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Restrict the search for
methyl salicylate
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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.
Status:
Investigational
Source:
NCT01766817: Phase 2 Interventional Completed Idiopathic Pulmonary Fibrosis
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT04560764: Not Applicable Interventional Withdrawn Stroke
(2023)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Fluthiacet-methyl, an isourazole herbicide is applied to actively growing weeds in soybeans to control annual broadleaf weeds. Fluthiacet-methyl induced the accumulation of protoporphyrin IX in cotyledons of cotton and inhibited chlorophyll biosynthesis in cotyledons of velvetleaf and cotton.
Class (Stereo):
CHEMICAL (ACHIRAL)
Furodazole, a benzimidazole derivative was studied as an anthelmintic drug. Information about the current use of this compound is not available.
Status:
Investigational
Source:
NCT01951235: Phase 2 Interventional Completed Type 2 Diabetes Mellitus
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Imeglimin is the first in class tetrahydrotriazine‐containing oral glucose-lowering agent that has been studied in clinical trials as a possible monotherapy or add-on therapy to lower fasting plasma glucose. It is being developed as an alternative and a complement to drugs that act on insulin‐resistant organs or drugs acting on insulin secretion and β‐cell protection. When investigated in preclinical studies, Imeglimin showed that it can target insulin‐resistant organs by decreasing excessive hepatic glucose production and increasing muscle glucose uptake. It also showed a potential to restore appropriate glucose‐stimulated insulin secretion and protect β‐cells from cell death under high glucose conditions. Imeglimin acts on the liver, muscle, and the pancreas (6), three key organs involved in the pathophysiology of type 2 diabetes through suspected mechanisms targeting the mitochondria and reduced oxidative stress. Imeglimin decreases hepatic glucose production and increases muscle glucose uptake. Recently, Imeglimin demonstrated increased insulin secretion in response to glucose in diabetic patients during a hyperglycemic clamp study. In clinical trials, Imeglimin treatment for 7 days raised the insulin secretory response to glucose, improved β-cell glucose sensitivity and tended to decrease hepatic insulin extraction. Imeglimin did not affect glucagon secretion.
Class (Stereo):
CHEMICAL (RACEMIC)
Dimepranol is an immunomodulator and antiviral agent. As a mixture ingredient dimepranol was used for the treatment of recurrent local herpes simplex virus infections but results have been disappointing. As a component of inosine pranobex, dimepranol was licensed for the treatment of cell-mediated immune deficiencies associated with viral infections. In particular, for the management of: Mucocutaneous infections due to herpes simplex virus (type 1 and/or type 2); Genital warts as adjunctive therapy to podophyllin or carbon dioxide laser; Subacute sclerosing panencephalitis. Dimepranol in treatment regimens with antibiotics and inosin didn’t show any effect on PFAPA syndrome management.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Timobesone is a topical corticosteroid and thiol ester derivative with anti-inflammatory activity.
Status:
Investigational
Source:
NCT00363454: Phase 1 Interventional Completed Cancer
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.
Class (Stereo):
CHEMICAL (ACHIRAL)
Triflubazam is a 1,5-benzodiazepine derivative. The hypnotic activity of the 1,5-benzodiazepines is limited, and that this is particularly so in the case of triflubazam. Subjects reported impaired sleep with triflubazam (40 mg), and a sense of less wakefulness the morning. The effect of triflubazam may have persisted beyond the night of ingestion. No effect of triflubazam was observed on total sleep time, stage shifts in the first 6 h or latency to the first rapid eye movement period of sleep. Triflubazam has psychopharmacological properties in animals suggestive of antianxiety activity of a longer duration than that of diazepam. The metabolism of triflubazam by man is characterized by extensive N-demethylation, aromatic hydroxylation, aromatic O-methylation and dihydrodiol formation.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Tubulozole is a stereospecific microtubule inhibitor. Structurally it is related to the benzimidazole carbamates by its carbamate moiety, which is essential for the activity of both types of compounds. The compound exists as a cis-isomer called tubulozole-C (R 46 846) and as a trans-isomer called tubulozole-T. The cis-isomer appears to be a potent and specific microtubule inhibitor, the trans-isomer being inactive at 100 times higher concentrations. At low concentrations, both isomers of tubulozole (C, T) inhibit Plasmodium falciparum but only tubulozole C inhibits mammalian cells. Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules. Tubulozole-C, a new synthetic anticancer drug, interfered with the structure and function of microtubules in both interphase and mitotic cells. The activity of Tubulozole-C in experimental tumor systems can be explained partly by a direct antimitotic effect and partly by the disintegration of the normal subcellular organization of the nondividing cells. At concentrations which affect the microtubule system, tubulozole-C arrested directional migration of transformed cells and malignant invasion in a three-dimensional organ culture system. Investigations in vivo show that malignant L1210 leukemia cells are more susceptible to the antimicrotubular effect of tubulozole-C than are the normal leukocytes of the host. The trans-isomer of tubulozole (tubulozole-T, R 48 265), which has no antitumor activity in vivo, did not affect the microtubule system of cells in vitro or their capacity for directional migration or for malignant invasion.