{{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?
Class (Stereo):
CHEMICAL (ACHIRAL)
Iosulamide is triiodobenzoic acid derivative patented by Sterling Drug Inc as an X-ray contrast agent. Iosulamide shows clear advantages in animal tests over meglumine iodipamide. The intravenous toxicity of Iosulamide meglumine is considerably lower than that of iodipamide (Cholografin) in the mouse and rat. Studies of biliary and urinary excretion patterns indicate Iosulamide is rapidly excreted compared to iodipamide, while at the same time providing equal concentrations in bile. More efficient blood to bile clearance rate and a shorter blood half-life for Iosulamide may account for the lower circulating blood levels and rapid total excretion compared to iodipamide. Iosulamide's rapid blood-bile clearance coupled with its extremely low toxicity may allow rapid administration of high doses, affording superior visualization and safety compared to iodipamide.
Class (Stereo):
CHEMICAL (RACEMIC)
Carbenzide is hydrazine derivative with the high antidepressant activity and low toxicity patented by pharmaceutical company Warner-Lambert Pharmaceutical Co. Carbenzide acts via monoamine oxidase (MAO) inhibition and increase the level of brain serotonin.
Status:
Investigational
Source:
NCT01670357: Phase 2 Interventional Completed Dry Eye Syndrome
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Recoflavone (DA-6034) is a synthetic derivative of eupatillen (flavone derivative). It has antioxidant properties, and anti-inflammatory effects in inflammatory bowel disease (IBD). Although the exact mechanism is still unknown, recoflavone may decrease intestinal permeability in an indomethacin-induced intestinal injury model via the extracellular signal-regulated kinase pathway. In a phase I clinical trial, recoflavone was well tolerated and minimally absorbed in healthy volunteers. In other (phase II and III) clinical trials, the drug has been evaluated for use in treatment of gastritis (phase III), dry eyes, and Crohn’s disease (discontinued).
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Buthalital is a barbiturate derivative which was under development as a short-acting anesthetic. However, development was discontinued, perhaps due to its extremely rapid elimination rate] and buthalital sodium was never marketed.
Status:
Investigational
Source:
NCT03897036: Phase 1 Interventional Active, not recruiting Carcinoma, Basal Cell
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Silmitasertib (CX-4945) is a potent and selective orally bioavailable small molecule inhibitor of Casein kinase II (CK2). The antiproliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. CX-4945 caused cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells. When administered orally in murine xenograft models, CX-4945 was well tolerated and demonstrated robust antitumor activity. Senhwa Biosciences is developing silmitasertib for the treatment of cholangiocarcinoma, other solid tumours, Castleman's disease (giant lymph node hyperplasia) and multiple myeloma. The compound was originally developed by Cylene Pharmaceuticals. Phase Ib/II development is underway in the US and South Korea for the treatment of cholangiocarcinoma, and development in the remaining indications is at the phase I stage. As at July 2016, no recent reports of development had been identified for phase-I development in Giant-lymph-node-hyperplasia in USA (PO, Capsule), phase-I development in Multiple-myeloma in USA (PO, Capsule), phase-I development in Solid-tumours (Late-stage disease) in USA (PO, Capsule).
Class (Stereo):
CHEMICAL (RACEMIC)
Serazapine (CGS15040) is an anxiolytic agent. It is structurally novel 5-HT2 receptor antagonist. Preliminary preclinical findings indicated an anticonflict effect in a behavioral suppression test, and two preliminary investigations in volunteers also suggested anxiolytic potential. In the first of these studies serazapine resembled diazepam, a reference anxiolytic drug, electroencephalographically. Additionally, in a test of psychogenic stress in volunteers it reduced cardiac output.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Lodelaben (SC-39026) is a human neutrophil elastase inhibitor. Its inhibition of elastase is reversible and noncompetitive at low concentrations. Inhibition is "mixed" at higher inhibitor concentrations. SC-39026 is inactive against hog pancreatic elastase, bovine alpha-chymotrypsin and Pseudomonas aeruginosa elastase, but does inhibit human neutrophil cathepsin G. Lodelaben was developed as antiarthritic agent and tested as adjunct to emphysema therapy. Monocrotaline-injected rats given SC-39026 had significantly lower mean pulmonary artery pressure than those given vehicle, and this correlated with a significant reduction in the number of abnormally muscularized arteries at alveolar wall level. SC-39026 did not significantly reduce monocrotaline-induced medial hypertrophy of muscular arteries, endothelial injury, and associated subendothelial edema. Lodelaben reduces endotoxin-induced lung dysfunction in awake sheep.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
ISALMADOL is an analgesic agent.
Status:
Investigational
Source:
NCT03703388: Not Applicable Interventional Completed Healthy
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Arctigenin is a plant lignan extracted from Arctium lappa that has been shown to have estrogenic properties. In ER-positive MCF-7 cells, arctigenin efficiently inhibited 12-O-tetradecanoylphorbol-13-acetate (TPA)-induced cell migration and invasion. Arctigenin confers anti-metastatic effects by inhibiting MMP-9 and uPA via the Akt, NF-κB and MAPK signaling pathways on breast cancer, regardless of ER expression. Intake of arctigenin could be an effective supplement for breast cancer patients. Arctigenin is a phenylpropanoid dibenzylbutyrolactone lignan compound possessing antitumor, anti-inflammatory, anti-influenza, antioxidant, antibacterial, and hypoglycaemic activities. Arctigenin exhibited significant antiproliferative activity against CCRF-CEM cells after 72 h treatment with IC50 values of 1.21 ± 0.15 um. It arrested CCRF-CEM cells in the S phase. It induced apoptosis in CCRF-CEM cells in a concentration- and time-dependent manner. Arctigenin is a good candidate for the development of novel agents against T-cell lymphoma. Arctigenin has been found to act as an agonist of adiponectin receptor 1 (AdipoR1). Arctigenin is an antagonist of MR and effectively decreases the Na/K-ATPase 1 gene expression, thus highlighting its potential as an anti-hypertensive drug lead compound.
Class (Stereo):
CHEMICAL (RACEMIC)
Profadol is a pyrrolidine derivative patented in the 1960s by pharmaceutical company Parke-Davis as opioid analgesic. Profadol acts as a mixed agonist-antagonist of the μ-opioid receptor and in preclinical studies, Profadol precipitates abstinence in morphine-dependent monkeys and can reverse pethidine- induced narcosis in nondependent monkeys. In morphine-dependent human subjects, Profadol was also found to pre¬cipitate acute abstinence syndromes, with a potency 40 to 50 times less than that of nalorphine. Profadol, unlike other morphine-antagonists, does not produce nalorphine-like subjective effects. Over a fourfold range of doses, this drug was found to produce subjective effects indistinguishable from those of morphine. Also unlike other morphine-antagonists, profadol is quite active on the "classical" rodent tests for analgesia. It is about 1.3 times as potent as pethidine on the mouse hot-plate test, and about four times as potent on the rat tail-pressure test.
