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

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Showing 911 - 920 of 1728 results

Olamufloxacin (HSR-903) is an oral fluoroquinolone antimicrobial agent which has been reported to have a potent activity against respiratory pathogens, such as Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis, Klebsiella pneumoniae, Staphylococcus aureus, Chlamydia spp. and Legionella spp., as well. Olamufloxacin inhibits DNA gyrase from the susceptible and resistant bacterial strains. It has been shown that olamufloxacin possesses a more potent antibacterial activity against potential respiratory pathogens compared with other quinolone derivatives. An oral formulation of olamufloxacin was undergoing phase III for Bacterial infections in Japan (Discontinued).
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Buciclovir is an acyclic guanosine analog with activity against herpes simplex virus (HSV). Buciclovir is phosphorylated to its triphosphate form by HSV thymidine kinase in infected cells and acts as a specific inhibitor of the viral DNA polymerase. Buciclovir inhibited DNA synthesis, not RNA synthesis, and prevented an increase in the size of newly synthesized DNA. Topical treatment initiated early after infection was efficacious, in contrast to topical treatment delayed 24 h or more. Systemic treatment of infected mice could not prevent the spread of the virus to the brain and mortality. Systemically administered buciclovir had an effect in guinea pigs, even after the delayed onset of treatment, but this effect required high doses of the drug. Buciclovir has only a limited effect against herpesvirus infections once the virus is present in the nervous systems of infected
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Sulfametomidine (or sulfamethomidine) is a sulfonamide antibacterial with a broad spectrum of activity; it’s an inhibitor of dihydrofolate reductase.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

5-iodo-2'-deoxycytidine (IBACITABINE) is an anti-herpetic agent. Experiments with a tumor mouse model have revealed, that radioiodinated compound, (131)I-5-iodo-2'-deoxycytidine was a promising single photon emission computed tomography probe for imaging proliferation.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Brivudine (trade names Zostex, Mevir, Brivir, among others) is an antiviral drug used in the treatment of herpes zoster ("shingles"). Brivudine is an analog of the nucleoside thymidine. The active compound is brivudine 5'-triphosphate, which is formed in subsequent phosphorylations by viral (but not human) thymidine kinase and presumably by the nucleoside-diphosphate kinase. Brivudine 5'-triphosphate works because it is incorporated into the viral DNA, but then blocks the action of DNA polymerases, thus inhibiting viral replication. Brivudine is used for the treatment of herpes zoster in adult patients. It is taken orally once daily, in contrast to aciclovir, valaciclovir, and other antivirals. A study has found that it is more effective than aciclovir, but this has been disputed because of a possible conflict of interest on part of the study authors. The drug is contraindicated in patients undergoing immunosuppression (for example because of an organ transplant) or cancer therapy, especially with fluorouracil (5-FU) and chemically related (pro)drugs such as capecitabine and tegafur, as well as the antimycotic drug flucytosine, which is also related to 5-FU. It has not been proven to be safe for children and pregnant or breastfeeding women. The drug is generally well tolerated. The only common side effect is nausea (in 2% of patients). Less common side effects (<1%) include a headache, increased or lowered blood cell counts (granulocytopenia, anemia, lymphocytosis, monocytosis), increased liver enzymes, and allergic reactions. Brivudine is approved for use in a number of European countries including Austria, Belgium, Germany, Greece, Italy, Portugal, Spain, and Switzerland.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (UNKNOWN)

Apicycline is a semisynthetic antibiotic. It belongs to the tetracyclines.
Status:
Possibly Marketed Outside US
Source:
NCT04260594: Phase 4 Interventional Completed 2019-nCoV
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Umifenovir or arbidol (ethyl-6-bromo-4-[(dimethylamino)methyl]-5-hydroxy-1-methyl-2-[(phenylthio)methyl]-indole-3-carboxylate hydrochloride monohydrate) is a Russian-made potent broad-spectrum antiviral with demonstrated activity against a number of enveloped and non-enveloped viruses.For both viral infections the anti-viral mechanism involves umifenovir inhibition of virus-mediated fusion with target membrane and a resulting block of virus entry into target cells. Arbidol was shown to have effects on nonspecific defense factors, on its capacity to induce interferon and activate phagocytes in particular. Arbidol-treated patients with lower baseline immunity showed improvement in immunological parameters (in the counts of CD4 and CD8 lymphocytes, B lymphocytes, in the levels of serum immunoglobulins). Arbidol produces a high preventive and therapeutical effects in influenza A and B and other acute respiratory viral infections, prevents postinfluenza complications, reduces the incidence of exacerbations of chronic diseases in postinfluenza patients. In influenza, the therapeutical efficiency of the drug appears as decreases in intoxication, the severity of catarrhal syndrome, shorter fever and disease in general. Arbidol is beneficial for patients with secondary immunodeficiency, in those with recurrent herpes infection or chronic bronchitis.
Status:
Possibly Marketed Outside US
Source:
Japan:Sorivudine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



SORIVUDINE (BV-araU) is an Anti-Herpes Virus Drugs, which was Withdrawn in 1995. Aantiviral action of BV-araU against VZV (varicella-zoster virus) and herpes simplex virus type 1 (HSV-1) is based on the inhibition of DNA synthesis in herpesvirus-infected cells.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ambruticin is a natural polyketide isolated from the myxobacteria Sorangium cellulosum. Ambruticin possesses antifungal activity and works by interfering with the osmoregulatory system by activating fungal high osmolarity glycerol (HOG) pathway. This results in an accumulation of intracellular glycerol, which in turn causes water influx and swelling of the cell. This ultimately leads to cellular leakage and cell death. Although ambruticin appeared to be the only oral agent capable of eliciting a high order of biological cure against experimental coccidioidomycosis, research support was discontinued in 1977 because this antibiotic had limited activity against Candida albicans.
Status:
Possibly Marketed Outside US
Source:
TOMIRON by Toyama
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefteram is a semisynthetic cephalosporin formulated for oral administration as the prodrug ester, cefteram pivoxil. The mechanism of action of cefteram is inhibition of bacterial cell wall synthesis. Cefteram exerts its bactericidal activity by strongly binding to penicillin-binding protein (PBP) 3, 1A, and 1Bs. The drug is available in Japan and is used for the treatment of bacterial infections.