Benzimidazoles
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Benzimidazoles
Benzimidazole is a heterocyclic aromatic organic compound. This bicyclic compound may be viewed as fused rings of the aromatic compounds benzene and imidazole. It is a white solid that appears in form of tabular crystals. Preparation Benzimidazole was discovered during research on vitamin B12. The benzimidazole nucleus was found to be a stable platform on which drugs could be developed. Benzimidazole is produced by condensation of o-phenylenediamine with formic acid, or the equivalent trimethyl orthoformate: :C6H4(NH2)2 + HC(OCH3)3 → C6H4N(NH)CH + 3 CH3OH 2-Substituted derivatives are obtained when the condensation is conducted with aldehydes in place of formic acid, followed by oxidation. Reactions Benzimidazole is a base: :C6H4N(NH)CH + H+ → 6H4(NH)2CHsup>+ It can also be deprotonated with stronger bases: :C6H4N(NH)CH + LiH → Li 6H4N2CH + H2 The imine can be alkylated and also serves as a ligand in coordination chemistry. The most pro ...
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Fenbendazole
Fenbendazole is a broad-spectrum benzimidazole anthelmintic used against gastrointestinal parasites including: roundworms, hookworms, whipworms, the tapeworm genus '' Taenia'' (but not effective against '' Dipylidium caninum'', a common dog tapeworm), pinworms, '' Aelurostrongylus'' spp., paragonimiasis, strongyles, and strongyloides that can be administered to sheep, cattle, horses, fish, dogs, cats, rabbits, most reptiles, freshwater shrimp tanks as planaria and hydra treatments, and seals. Mechanism of action Fenbendazole works by binding to tubulin, a protein that is part of the microtubules in the cells of parasites. This binding disrupts the microtubules' formation and function, leading to the parasites' inability to absorb nutrients, resulting in their eventual death. This mode of action makes fenbendazole effective against both adult and larval stages of many parasitic worms. Uses in veterinary medicine Dogs and cats Fenbendazole is commonly used ...
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Ciclobendazole
Ciclobendazole is an anthelmintic, that is a pharmaceutical drug against parasitic worms. It underwent a clinical trial in the 1970s, where it was found to be as effective as mebendazole in the treatment of hookworm infection and ascariasis Ascariasis is a disease caused by the parasitic roundworm ''Ascaris lumbricoides''. Infections have no symptoms in more than 85% of cases, especially if the number of worms is small. Symptoms increase with the number of worms present and may in ..., but significantly less effective in the treatment of trichuriasis. It is not known to be marketed anywhere in the world. References Anthelmintics Aromatic ketones Benzimidazoles Carbamates Cyclopropyl compounds {{antiinfective-drug-stub ...
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Albendazole
Albendazole is a broad-spectrum antihelmintic and antiprotozoal agent of the benzimidazole type. It is used for the treatment of a variety of intestinal parasite infections, including ascariasis, pinworm infection, hookworm infection, trichuriasis, strongyloidiasis, taeniasis, clonorchiasis, opisthorchiasis, cutaneous larva migrans, giardiasis, and gnathostomiasis, among other diseases. Common side effects include nausea, abdominal pain, and headache. Rare but potentially serious side effects include bone marrow suppression which usually improves on discontinuing the medication. Hepatitis, Liver inflammation has been reported and those with prior liver problems are at greater risk. It is pregnancy category D in Australia, meaning it may cause harm if taken by pregnant women. Albendazole was developed in 1975. It is on the WHO Model List of Essential Medicines, World Health Organization's List of Essential Medicines. Albendazole is available in a fixed-dose combination with ...
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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 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, particularly small ruminants such as goats and sheep. Anthelmintic medication is also used in mass deworming campaigns of school-aged children in many developing countries. Anthelmintics are also used for mass deworming of livestock. The drugs of choice for soil-transmitted helminths are mebendazole and albendazole; for schistosomiasis and tapeworms it is praziquantel. Types Many early treatments were herbal, such as the oil of herbs of the genus '' Chenopodium'' that were given as anthelmintic treatment for ...
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Telmisartan
Telmisartan, sold under the brand name Micardis among others, is a medication used to treat high blood pressure and heart failure. It is a reasonable initial treatment for high blood pressure. It is taken by mouth. Common side effects include upper respiratory tract infections, diarrhea, and back pain. Serious side effects may include kidney problems, low blood pressure, and angioedema. Use in pregnancy may harm the baby and use when breastfeeding is not recommended. It is an angiotensin II receptor blocker and works by blocking the effects of angiotensin II. Telmisartan was patented in 1991 and came into medical use in 1999. It is available as a generic medication. In 2022, it was the 228th most commonly prescribed medication in the United States, with more than 1million prescriptions. It is available in combination with hydrochlorothiazide as telmisartan/hydrochlorothiazide; with cilnidipine as telmisartan/cilnidipine; and with amlodipine as telmisartan/amlodipine. ...
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Candesartan
Candesartan is an angiotensin receptor blocker (ARB) primarily used to treat high blood pressure and congestive heart failure. It is always administered in its inactive prodrug form, candesartan cilexetil, which is converted to the active drug during absorption in the gastrointestinal tract. Like olmesartan, candesartan is a cascading prodrug, a feature that influences its pharmacokinetics. It has good bioavailability and is considered one of the most potent AT1 receptor antagonists by weight. Its effective maintenance dose is also relatively low. It was patented in 1990 and approved for medical use in 1997. Medical uses Hypertension As with other angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Candesartan has an additive antihypertensive effect when combined with a diuretic, such as chlorthalidone. It is available in a fixed-combination formulation with a low dose of the thiazide diuretic hydrochlorothiazide. Candesartan/ ...
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Azilsartan
Azilsartan, sold under the brand name Edarbi among others, is used for the treatment of hypertension. It is used as the prodrug azilsartan medoxomil, is an angiotensin II receptor antagonist, and was developed by Takeda Pharmaceutical Company, Takeda. The most common adverse reaction in adults is diarrhea. It is available as a generic medication. It is also sold as a combination drug with chlortalidone under the brand name Edarbyclor. Medical uses Azilsartan is used for the treatment of hypertension in adults. One of the benefits of the medication is that Azilsartan does not need dose adjustments for patients with renal or hepatic dysfunction. Contraindications Azilsartan must not be used with aliskiren, a renin inhibitor, in patients with diabetes as this increases the risk of serious adverse effects. Like other antihypertensive drugs acting on the renin–angiotensin system, it is contraindicated during the second and third trimesters of pregnancy. It should not be used duri ...
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Benomyl
Benomyl (also marketed as Benlate) is a fungicide introduced in 1968 by DuPont. It is a systemic benzimidazole fungicide that is selectively toxic to microorganisms and invertebrates (especially earthworms), but relatively nontoxic toward mammals. Due to the prevalence of resistance of parasitic fungi to benomyl, it and similar pesticides are of diminished effectiveness. Nonetheless, it is widely used. Toxicity Benomyl is of low toxicity to mammals. It has an arbitrary LD50 of "greater than 10,000 mg/kg/day for rats". Skin irritation may occur through industrial exposure, and florists, mushroom pickers and floriculturists have reported allergic reactions to benomyl. In a laboratory study, dogs fed benomyl in their diets for three months developed no major toxic effects, but did show evidence of altered liver function at the highest dose (150 mg/kg). With longer exposure, more severe liver damage occurred, including cirrhosis. The US Environmental Protection Agency classi ...
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Vitamin B12
Vitamin B12, also known as cobalamin, is a water-soluble vitamin involved in metabolism. One of eight B vitamins, it serves as a vital cofactor (biochemistry), cofactor in DNA synthesis and both fatty acid metabolism, fatty acid and amino acid metabolism. It plays an essential role in the nervous system by supporting myelinogenesis, myelin synthesis and is critical for the maturation of red blood cells in the bone marrow. While animals require B12, plants do not, relying instead on alternative enzymatic pathways. Vitamin B12 is the most chemically complex of all vitamins, and is synthesized exclusively by certain archaea and bacteria. Natural food sources include meat, shellfish, liver, fish, poultry, Egg as food, eggs, and dairy products. It is also added to many breakfast cereals through food fortification and is available in dietary supplement and pharmaceutical forms. Supplements are commonly taken orally but may be administered via intramuscular injection to treat defic ...
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Angiotensin II Receptor Blocker
Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin II receptor antagonists, or AT1 receptor antagonists, are a group of pharmaceuticals that bind to and inhibit the angiotensin II receptor type 1 (AT1) and thereby block the arteriolar contraction and sodium retention effects of renin–angiotensin system. Their main uses are in the treatment of hypertension (high blood pressure), diabetic nephropathy ( kidney damage due to diabetes) and congestive heart failure. They ''selectively'' block the activation of the AT1 receptor, preventing the binding of angiotensin II compared to ACE inhibitors. ARBs and the similar-attributed ACE inhibitors are both indicated as the first-line antihypertensives in patients developing hypertension along with left-sided heart failure. However, ARBs appear to produce fewer adverse effects compared to ACE inhibitors. Medical uses ...
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Food And Drug Administration
The United States Food and Drug Administration (FDA or US FDA) is a List of United States federal agencies, federal agency of the United States Department of Health and Human Services, Department of Health and Human Services. The FDA is responsible for protecting and promoting public health through the control and supervision of food safety, tobacco products, caffeine products, dietary supplements, Prescription drug, prescription and Over-the-counter drug, over-the-counter pharmaceutical drugs (medications), vaccines, biopharmaceuticals, blood transfusions, medical devices, electromagnetic radiation emitting devices (ERED), cosmetics, Animal feed, animal foods & feed and Veterinary medicine, veterinary products. The FDA's primary focus is enforcement of the Federal Food, Drug, and Cosmetic Act (FD&C). However, the agency also enforces other laws, notably Section 361 of the Public Health Service Act as well as associated regulations. Much of this regulatory-enforcement work is ...
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Small Molecule
In molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs are small molecules; the terms are equivalent in the literature. Larger structures such as nucleic acids and proteins, and many polysaccharides are not small molecules, although their constituent monomers (ribo- or deoxyribonucleotides, amino acids, and monosaccharides, respectively) are often considered small molecules. Small molecules may be used as research tools to probe biological function as well as leads in the development of new therapeutic agents. Some can inhibit a specific function of a protein or disrupt protein–protein interactions. Pharmacology usually restricts the term "small molecule" to molecules that bind specific biological macromolecules and act as an effector, altering the activity or function of the target. Small molecules can ...
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