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Pyrvinium Pamoate
Pyrvinium (Viprynium) is an anthelmintic effective for pinworms. Several forms of pyrvinium have been prepared with variable counter anions, such as halides, tosylate, triflate and pamoate. Pyrvinium was identified as a potent Wnt inhibitor, acting through activation of Casein kinase CK1α. Pyrvinium salts can also inhibit the growth of cancer cells. More specifically, the pamoate salt has been shown to have preferential toxicity for various cancer cell lines during glucose starvation. Synthesis One synthetic method is based on Skraup synthesis and Paal-Knorr synthesis. More recently, an alternative convergent, synthetic strategy to pyrvinium triflate salts through Friedländer synthesis The Friedländer synthesis is a chemical reaction of 2-aminobenzaldehydes with ketones to form quinoline derivatives. It is named after German chemist Paul Friedländer (1857–1923). This reaction has been catalyzed by trifluoroacetic acid, t ... was reported. References Anthe ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anthelmintic
Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. They may also be called vermifuges (those that stun) or vermicides (those that kill). Anthelmintics are used to treat people who are infected by helminths, a condition called helminthiasis. These drugs are also used to treat infected animals. Pills containing anthelmintics are used in mass deworming campaigns of school-aged children in many developing countries. The drugs of choice for soil-transmitted helminths are mebendazole and albendazole; for schistosomiasis and tapeworms it is praziquantel. Types Antiparasitics that specifically target worms of the genus ''Ascaris'' are called ascaricides. * Benzimidazoles: ** Albendazole – effective against threadworms, roundworms, whipworms, tapeworms, hookworms ** Mebendazole – effective against v ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pinworms
Pinworm infection (threadworm infection in the UK), also known as enterobiasis, is a human parasitic disease caused by the pinworm. The most common symptom is itching in the anal area. The period of time from swallowing eggs to the appearance of new eggs around the anus is 4 to 8 weeks. Some people who are infected do not have symptoms. The disease is spread between people by pinworm eggs. The eggs initially occur around the anus and can survive for up to three weeks in the environment. They may be swallowed following contamination of the hands, food, or other articles. Those at risk are those who go to school, live in a health care institution or prison, or take care of people who are infected. Other animals do not spread the disease. Diagnosis is by seeing the worms which are about one centimetre long or the eggs under a microscope. Treatment is typically with two doses of the medications mebendazole, pyrantel pamoate, or albendazole two weeks apart. Everyone who lives with ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Halide
In chemistry, a halide (rarely halogenide) is a binary chemical compound, of which one part is a halogen atom and the other part is an element or radical that is less electronegative (or more electropositive) than the halogen, to make a fluoride, chloride, bromide, iodide, astatide, or theoretically tennesside compound. The alkali metals combine directly with halogens under appropriate conditions forming halides of the general formula, MX (X = F, Cl, Br or I). Many salts are halides; the ''hal-'' syllable in ''halide'' and ''halite'' reflects this correlation. All Group 1 metals form halides that are white solids at room temperature. A halide ion is a halogen atom bearing a negative charge. The halide anions are fluoride (), chloride (), bromide (), iodide () and astatide (). Such ions are present in all ionic halide salts. Halide minerals contain halides. All these halides are colourless, high melting crystalline solids having high negative enthalpies of formation. Test ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tosylate
In organic chemistry, a toluenesulfonyl group (tosyl group, abbreviated Ts or Tos) is a univalent functional group with the chemical formula –. It consists of a tolyl group, –, joined to a sulfonyl group, ––, with the open valence on sulfur. This group is usually derived from the compound tosyl chloride, (abbreviated TsCl), which forms esters and amides of toluenesulfonic acid, (abbreviated TsOH). The para orientation illustrated (''p''-toluenesulfonyl) is most common, and by convention ''tosyl'' without a prefix refers to the ''p''-toluenesulfonyl group. The toluenesulfonate (or tosylate) group refers to the – (TsO–) group, with an additional oxygen attached to sulfur and open valence on an oxygen. In a chemical name, the term ''tosylate'' may either refer to the salts containing the anion of ''p''-toluenesulfonic acid, (M = alkali metal, , , etc), or it may refer to esters of ''p''-toluenesulfonic acid, TsOR (R = organyl group). Applications For SN2 reacti ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Triflate
In organic chemistry, triflate (systematic name: trifluoromethanesulfonate), is a functional group with the formula and structure . The triflate group is often represented by , as opposed to −Tf, which is the triflyl group, . For example, ''n''-butyl triflate can be written as . The corresponding triflate anion, , is an extremely stable polyatomic ion; this comes from the fact that triflic acid () is a superacid; i.e. it is more acidic than pure sulfuric acid, already one of the strongest acids known. Applications A triflate group is an excellent leaving group used in certain organic reactions such as nucleophilic substitution, Suzuki couplings and Heck reactions. Since alkyl triflates are extremely reactive in SN2 reactions, they must be stored in conditions free of nucleophiles (such as water). The anion owes its stability to resonance stabilization which causes the negative charge to be spread symmetrically over the three oxygen atoms. An additional stabilization is a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pamoate
Pamoic acid, also called embonic acid, is a 2-Naphthoic acid derivative. Salts and esters of pamoic acid are known as pamoates or embonates. It can be prepared by the reaction of 3-hydroxy-2-naphthoic acid with formaldehyde. In pharmacology, the salt form of pamoic acid (pamoate ion) can be used as a counterion of a drug compound to affect the dissolution rate of the drug. The presence of multiple oxygen atoms enables significant hydrogen bonding to occur. Hydrogen bonds facilitate the dissolution of compounds in water. Pharmaceutical drugs formulated this way include cycloguanil pamoate, hydroxyzine pamoate, imipramine pamoate, olanzapine pamoate hydrate, oxantel pamoate, pyrantel pamoate, and pyrvinium pamoate. Pamoic acid has agonist activity for the orphan G protein-coupled receptor GPR35 by which it activates ERK and beta-arrestin2, and causes antinociceptive Nociception (also nocioception, from Latin ''nocere'' 'to harm or hurt') is the Somatosensory system, s ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Wnt Signaling Pathway
The Wnt signaling pathways are a group of signal transduction pathways which begin with proteins that pass signals into a cell through cell surface receptors. The name Wnt is a portmanteau created from the names Wingless and Int-1. Wnt signaling pathways use either nearby cell-cell communication (paracrine) or same-cell communication (autocrine). They are highly evolutionarily conserved in animals, which means they are similar across animal species from fruit flies to humans. Three Wnt signaling pathways have been characterized: the canonical Wnt pathway, the noncanonical planar cell polarity pathway, and the noncanonical Wnt/calcium pathway. All three pathways are activated by the binding of a Wnt-protein ligand to a Frizzled family receptor, which passes the biological signal to the Dishevelled protein inside the cell. The canonical Wnt pathway leads to regulation of gene transcription, and is thought to be negatively regulated in part by the SPATS1 gene. The noncanonical plana ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Casein Kinase 1
The Casein kinase 1 family () of protein kinases are serine/threonine-selective enzymes that function as regulators of signal transduction pathways in most eukaryotic cell types. CK1 isoforms are involved in Wnt signaling, circadian rhythms, nucleo-cytoplasmic shuttling of transcription factors, DNA repair, and DNA transcription. Discovery By the early 1950s it was known from metabolic labeling studies using radioactive phosphate that phosphate groups attached to phosphoproteins inside cells can sometimes undergo rapid exchange of new phosphate for old. In order to perform experiments that would allow isolation and characterization of the enzymes involved in attaching and removing phosphate from proteins, there was a need for convenient Substrate (biochemistry), substrates for protein kinases and phosphatase, protein phosphatases. Casein has been used as a substrate since the earliest days of research on protein phosphorylation. By the late 1960s, CAMP-dependent protein kinase, cycl ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Skraup Synthesis
The Skraup synthesis is a chemical reaction used to synthesize quinolines. It is named after the Czech chemist Zdenko Hans Skraup (1850-1910). In the archetypal Skraup reaction, aniline is heated with sulfuric acid, glycerol, and an oxidizing agent such as nitrobenzene to yield quinoline. In this example, nitrobenzene serves as both the solvent and the oxidizing agent. The reaction, which otherwise has a reputation for being violent, is typically conducted in the presence of ferrous sulfate. Arsenic acid Arsenic acid or trihydrogen arsenate is the chemical compound with the formula . More descriptively written as , this colorless acid is the arsenic analogue of phosphoric acid. Arsenate and phosphate salts behave very similarly. Arsenic acid as ... may be used instead of nitrobenzene and the former is better since the reaction is less violent. See also * Bischler-Napieralski reaction * Doebner-Miller reaction References {{DEFAULTSORT:Skraup Reaction Condensatio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Friedländer Synthesis
The Friedländer synthesis is a chemical reaction of 2-aminobenzaldehydes with ketones to form quinoline derivatives. It is named after German chemist Paul Friedländer (1857–1923). This reaction has been catalyzed by trifluoroacetic acid, toluenesulfonic acid, iodine, and Lewis acids. Several reviews have been published. Mechanism Two viable reaction mechanisms exist for this reaction. In the first mechanism 2-amino substituted carbonyl compound 1 and carbonyl compound 2 react in a rate-limiting step to aldol adduct 3. This intermediate loses water in an elimination reaction to unsaturated carbonyl compound 4 and then loses water again in imine formation to quinoline 7. In the second mechanism the first step is Schiff base formation to 5 followed by Aldol reaction to 6 and elimination to 7. : The Pfitzinger reaction and the Niementowski quinoline synthesis are variations of the Friedländer reaction. See also * Doebner-Miller reaction *Povarov reaction *Skraup reaction ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anthelmintics
Anthelmintics or antihelminthics are a group of antiparasitic drugs that expel parasitic worms (helminths) and other internal parasites from the body by either stunning or killing them and without causing significant damage to the host. They may also be called vermifuges (those that stun) or vermicides (those that kill). Anthelmintics are used to treat people who are infected by helminths, a condition called helminthiasis. These drugs are also used to treat infected animals. Pills containing anthelmintics are used in mass deworming campaigns of school-aged children in many developing countries. The drugs of choice for soil-transmitted helminths are mebendazole and albendazole; for schistosomiasis and tapeworms it is praziquantel. Types Antiparasitics that specifically target worms of the genus ''Ascaris'' are called ascaricides. * Benzimidazoles: ** Albendazole – effective against threadworms, roundworms, whipworms, tapeworms, hookworms ** Mebendazole – effective against va ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
