Page last updated: 2024-11-12

ar-709

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

Cross-References

ID Source	ID
PubMed CID	11226413
CHEMBL ID	242199
SCHEMBL ID	3258035
MeSH ID	M0593065

Synonyms (13)

Synonym
5-chloro-3-({4-[(2,4-diaminopyrimidin-5-yl)methyl]-6,7-dimethoxy-1-benzofuran-2-yl}methyl)-n,n-dimethyl-1h-indole-2-carboxamide
bdbm18071
ar-709
CHEMBL242199
952042-29-4
unii-qua6ejn8tl
663214-64-0
1h-indole-2-carboxamide, 5-chloro-3-((4-((2,4-diamino-5-pyrimidinyl)methyl)-6,7-dimethoxy-2-benzofuranyl)methyl)-n,n-dimethyl-
qua6ejn8tl ,
SCHEMBL3258035
Q27287499
5-chloro-3-[[4-[(2,4-diaminopyrimidin-5-yl)methyl]-6,7-dimethoxy-1-benzofuran-2-yl]methyl]-n,n-dimethyl-1h-indole-2-carboxamide
DTXSID401026061

Research Excerpts

Bioavailability

After IV administration, clearance of AR-709 was 496 mL/min. Volume of distribution was 1,700 L and the absolute oral bioavailability was 2.

Excerpt	Reference	Relevance
"To explore, in a microdose (phase-0) study, the pharmacokinetics, bioavailability and concentrations in key compartments of the lung, of AR-709, a novel diaminopyrimidine antibiotic for the treatment of respiratory infection."	( A microdose study of ¹⁴C-AR-709 in healthy men: pharmacokinetics, absolute bioavailability and concentrations in key compartments of the lung. Boyce, MJ; Lappin, G; Lociuro, S; Matzow, T; Seymour, M; Warrington, SJ, 2013)	0.9
" Its low oral bioavailability however, precludes oral administration."	( A microdose study of ¹⁴C-AR-709 in healthy men: pharmacokinetics, absolute bioavailability and concentrations in key compartments of the lung. Boyce, MJ; Lappin, G; Lociuro, S; Matzow, T; Seymour, M; Warrington, SJ, 2013)	0.69

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (27)

Assay ID	Title	Year	Journal	Article
AID519207	Antibacterial activity against penicillin intermediate Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID519208	Antibacterial activity against penicillin resistant Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID520406	Antimicrobial activity against quinolone-resistant Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID520405	Antimicrobial activity against quinolone-susceptible Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID519214	Antibacterial activity against amoxicillin-clavulanic acid susceptible Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID520414	Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID519210	Antibacterial activity against cotrimoxazole intermediate Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID519212	Antibacterial activity against azithromycin susceptible Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID519217	Antibacterial activity against Streptococcus pneumoniae ATCC 49619 by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID520407	Antimicrobial activity against trimethoprim-sulfamethoxazole-susceptible Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID297557	Inhibition of Bacillus anthracis DHFR	2007	Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18	Crystal structure of the anthrax drug target, Bacillus anthracis dihydrofolate reductase.
AID519213	Antibacterial activity against azithromycin resistant Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID520409	Antimicrobial activity against macrolide-susceptible Streptococcus sp. 'group A' by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID519206	Antibacterial activity against penicillin susceptible Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID519205	Antibacterial activity against Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID519216	Antibacterial activity against multidrug resistant Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID520413	Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID520412	Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID520403	Antimicrobial activity against macrolide-susceptible Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID519211	Antibacterial activity against cotrimoxazole resistant Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID520408	Antimicrobial activity against trimethoprim-sulfamethoxazole-resistant Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID520404	Antimicrobial activity against macrolide-resistant Streptococcus pneumoniae by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID519066	Antibacterial activity against multidrug resistant Streptococcus pneumoniae ATCC 49619 by CLSI microdilution susceptibility testing method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	Activity of the Diaminopyrimidine AR-709 against recently collected multidrug-resistant isolates of invasive Streptococcus pneumoniae from North America.
AID520410	Antimicrobial activity against macrolide-resistant Streptococcus sp. 'group A' by agar dilution method	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
AID519215	Antibacterial activity against amoxicillin-clavulanic acid resistant Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID519209	Antibacterial activity against cotrimoxazole susceptible Streptococcus pneumoniae by microdilution method	2008	Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3	In vitro activity of AR-709 against Streptococcus pneumoniae.
AID520411	Antimicrobial activity against Streptococcus pneumoniae assessed as time required to show antibiotic effect	2008	Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6	Antistreptococcal activity of AR-709 compared to that of other agents.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (66.67)	29.6817
2010's	2 (33.33)	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]

Market Indicators

Research Demand Index: 17.48

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.

Metric	This Compound (vs All)
Research Demand Index	17.48 (24.57)
Research Supply Index	2.08 (2.92)
Research Growth Index	4.37 (4.65)
Search Engine Demand Index	10.37 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (17.48)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (16.67%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	5 (83.33%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.	2.04	1	aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion	antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic
gatifloxacin Gatifloxacin: A fluoroquinolone antibacterial agent and DNA TOPOISOMERASE II inhibitor that is used as an ophthalmic solution for the treatment of BACTERIAL CONJUNCTIVITIS.. gatifloxacin : A monocarboxylic acid that is 4-oxo-1,4-dihydroquinoline-3-carboxylic acid which is substituted on the nitrogen by a cyclopropyl group and at positions 6, 7, and 8 by fluoro, 3-methylpiperazin-1-yl, and methoxy groups, respectively. Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial topoisomerase type-II enzymes.	2.04	1	N-arylpiperazine; organofluorine compound; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone	antiinfective agent; antimicrobial agent; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor
trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.	2.44	2	aminopyrimidine; methoxybenzenes	antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic
penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group.	2.73	3	penicillin allergen; penicillin	antibacterial drug; drug allergen; epitope
erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.	2.04	1	cyclic ketone; erythromycin
amoxicillin Amoxicillin: A broad-spectrum semisynthetic antibiotic similar to AMPICILLIN except that its resistance to gastric acid permits higher serum levels with oral administration.. amoxicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-(4-hydroxyphenyl)acetamido group.	2.73	3	penicillin allergen; penicillin	antibacterial drug
methotrexate [no description available]	2.03	1	dicarboxylic acid; monocarboxylic acid amide; pteridines	abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent
levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.	2.44	2	9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic	antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor
meropenem Meropenem: A thienamycin derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of bacterial infections, including infections in immunocompromised patients.. meropenem : A carbapenemcarboxylic acid in which the azetidine and pyrroline rings carry 1-hydroxymethyl and in which the azetidine and pyrroline rings carry 1-hydroxymethyl and 5-(dimethylcarbamoyl)pyrrolidin-3-ylthio substituents respectively.	2.04	1	alpha,beta-unsaturated monocarboxylic acid; carbapenemcarboxylic acid; organic sulfide; pyrrolidinecarboxamide	antibacterial agent; antibacterial drug; drug allergen
clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.	2.04	1
zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.	2.44	2	macrolide antibiotic	antibacterial drug; environmental contaminant; xenobiotic
hmr 3647 [no description available]	2.04	1
cefuroxime [no description available]	2.04	1	3-(carbamoyloxymethyl)cephalosporin; furans; oxime O-ether	drug allergen
cefotaxime Cefotaxime: Semisynthetic broad-spectrum cephalosporin.. cefotaxime : A cephalosporin compound having acetoxymethyl and [2-(2-amino-1,3-thiazol-4-yl)-2-(methoxyimino)acetyl]amino side groups.	2.04	1	1,3-thiazoles; cephalosporin; oxime O-ether	antibacterial drug; drug allergen

Condition	Relationship Strength	Studies
Infections, Pneumococcal [description not available]	2.04	1
Pneumococcal Infections Infections with bacteria of the species STREPTOCOCCUS PNEUMONIAE.	2.04	1
Community Acquired Infection [description not available]	2.04	1
Infections, Respiratory [description not available]	2.04	1
Respiratory Tract Infections Invasion of the host RESPIRATORY SYSTEM by microorganisms, usually leading to pathological processes or diseases.	2.04	1

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