 537 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID1651342 | Antifungal activity against Cryptococcus neoformans 32605 by NCCLS protocol based broth microdilution assay | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID195070 | In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 5 mg/kg, bid, po | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID725878 | Antifungal activity against acquired-resistant Candida parapsilosis CAPA2 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID1651347 | Antifungal activity against Microsporum gypseum CMCC by NCCLS protocol based broth microdilution assay | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID725870 | Antifungal activity against Rhizomucor pusillus RHPU1 after 48 hrs by broth microdilution test | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID307395 | Antifungal activity against Candida krusei ATCC 6528 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID1247370 | Antifungal activity against Candida albicans Y0109 after 24 hrs by serial dilution method | 2015 | European journal of medicinal chemistry, Sep-18, Volume: 102 | Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates. |
AID307393 | Antifungal activity against Candida albicans ATCC 36082 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID1138340 | Aqueous solubility of the compound in hydrochloric acid solution at pH 1.2 | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID1651349 | Antifungal activity against fluconazole-resistant Candida albicans isolate 103 by NCCLS protocol based broth microdilution method | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID195071 | In vivo activity against disseminated aspergillosis (liver) in immunocompromized rat model at a dose of 50 mg/kg, bid, po | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID165450 | In vivo antifungal activity against systemic candidosis in rabbit lung at a dose of 0.5 mg/kg, qd, po. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID167737 | In vivo antifungal activity against systemic candidosis in rabbit kidney at a dose of 2.5 mg/kg, qd, po. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID1138341 | Aqueous solubility of the compound in phosphate buffer at pH 7.4 | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID562991 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage once daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID562997 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 20 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID725876 | Antifungal activity against Aspergillus fumigatus ASFU7 after 48 hrs by M38 method | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID725873 | Antifungal activity against Aspergillus fumigatus ASFU19 after 48 hrs by M38 method | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID563002 | Antifungal activity against Candida albicans isolate 03-2718 after 48 hrs | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID725875 | Antifungal activity against Aspergillus fumigatus ASFU17 after 48 hrs by M38 method | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID165451 | In vivo antifungal activity against systemic candidosis in rabbit lung at a dose of 12.5 mg/kg, qd, po. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID1138332 | Antimicrobial activity against Aspergillus fumigatus 7544 after 48 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID1138328 | Antimicrobial activity against Candida albicans Y0109 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID1138334 | Antimicrobial activity against fluconazole-resistant Candida albicans 103 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID49099 | The compound was tested in vitro for antifungal activity against Candida albicans. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID1138327 | Antimicrobial activity against Candida albicans SC5314 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID562999 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 10 mg/kg, administered through oral gavage once daily for 5 days measured on day 1 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID725885 | Antifungal activity against fluconazole-susceptible Candida albicans CAAL93 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID1138329 | Antimicrobial activity against Candida parapsilosis 22019 after 24 hrs by serial dilution method | 2014 | Journal of medicinal chemistry, May-08, Volume: 57, Issue:9 | Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility. |
AID562986 | Antifungal activity against Candida albicans isolate 03-2718 infected BALB/c mouse vaginitis model assessed as reduction in fungal load in vagina at 40 mg/kg, administered through oral gavage twice daily for 5 days measured on day 6 post inoculation | 2009 | Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10 | Efficacy of albaconazole against Candida albicans in a vaginitis model. |
AID1915709 | Inhibition of Trypanosoma cruzi Sterol 14-alpha demethylase | 2021 | European journal of medicinal chemistry, Feb-05, Volume: 211 | Therapeutic progression of quinazolines as targeted chemotherapeutic agents. |
AID725872 | Antifungal activity against Aspergillus fumigatus ASFU23 after 48 hrs by M38 method | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID307402 | Antifungal activity against Aspergillus terreus ATCC 28301by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID1651346 | Antifungal activity against Candida glabrata 537 by NCCLS protocol based broth microdilution assay | 2020 | Bioorganic & medicinal chemistry letters, 02-15, Volume: 30, Issue:4 | Design, synthesis, and structure-activity relationship studies of novel triazole agents with strong antifungal activity against Aspergillus fumigatus. |
AID118889 | In vivo antifungal activity against murine candidosis model after peroral administration with 1 mg/kg at various time intervals. (percent protection for 100% mortality with fluconazole-treated group.) | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID725883 | Antifungal activity against fluconazole-resistant Candida albicans DSY292 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID725884 | Antifungal activity against fluconazole-susceptible Candida albicans CAAL97 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
AID15872 | Log P value of the compound. | 1998 | Journal of medicinal chemistry, May-21, Volume: 41, Issue:11 | New azole antifungals. 3. Synthesis and antifungal activity of 3-substituted-4(3H)-quinazolinones. |
AID307396 | Antifungal activity against Cryptococcus neoformans ATCC 21019 by broth microdilution assay | 2007 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12 | Discovery of novel indazole-linked triazoles as antifungal agents. |
AID725879 | Antifungal activity against acquired-resistant Candida parapsilosis CAPA1 after 24 hrs by spectrofluorometric analysis | 2013 | ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2 | Discovery of a novel broad-spectrum antifungal agent derived from albaconazole. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (33)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 2 (6.06) | 18.2507 |
2000's | 20 (60.61) | 29.6817 |
2010's | 9 (27.27) | 24.3611 |
2020's | 2 (6.06) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 34.35
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 (34.35) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 1 (2.94%) | 5.53% |
Reviews | 7 (20.59%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 26 (76.47%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Clinical Trials (3)
Trial Overview
Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
---|---|---|---|---|---|---|---|
A Phase 1, Randomized, Open-Label, Crossover Safety and Pharmacokinetic Study of 400 mg Albaconazole as a Tablet Formulation Versus a Capsule Formulation in Healthy Subjects [NCT01039883] | Phase 1 | 40 participants (Actual) | Interventional | 2009-11-23 | Completed | ||
A Phase 2, Randomized, Double-blind, Placebo-controlled, Parallel-group, Dose-ranging Study to Investigate the Efficacy and Safety of 4 Dose Regimens of Oral Albaconazole in Subjects With Distal Subungual Onychomycosis [NCT00730405] | Phase 2 | 582 participants (Actual) | Interventional | 2008-07-16 | Completed | ||
A Single-Blind, Randomized, Dose-Finding Study Versus Fluconazole to Assess the Efficacy and Tolerability of Five Single Doses of Albaconazole in the Treatment of Acute Non-Recurrent Candida Spp Vulvovaginitis [NCT00199264] | Phase 2 | 60 participants | Interventional | 2004-06-30 | Terminated | ||
[information is prepared from clinicaltrials.gov, extracted Sep-2024] |