U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 31 - 40 of 261 results

Status:
Investigational
Source:
INN:nitroclofene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nitroclofene is an anthelminthic drug. Nitroclofene is a selective inhibitor of the fumarate reductase system of the adult liver fluke at a concentration of 4 umol/L. The enzyme plays an important role in the process of energy utilization. Consequently, it possesses good flukicidal activity against both Fasciola hepatica and F. gigantica.
Status:
Investigational
Source:
INN:diamfenetide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Diamfenetide (aka diamphenethide) is a fasiolicide used in sheep. It is effective against immature flukes but with diminishing activity as the fluke ages. It has proven an effective compound for use in prophylactic programs against Fasciola hepatica. Diamphenethide is deacetylated in the host liver to an active monoamine and diamine. The amine of diamfenetide has an action which produces an elevation of malate concentration in Fasciola. Malate is an intermediary product of glucose in this parasite. It is known that dopamine, a putative neurotransmitter in Fasciola has a protective effect against diamfenetide but the mode of action of a diamfenetide has yet to be defined in greater detail.
Status:
Investigational
Source:
INN:symetine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Symetine is a benzylamine derivative patented by Eli Lilly & Co. as an antiparasitic and antispirochete agent. In preclinical models, Symetine effectively suppresses amebic liver abscess in guinea pigs.
Status:
Investigational
Source:
INN:bitoscanate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Bitoscanate is a tasteless, odorless, colorless, needle-like crystalline solid material prepared from mustard powder acid and used as an anthelmintic against nematodes, especially hookworms (Necator sp.) and Ancylostoma duodenale. Side effects reported with therapeutic use have been nausea, vomiting, diarrhea, abdominal pain or discomfort, loss of appetite, dizziness or giddiness, vertigo, weakness, headache, and an itching sensation over the body. Such side effects have most often been mild and required no treatment. Bitoscanate is classified as an extremely hazardous substance in the United States as defined in Section 302 of the U.S. Emergency Planning and Community Right-to-Know Act (42 U.S.C. 11002), and is subject to strict reporting requirements by facilities which produce, store, or use it in significant quantities.
Status:
Investigational
Source:
INN:troquidazole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Troquidazole (EGIS-4136) is a radiosensitizer. It is a nitroquinoline derivative which enhances the radiosensitivity of hamster’s ovarian cells in both normoxia and hypoxia. Misonidazole at a concentration of 5 mM exerted a radiosensitizing effect as strong as 0.5 mM EGIS-4136.
Status:
Investigational
Source:
INN:flurantel
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Flurantel is an anthelmintic agent. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:nocodazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Nocodazole is an anti-mitotic drug that has long been used as an experimental tool in cell biology. Nocodazole is known to bind with high affinity to tubulin and to inhibit microtubule assembly. The tubulin molecule is a α/β heterodimer; both α and β exist as various isotypes whose distribution and drug-binding properties are significantly different. Nocodazole has the highest affinity for αβIV and the lowest affinity for αβIII. In addition, nocodazole was investigated as an anticancer drug on xenografts model and it was revealed, that nocodazole possessed a high-affinity for the cancer-related kinases ABL, c-KIT, BRAF, and MEK, and inhibited Abl, Abl(E255K) and Abl(T315I).
Status:
Investigational
Source:
INN:broxaldine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Broxaldine, also known as brobenzoxaldine, is a dibromo derivative of quinaldine. It was used in combination with other halogenated hydroxyquinoline compound broxyquinoline (INTESTOPAN) for the treatment of intestinal amoebiasis and childhood diarrhea. In a specific ratio of 5/1, they were shown to act synergistically against several pathogens.
Status:
Investigational
Source:
INN:diminazene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Diminazene is an aromatic diamidine derived from Surfen C. Diminazene is used as aceturate salt. Diminazene is highly active against both Trypanosoma and Babesia spp. It is also of value in the treatment of theileriosis due to Theileria annulata. Diminazene has become the most commonly used therapeutic agent for trypanosomiasis in animals. It is said to be effective in canine, ovine and bovine babesiosis and, unlike some drugs, is less susceptible to relapse. It may also possess antibacterial properties. Diminazene binds to trypanosomal kDNA. This binding does not occur by intercalation but via specific interaction with sites rich in adenine-thymine (A-T) base pairs. Diminazene specifically inhibits mitochondrial type II topoisomerase in viable trypanosomes. Thus, inhibition of DNA replication may also occur via this interaction. Diminazene is extensively distributed in the body of treated animals. Residues of the compound may persist for several weeks, principally in the liver and kidneys, and also, to a lesser extent, in the gastrointestinal tract, lungs, muscle, brain and fat.
Status:
Investigational
Source:
INN:subendazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Subendazole is an antiparasitic and antispirochete agent used to treat helminth infection.