pf 1022a profile

PF 1022A: structure given in first source; isolated from Mycelia Sterilia [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	159590
CHEMBL ID	186158
CHEBI ID	180461
SCHEMBL ID	14030033
MeSH ID	M0203516

Synonym
CHEBI:180461
pf1022a
cyclo(d-2-hydroxypropanoyl-n-methyl-l-leucyl-3-phenyl-d-2-hydroxypropanoyl-n-methyl-l-leucyl-d-2-hydroxypropanoyl-n-methyl-l-leucyl-3-phenyl-d-2-hydroxypropanoyl-n-methyl-l-leucyl)
pf 1022
cyclo(d-2-hydroxypropanoyl-n-methyl-l-leucyl-3-phenyl-d-2-hydroxypropanoyl-n-metrhyl-l-leucyl-d-2-hydroxypropanoyl-n-methyl-l-leucyl-3-phenyl-d-2-hydroxypropanoyl-n-methyl-l-leucyl)
pf 1022a
pf-1022a
CHEMBL186158
133413-70-4
(3s,6r,9s,12r,15s,18r,21s,24r)-6,18-dibenzyl-4,10,12,16,22,24-hexamethyl-3,9,15,21-tetrakis(2-methylpropyl)-1,7,13,19-tetraoxa-4,10,16,22-tetrazacyclotetracosane-2,5,8,11,14,17,20,23-octone
ec 444-350-6
cyclo(d-lactyl-l-n-methylleucyl-d-3-phenyllactyl-l-n-methylleucyl-d-lactyl-l-n-methylleucyl-d-3-phenyllactyl-l-n-methylleucyl)
(3s,6r,9s,12r,15s,18r,21s,24r)-6,18-dibenzyl-3,9,15,21-tetraisobutyl-4,10,12,16,22,24-hexamethyl-1,7,13,19-tetraoxa-4,10,16,22-tetraazacyclo-tetracosane-2,5,8,11,14,17,20,23-octaone
HY-12361
CS-3377
SCHEMBL14030033
AKOS030526415
pf1022
EX-A1669
MS-31776
DTXSID201335234
cyclo[n(me)leu-d-oala-n(me)leu-d-ophe-n(me)leu-d-oala-n(me)leu-d-ophe]
GLXC-26269

Excerpt	Reference	Relevance
"PF 1022A is a member of a new class of cyclic depsipeptides with antiparasitic activity. "	( In vivo activities of the new anthelmintic depsipeptide PF 1022A. Harder, A; Kalbe, J; Mencke, N; Schnieder, T; von Samson-Himmelstjerna, G, 2000)	2

Excerpt	Reference	Relevance
"To enhance the bioavailability of PF1022A (cyclo(D-lactyl-L-N-methylleucyl-D-3-phenyllactyl-L-N-met hylleucyl-D-lactyl-L-N-methylleucyl-D-3-phenyllactyl-L-N- methylleucyl)), a newly developed antinematode drug, we examined whether the new drug has polymorphism or not."	( Effects of amorphous and polymorphs of PF1022A, a new antinematode drug, on Angiostrongylus costaricensis in mice. Hashimoto, H; Kachi, S; Terada, M, 1998)	0.3

Class	Description
cyclooctadepsipeptide	A cyclodepsipeptide consisting of eight hydroxy- or amino-acids joined in sequence to give a macrocycle. They form the basis of a relatively new class of anthelmintic agents with a novel mechanism of action.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (8)

Assay ID	Title	Year	Journal	Article
AID203794	Anthelmintic activity against Haemonchus contortus nematode in sheep was determined as a function of >/= 90% egg reduction after p.o. administration	1998	Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9	PF1022A--a novel anthelmintic cyclooctadepsipeptide. Modification and exchange of the N-methyl leucine residues.
AID251466	anthelmintic activity as the percent reduction in faecal egg count in sheep infected with 5000 Haemonchus contortus L3 larvae at 0.1 mg/kg	2004	Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24	Chimeric cyclodepsipeptides as mimetics for the anthelmintic PF1022A.
AID251000	anthelmintic activity as the eggs per gram of faeces in sheep infected with 5000 Haemonchus contortus L3 larvae at 0.01 mg/kg	2004	Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24	Chimeric cyclodepsipeptides as mimetics for the anthelmintic PF1022A.
AID250998	anthelmintic activity as the eggs per gram of faeces in sheep infected with 5000 Haemonchus contortus L3 larvae at 0.1 mg/kg	2004	Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24	Chimeric cyclodepsipeptides as mimetics for the anthelmintic PF1022A.
AID203793	Anthelmintic activity against Haemonchus contortus nematode in sheep was determined as a function of >/= 90% egg reduction after i.v. administration	1998	Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9	PF1022A--a novel anthelmintic cyclooctadepsipeptide. Modification and exchange of the N-methyl leucine residues.
AID251467	anthelmintic activity as the percent reduction in faecal egg count in sheep infected with 5000 Haemonchus contortus L3 larvae at 0.01 mg/kg	2004	Bioorganic & medicinal chemistry letters, Dec-20, Volume: 14, Issue:24	Chimeric cyclodepsipeptides as mimetics for the anthelmintic PF1022A.
AID94929	Percent reduction of Haemonchus contortus in immunosuppressed jird (Meriones unguiculatus) when CDP administered 0.11 mg/jird orally	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Restricted conformation analogues of an anthelmintic cyclodepsipeptide.
AID23462	Partition coefficient in n-octanol/ water system at pH= 7.0	1998	Bioorganic & medicinal chemistry letters, May-05, Volume: 8, Issue:9	PF1022A--a novel anthelmintic cyclooctadepsipeptide. Modification and exchange of the N-methyl leucine residues.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	9 (27.27)	18.2507
2000's	19 (57.58)	29.6817
2010's	5 (15.15)	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]

Publication Type	This drug (%)	All Drugs (%)
Trials	1 (3.03%)	5.53%
Reviews	5 (15.15%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	27 (81.82%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
lactic acid Lactic Acid: A normal intermediate in the fermentation (oxidation, metabolism) of sugar. The concentrated form is used internally to prevent gastrointestinal fermentation. (From Stedman, 26th ed). 2-hydroxypropanoic acid : A 2-hydroxy monocarboxylic acid that is propanoic acid in which one of the alpha-hydrogens is replaced by a hydroxy group.	2.05	1	0	2-hydroxy monocarboxylic acid	algal metabolite; Daphnia magna metabolite
phaclofen phaclofen: peripheral & central baclofen & GABA antagonist; structure given in first source	1.99	1	0	organophosphate oxoanion; zwitterion
albendazole [no description available]	2.06	1	0	aryl sulfide; benzimidazoles; benzimidazolylcarbamate fungicide; carbamate ester	anthelminthic drug; microtubule-destabilising agent; tubulin modulator
baclofen [no description available]	1.99	1	0	amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound	central nervous system depressant; GABA agonist; muscle relaxant
piperazine [no description available]	2	1	0	azacycloalkane; piperazines; saturated organic heteromonocyclic parent	anthelminthic drug
chloramphenicol Amphenicol: Chloramphenicol and its derivatives.	2.02	1	0	C-nitro compound; carboxamide; diol; organochlorine compound	antibacterial drug; antimicrobial agent; Escherichia coli metabolite; geroprotector; Mycoplasma genitalium metabolite; protein synthesis inhibitor
leucine Leucine: An essential branched-chain amino acid important for hemoglobin formation.. leucine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isobutyl group.	1.99	1	0	amino acid zwitterion; L-alpha-amino acid; leucine; proteinogenic amino acid; pyruvate family amino acid	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; plant metabolite; Saccharomyces cerevisiae metabolite
thiazoles [no description available]	3.1	1	0	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
levamisole Levamisole: An antihelminthic drug that has been tried experimentally in rheumatic disorders where it apparently restores the immune response by increasing macrophage chemotaxis and T-lymphocyte function. Paradoxically, this immune enhancement appears to be beneficial in rheumatoid arthritis where dermatitis, leukopenia, and thrombocytopenia, and nausea and vomiting have been reported as side effects. (From Smith and Reynard, Textbook of Pharmacology, 1991, p435-6). levamisole : A 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole that has S configuration. It is used (generally as the monohydrochloride salt) to treat parasitic worm infections in pigs, sheep and cattle and was formerly used in humans as an adjuvant to chemotherapy for the treatment of various cancers. It is also widely used as an adulterant to coccaine.	3.83	2	1	6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b][1,3]thiazole	antinematodal drug; antirheumatic drug; EC 3.1.3.1 (alkaline phosphatase) inhibitor; immunological adjuvant; immunomodulator
nitazoxanide nitazoxanide: a 5-nitrothiazolyl derivative used for a broad range of intestinal parasitic infections including CRYPTOSPORIDIUM and GIARDIA; it is a redox-active nitrothiazolyl-salicylamide prodrug	3.1	1	0	benzamides; carboxylic ester
bay 44-4400 Bay 44-4400: a semisynthetic derivative of anthelminitic cyclodepsipeptide; PF1022A. emodepside : A cyclooctadepsipeptide consisting of D-lactoyl, N-methyl-L-leucyl, 3-[4-(4-morpholinyl)phenyl]-D-lactoyl, N-methyl-L-leucyl, D-lactoyl, N-methyl-L-leucyl, 3-[4-(4-morpholinyl)phenyl]-D-lactoyl, and N-methyl-L-leucyl residues joined in sequence to give a 24-membered macrocycle. An anthelmintic, it is used with praziquantel for the treatment and control of hookworm, roundworm and tapeworm infections in cats.	6.28	6	1	cyclooctadepsipeptide; semisynthetic derivative	antinematodal drug
dextrothyroxine [no description available]	5.2	3	1
moxidectin moxidectin: family of macrolide antibiotics with insecticidal & acaricidal activity	3.1	1	0
avermectin avermectin: produced by actinomycete, Streptomyces avermitilis; structure; see also records for specific avermectins. avermectin : Any of the macrolides obtained as fermentation products from the bacterium Streptomyces avermitilis and consisting of a 16-membered macrocyclic backbone that is fused both benzofuran and spiroketal functions and contains a disaccharide substituent. They have significant anthelmintic and insecticidal properties.	3.1	1	0

Condition	Relationship Strength	Studies	Trials
Haemonchiasis Infection with nematodes of the genus HAEMONCHUS, characterized by digestive abnormalities and anemia similar to that from hookworm infestation.	2.69	3	0
Infections, Nematomorpha [description not available]	3.36	2	0
Helminthiasis Infestation with parasitic worms of the helminth class.	3.36	2	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	2.05	1	0
Angiostrongylus Infections [description not available]	2.7	3	0
Helminthiasis, Animal Infestation of animals with parasitic worms of the helminth class. The infestation may be experimental or veterinary.	4.49	5	0
Bovine Diseases [description not available]	5	3	1
Infections, Nematode [description not available]	5.7	4	1
Ovine Diseases [description not available]	5	3	1
Canine Diseases [description not available]	2	1	0
Equine Diseases [description not available]	2	1	0
Rodent Diseases Diseases of rodents of the order RODENTIA. This term includes diseases of Sciuridae (squirrels), Geomyidae (gophers), Heteromyidae (pouched mice), Castoridae (beavers), Cricetidae (rats and mice), Muridae (Old World rats and mice), Erethizontidae (porcupines), and Caviidae (guinea pigs).	2	1	0
Human Trichinellosis [description not available]	2	1	0
Ascaridida Infections Infections with nematodes of the order ASCARIDIDA.	2	1	0
Trichinellosis An infection with TRICHINELLA. It is caused by eating raw or undercooked meat that is infected with larvae of nematode worms TRICHINELLA genus. All members of the TRICHINELLA genus can infect human in addition to TRICHINELLA SPIRALIS, the traditional etiological agent. It is distributed throughout much of the world and is re-emerging in some parts as a public health hazard and a food safety problem.	2	1	0
Trichostrongylosis Infestation with nematode worms of the genus TRICHOSTRONGYLUS. Man and animals become infected by swallowing larvae, usually with contaminated food or drink, although the larvae may penetrate human skin.	2	1	0
Parasitemia The presence of parasites (especially malarial parasites) in the blood. (Dorland, 27th ed)	2	1	0
Elaeophoriasis [description not available]	2	1	0
Filariasis Infections with nematodes of the superfamily FILARIOIDEA. The presence of living worms in the body is mainly asymptomatic but the death of adult worms leads to granulomatous inflammation and permanent fibrosis. Organisms of the genus Elaeophora infect wild elk and domestic sheep causing ischemic necrosis of the brain, blindness, and dermatosis of the face.	2	1	0

pf 1022a

Description

Cross-References

Synonyms (23)

Research Excerpts

Overview

Bioavailability

Drug Classes (1)

Bioassays (8)

Research

Studies (33)

Market Indicators

Research Demand Index: 10.83

Study Types

pf 1022a

Description

Cross-References

Synonyms (23)

Research Excerpts

Overview

Bioavailability

Drug Classes (1)

Bioassays (8)

Research

Studies (33)

Market Indicators

Research Demand Index: 10.83

Study Types

Related Drugs (14)

Related Conditions (19)