{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
FENLEUTON is a potent, reversible and selective inhibitor of 5-lipoxygenase with IC50 values ranging from 80 to 1100 nM. It was studied for potential use in veterinary medicine to treat chronic obstructive pulmonary disease in horses.
Status:
Investigational
Source:
INN:dichloroxylenol [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Dichloroxylenol is a bactericide, preservative and deodorant. It is often used in the preparation of antiseptic and deodorant lotions and bath preparations. Dichloroxylenol also showed slightly greater activity against S. aureus Oxoid 701/1 Lot 610254 than against Escherichia coli and Salmonella typhi, indicating a probable role for cell wall in the susceptibility of bacteria to dichloroxylenol. The efficacy of either povidone-iodine (Betadine) or dichloroxylenol (Septocid) intrauterine infusions on the treatment of endometritis and/or cervicitis in cows was examined. The recovery and conception rates obtained after Betadine treatment were better than those obtained after Septocid. Moreover, healthy cows and those inseminated before post-partum day 180, having no more than 4-7 previous services, responded well to either Betadine or Septocid treatment.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Obatoclax (GX15-070) is a novel BH3 mimetic pan Bcl-
2 inhibitor. The clinically studied formulation is as obatoclax mesylate (Box 1), a salt. It is only under study as an intravenous preparation. It functions to block BH3-mediated binding of Bcl-2, Bcl-XL, Mcl-1 and A1 to Bax and Bak. Bax and Bak thus are unopposed and able to dimerize to allow initiation of intrinsic apoptosis. Preclinically, obatoclax has been shown to reverse inhibition of Bax or Bak by Bcl-2, Bcl-XL, Bcl-w and Mcl-1. Obatoclax was discovered by Gemin X, which was acquired by Cephalon, which has since been acquired by Teva Pharmaceuticals. Obatoclax had been in phase III clinical trials by Gemin X Biotechnologies (subsidiary of Teva) for the treatment of non-small lung cancer (NSCLC).
The compound received orphan drug designation in the U.S. in 2004 for the treatment of chronic lymphocytic leukemia (CLL). However, Teva discontinued the development of obatoclax in 2013.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Peretinoin is an orally available, acyclic retinoid with potential antineoplastic and chemopreventive activities. Peretinoin binds to and activates nuclear retinoic acid receptors (RAR), which in turn recruit coactivator proteins and promote, with other transcriptional complexes, the transcription of target genes. As a result, this agent may modulate the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis of both normal and tumor cells. Peretinoin inhibits post-therapeutic recurrence of hepatocellular carcinoma via unclear mechanisms. The European Commission granted Orphan Drug designation for Kowa's peretinoin to treat hepatocellular carcinoma (HCC).
Status:
Investigational
Source:
NCT01644682: Phase 3 Interventional Completed Cost-effective and Sustainable Vector Control Methods Will be Established to Reduce VL in India, Bangladesh and Nepal
(2012)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Class (Stereo):
CHEMICAL (ACHIRAL)
Cinnamaverine is an aminodiphenylacrylate, a smooth muscle relaxant and antispasmodic with some local anesthetic activity.
Class (Stereo):
CHEMICAL (MIXED)
Difebarbamate is a barbituric acid derivative. It is a hypnotic drug. Difebarbamate is a component of Tetrabamate complex, which was introduced for clinical use in the treatment of alcoholism and various types of drug dependence. After oral administration of difebarbamate, the compound was completely metabolized and three metabolic pathways were observed: oxidation of Cl of the n-butyl chain which leads to the oxygen dealkylation; hydrolysis of the carbamoyloxy group; oxidation of the benzene ring in position 4. Tetrabamate can induce hepatotoxicity, probably due to an idiosyncratic metabolic mechanism. Despite restrictions on its indications and treatment duration introduced in 1997, cases of severe liver damage have continued to be notified in France.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Dazoxiben is a selective inhibitor of thromboxane synthetase (IC50 3 nM), an enzyme that converts the endo-peroxide PGH2 into thromboxane A2, which is a potent vasoconstrictor and platelet aggregating agent. Dazoxiben has demonstrated efficacy in some clinical trial for the treatment of Raynaud's syndrome, an ischaemic condition manifested by the pallor of affected digits. In subsequent studies, however, no significant effect of dazoxiben was found. Dazoxiben was also evaluated in patients with sepsis, adult respiratory distress syndrome, stable angina, and other conditions.
Class (Stereo):
CHEMICAL (ACHIRAL)
Dazoquinast is an imidazoquinoxaline derivative with antiallergic properties, developed by the British company Roussel Laboratories Ltd. Dazoquinast inhibited the IgE-mediated passive cutaneous anaphylaxis in rats passively sensitized to ovalbumen after intravenous and oral administration with ED50s of 0.073 and 0.13 mg/kg respectively.
Status:
Investigational
Source:
INN:loreclezole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Loreclezole was found to be active in all animal models of seizures, whether a genetic model of reflex epilepsy was used or models where seizures were elicited by chemical or electrical stimulation. In addition, loreclezole was active against both TON and CLON seizures and increased the threshold for behavioral as well as EEG seizures. Loreclezole has a very rapid onset of action and a duration of the activity, which in certain tests last for more than 24 hr. Chronic administration for 5-7 days did not lead to tolerance to the anticonvulsant action of loreclezole. Loreclezole potentiates gamma-aminobutyric acid (GABA) type A receptor function, by interacting with a specific allosteric modulatory site on receptor beta-subunits. It also acts as a negative modulator at a novel regulatory site, enhancing GABAA receptor sensitization. Inhibits homomeric ρ1 GABAC receptors.
