Pyrimidines

Monastrol is a cell-permeable small molecule inhibitor discovered by Thomas U. Mayer in the lab of Tim Mitchison. Monastrol was shown to inhibit the kinesin-5 (also known as KIF11, Kinesin Eg5), a motor protein important for spindle bipolarity.

4-Thiouridine is an atypical nucleoside formed with the 4-thiouracil base found in transfer RNA (tRNA). Its biosynthesis has been determined.

Allithiamine (thiamine allyl disulfide or TAD) is a lipid-soluble form of vitamin B1 which was discovered in garlic (Allium sativum) in the 1950s along with its homolog prosultiamine. They were both investigated for their ability to treat Wernicke–Korsakoff syndrome and beriberi better than thiamine.

Copanlisib, sold under the brand name Aliqopa, is a medication used for the treatment of adults experiencing relapsed follicular lymphoma who have received at least two prior systemic therapies.

Acefurtiamine (INN) is a vitamin B1 analog in a manner similar to the GABAergic activity of the thiamine derivative clomethiazole. It functions as an analgesic agent at sufficient doses.

4-Thiouracil is a heterocyclic organic compound having a pyrimidine skeleton. It is a derivative of the nucleobase uracil with a sulfur instead of oxygen in position 4. It is found naturally in the 4-thiouridine nucleoside.

Avitriptan (; development code BMS-180048) is an antimigraine drug of the triptan family which was never marketed. It acts as a serotonin 5-HT1B and 5-HT1D receptor agonist. The drug reached phase 3 clinical trials prior to the discontinuation of its development.

Oxyphencyclimine is a muscarinic receptor antagonist, given orally to treat peptic ulcer disease and gastrointestinal spasms. It has antispasmodic and antimotility properties.

5-Hydroxyuracil is an oxidized form of cytosine that is produced by the oxidative deamination of cytosines by reactive oxygen species. It does not distort the DNA molecule and is bypassed by replicative DNA polymerases. It can miscode for adenine and is potentially mutagenic.

N1-Methylpseudouridine (abbreviated m1Ψ) is a natural archaeal tRNA component, and "hypermodified" pyrimidine nucleoside used in biochemistry and molecular biology for in vitro transcription and is found in the SARS-CoV-2 mRNA vaccines tozinameran (Pfizer–BioNTech) and elasomeran (Moderna).

Nifekalant (INN) is a class III antiarrhythmic agent approved in Japan for the treatment of arrhythmias and ventricular tachycardia. It has the brand name Shinbit.

Mobocertinib, sold under the brand name Exkivity, is used for the treatment of non-small cell lung cancer.

Tezosentan is a non-selective ETA and ETB receptor antagonist. It acts as a vasodilator and was designed by Actelion as a therapy for patients with acute heart failure. However, studies showed that tezosentan did not improve dyspnea or reduce the risk of fatal or nonfatal cardiovascular events.

chemical compound

Prazitone (, ; developmental code name AGN-511) is a barbiturate derivative described as an antidepressant which was developed in the 1960s. Unlike most barbiturates, it has little or no sedative effects, instead acting as a non-sedating anxiolytic and antidepressant. The dosage range in humans is around 200–600 mg, although higher doses have been used in trials for the treatment of depression associated with Parkinson's disease.

chemical compound

TC-1827 is an orally active, selective agonist of the α4β2 nicotinic receptors. Administration of TC-1827 improved memory and learning in a variety of rodents and increased long-term potentiation in hippocampal slices. In addition, the compound was without significant cardiovascular side effects, except for a small, transient rise in arterial blood pressure. The pro-cognitive effects of TC-1827 last much longer than the short half-life (0.2–1.0 hours) would suggest.

Tolimidone (CP-26154; MLR-1023) is a compound which was discovered by scientists at Pfizer, was found to stimulate secretion of gastric mucosa, and was in development by Pfizer as a drug candidate to treat gastric ulcers but was abandoned. After the patent on the compound expired, scientists at the company Melior Discovery identified it as a potential drug candidate for diabetes through a phenotypic screen. The company proceeded to show that MLR-1023 is an allosteric activator of Lyn kinase with an EC50 of 63 nM. As of 2012 Melior was repurposing it for diabetes. In June 2016, the company repo

5-Iodowillardiine is a selective agonist for some kainate receptor subunits with only limited effects at AMPA receptors. It activates kainate receptors containing GluK1 (GluR5) or GluK5 (KA2) subunits, but it does not act on GluK2 (GluR6) subunits. It is an excitotoxic neurotoxin in vivo, but has proved highly useful for characterising the subtypes and function of the various kainate receptors in the brain and spinal cord.

Morantel is an anthelmintic drug used for the removal of parasitic worms in livestock. It affects the nervous system of worms given the drug is an inhibitor of acetylcholinesterase. It is derived in part from 3-methylthiophene. Morantel is closely related to pyrantel.

Gemigliptin (rINN), sold under the brand name Zemiglo, is an oral anti-hyperglycemic agent (anti-diabetic drug) of the dipeptidyl peptidase-4 inhibitor (DPP-4 inhibitor) class of drugs. Glucose lowering effects of DPP-4 inhibitors are mainly mediated by GLP-1 and gastric inhibitory polypeptide (GIP) incretin hormones which are inactivated by DPP-4.

Tozasertib (VX-680) is an aurora inhibitor.

Halosulfuron-methyl is a sulfonylurea post-emergence herbicide used to control some annual and perennial broad-leaved weeds and sedges (such as nutsedge/nutgrass) in a range of crops (particularly rice), established landscape woody ornamentals and turfgrass. It is marketed under several tradenames including Sedgehammer and Sandea.

Tebupirimfos, also known as phostebupirim, is an organothiophosphate insecticide. It is used on corn crops, including popcorn.

Sunepitron (developmental code name CP-93,393) is a combined 5-HT1A receptor agonist and α2-adrenergic receptor antagonist. It was previously under development by Pfizer for the treatment of depression and anxiety. It made it to phase III clinical trials before being discontinued.