FLESINOXAN, a phenylpiperazine derivative, is a selective agonist for 5-HT1A receptors. It is an antidepressant agent which clinical development was stopped.

Lodaxaprine is a chemically original compound which possesses the pharmacological properties of a potent, p.o. active anticonvulsant. In mice, lodaxaprine antagonized electroconvulsive shock and chemically induced seizures with an overall potency comparable to that of carbamazepine. In naturally photosensitive Senegalese Papio-papio baboons lodaxaprine antagonized myoclonus and cortical paroxysmal discharges. In this model lodaxaprine was approximately one-fourth as potent as phenobarbital, twice as potent as carbamazepine and 6 times more potent than sodium valproate. Lodaxaprine had been in phase II clinical trial for the treatment of epilepsy. However, this development was discontinued.

2,4,5-Trichlorophenol is a grey flake or needle-shaped solid. It is used as an intermediate in the manufacture of the herbicide 2,4,5-Trichlorophenoxyacetic Acid (2,4,5-T) and as a fungicide and bactericide. 2,4,5-trichlorophenol (triclofenol piperazine, Ranestol) is an antifungal agent, which was also used against light hookworm infections. Thirty persons who were positive for hookworm eggs in their stools were treated with 50 mg/kg of triclofenol piperazine dissolved in 5 per cent polyethylene glycol Ranestol® in soft gelatin capsules. Nineteen of these showed 77 to 100 % reduction in egg count average when compared with the pre-treatment counts. Side reactions were limited to mild and transient nausea in 23, vomiting in 7, transient abdominal cramps and headache in 2 each. 2,4,5-trichlorophenol complexed with dicyclohexylamine was used for treatment of experimental mycosis. From the mycological and clinical evaluation the conclusion can be drawn that the effect of phenol in lipophilic ointment is comparable to that of clotrimazole.

Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.

MB-07803 (VK-0612) is a potent inhibitor of fructose-1,6-bisphosphatase (FBPase). Inhibition of FBPase is an effective mechanism for lowering fasting and postprandial hyperglycemia in patients with poorly-controlled Type 2 diabetes. Viking Therapeutics is developing MB-07803 for the treatment of type 2 diabetes.

https://translate.google.ru/#view=home&op=translate&sl=en&tl=ru&text=Pyrrole%20is%20a%20five-membered%20aromatic%20heterocyclic%20compound%2C%20which%20contains%20one%20nitrogen%20atom.%20Pyrrole%20is%20a%20colorless%20volatile%20liquid%20that%20darkens%20readily%20upon%20exposure%20to%20air%20and%20is%20usually%20purified%20by%20distillation%20immediately%20before%20use.%20Due%20to%20its%20aromatic%20character%2C%20pyrrole%20is%20difficult%20to%20hydrogenate%2C%20does%20not%20easily%20react%20as%20a%20diene%20in%20Diels%E2%80%93Alder%20reactions%2C%20and%20does%20not%20undergo%20usual%20olefin%20reactions.%20Its%20reactivity%20is%20similar%20to%20that%20of%20benzene%20and%20aniline%2C%20in%20that%20it%20is%20easy%20to%20alkylate%20and%20acylate.%20Under%20acidic%20conditions%2C%20pyrroles%20polymerize%20easily%2C%20and%20thus%20many%20electrophilic%20reagents%20that%20are%20used%20in%20benzene%20chemistry%20are%20not%20applicable%20to%20pyrroles.%20Pyrrole%20and%20its%20derivatives%20(pyrroles)%20are%20widely%20used%20as%20an%20intermediate%20in%20the%20synthesis%20of%20pharmaceuticals%2C%20medicines%2C%20agrochemicals%2C%20dyes%2C%20photographic%20chemicals%2C%20perfumes%2C%20and%20other%20organic%20compounds.%20For%20example%2C%20chlorophyll%20and%20heme%20are%20the%20derivatives%20which%20are%20made%20by%20four%20pyrrole%20ring%20formation%20of%20the%20porphyrin%20ring%20system.%20Pyrrole%20is%20a%20precursor%20to%20the%20nonsteroidal%20anti-inflammatory%20drug%20tolmetin.

Fenclonine, also known as p-chlorophenylalanine, is an inhibitor of tryptophan hydroxylase, the enzyme that plays a rate-limiting role in the biosynthesis of serotonin. Fenclonine was studied for the treatment of carcinoid syndrome, but the psychological side effects, prevented for the further development for this use.