Compounds > cpzen-45
Page last updated: 2024-11-13

cpzen-45

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Description

CPZEN-45: caprazamycin derivative; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID67419859
CHEMBL ID4469883
SCHEMBL ID2468833
MeSH IDM0587863

Synonyms (6)

Synonym
(2s)-2-[(s)-[(2s,3r,4s,5r)-5-(aminomethyl)-3,4-dihydroxy-tetrahydrofuran-2-yl]oxy-[(2s,3s,4r,5r)-5-(2,4-dioxopyrimidin-1-yl)-3,4-dihydroxy-tetrahydrofuran-2-yl]methyl]-n-(4-butylphenyl)-1,4-dimethyl-3-oxo-2,7-dihydro-1,4-diazepine-5-carboxamide
cpzen-45
SCHEMBL2468833
CHEMBL4469883 ,
bdbm50526647
uridine, 5'-o-(5-amino-5-deoxy-.beta.-d-ribofuranosyl)-5'-c-((2s)-5-(((4-butylphenyl)amino)carbonyl)-2,3,4,7-tetrahydro-1,4-dimethyl-3-oxo-1h-1,4-diazepin-2-yl)-, (5's)-

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
" CPZEN-45 is a novel anti-tubercular drug that has poor oral bioavailability but has shown promise when administered via inhalation."( Optimization and Scale Up of Spray Dried CPZEN-45 Aerosol Powders for Inhaled Tuberculosis Treatment.
Barreda, AP; Daily, S; Durham, PG; Hickey, AJ; Maloney, SE; Mecham, JB; Moody, C; Severynse-Stevens, D; Simpson, C; Sittenauer, JM; Stewart, IE; Stowell, GW; Williams, MD, 2022)		0.72
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (29)

Assay IDTitleYearJournalArticle
AID1603562Antibacterial activity against methicillin resistant Staphylococcus aureus No. 52019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603555Inhibition of WecA in Mycobacterium smegmatis2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603530Antibacterial activity against Klebsiella pneumoniae after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603561Antibacterial activity against Staphylococcus aureus FDA209P2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603529Antibacterial activity against Escherichia coli after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603565Antibacterial activity against Streptococcus pneumoniae S-2232019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603564Antibacterial activity against Enterococcus faecalis NCTC1221032019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603526Antibacterial activity against Mycobacterium intracellulare after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603515Antibacterial activity against Mycobacterium smegmatis after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603553Inhibition of TagO in Bacillus subtilis2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603559Antibacterial activity against Mycobacterium avium subsp. avium ATCC 252912019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603523Antibacterial activity against Mycobacterium tuberculosis after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603516Antibacterial activity against Staphylococcus aureus after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603563Antibacterial activity against Enterococcus faecalis JCM 58032019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603533Inhibition of MraY in Bacillus subtilis2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603528Antibacterial activity against Mycobacterium phlei after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1724069Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2020Bioorganic & medicinal chemistry, 09-15, Volume: 28, Issue:18
Uridine natural products: Challenging targets and inspiration for novel small molecule inhibitors.
AID1603519Antibacterial activity against Bacillus subtilis after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603525Antibacterial activity against Mycobacterium avium after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603556Inhibition of WecA in Mycobacterium tuberculosis mc2 62302019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603554Inhibition of WecA in Mycobacterium tuberculosis2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603524Antibacterial activity against Mycobacterium bovis after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603557Antibacterial activity against Mycobacterium tuberculosis H37Rv2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603558Antibacterial activity against Mycobacterium intracellulare JCM36842019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1696844Inhibition of Mycobacterium tuberculosis WecA2020Journal of medicinal chemistry, 10-08, Volume: 63, Issue:19
DPAGT1 Inhibitors of Capuramycin Analogues and Their Antimigratory Activities of Solid Tumors.
AID1603518Antibacterial activity against methicillin resistant Staphylococcus aureus after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603566Antibacterial activity against Streptococcus pneumoniae CR-82019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603527Antibacterial activity against Mycobacterium vaccae after 20 hrs by NCCLS-based two-fold broth dilution method2019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
AID1603560Antibacterial activity against Mycobacterium avium subsp. paratuberculosis ATCC 430152019European journal of medicinal chemistry, Jun-01, Volume: 171Caprazamycins: Promising lead structures acting on a novel antibacterial target MraY.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's8 (66.67)24.3611
2020's4 (33.33)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews4 (33.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
nitromide
nitromide: antibacterial agent for prevention & treatment of Salmonella pullorum infections in chickens & turkeys & for fowl typhoid & paratyphoid; used in feed; structure		3.2310
uridine
[no description available]		3.2310uridinesdrug metabolite;
fundamental metabolite;
human metabolite
adamantane
Adamantane: A tricyclo bridged hydrocarbon.		3.2310adamantanes;
polycyclic alkane
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		3.23101,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
alpha-aminopyridine
alpha-aminopyridine: RN given refers to parent cpd; structure in Merck Index, 9th ed, #485. aminopyridine : Compounds containing a pyridine skeleton substituted by one or more amine groups.		3.2310
azomycin
azomycin: RN given refers to parent cpd with specified locant; structure		3.2310C-nitro compound;
imidazoles		antitubercular agent
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		2.2510organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
4-cyclohexylaniline
4-cyclohexylaniline: analgesic activity		3.3510
sq-641
SQ-641: a MurX inhibitor with antitubercular activity; structure in first source		3.2310
sq 109
N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine: has antitubercular activity		3.2310
bedaquiline
bedaquiline: a diarylquinoline Antitubercular Agent. bedaquiline : A quinoline-based antimycobacterial drug used (as its fumarate salt) for the treatment of pulmonary multi-drug resistant tuberculosis by inhibition of ATP synthase, an enzyme essential for the replication of the mycobacteria.		3.2310aromatic ether;
naphthalenes;
organobromine compound;
quinolines;
tertiary alcohol;
tertiary amino compound		antitubercular agent;
ATP synthase inhibitor
capuramycin
capuramycin: from Streptomyces griseus 446-S3; structure given in first source		2.2510
opc-67683
OPC-67683: an antitubercular agent		3.2310piperidines
caprazamycin b
caprazamycin B: anti-tuberculosis lipo-nucleoside antibiotic from Streptomyces sp.; structure in first source		4.2420
minocycline
Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.		3.2310
tigecycline
[no description available]		3.2310
pbtz169
macozinone: an antitubercular agent; structure in first source		3.2310
leucinostatin a
leucinostatin A: isolated from Penicillium lilacinum; A 20668 A,B,& C are polypeptide antibiotics that inhibit phosphorylation of ADP, Mg ATPase; RN given refers to leucinostatin A		3.3110
ConditionIndicatedRelationship StrengthStudiesTrials
Benign Neoplasms
[description not available]		02.2510
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.2510
Disease Models, Animal
Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.		02.4110
Pulmonary Consumption
[description not available]		02.4110
Tuberculosis, Pulmonary
MYCOBACTERIUM infections of the lung.		02.4110
Koch's Disease
[description not available]		02.8730
Tuberculosis
Any of the infectious diseases of man and other animals caused by species of MYCOBACTERIUM TUBERCULOSIS.		02.8730
Tuberculosis, Drug-Resistant
[description not available]		02.0810
Tuberculosis, Multidrug-Resistant
Tuberculosis resistant to chemotherapy with two or more ANTITUBERCULAR AGENTS, including at least ISONIAZID and RIFAMPICIN. The problem of resistance is particularly troublesome in tuberculous OPPORTUNISTIC INFECTIONS associated with HIV INFECTIONS. It requires the use of second line drugs which are more toxic than the first line regimens. TB with isolates that have developed further resistance to at least three of the six classes of second line drugs is defined as EXTENSIVELY DRUG-RESISTANT TUBERCULOSIS.		02.0810
Atypical Mycobacterial Infection, Disseminated
[description not available]		03.0410