|
Machaeriol A
Machaeriol A is one of a number of phytocannabinoids with a hexahydrocannabinol backbone, found in plants from the '' Machaerium'' family such as '' Machaerium multiflorum''. While they are related in structure to tetrahydrocannabinols such as those from cannabis, the machaeriol compounds have opposite ''trans'' stereochemistry from THC and have no affinity for the psychoactive CB1 receptor. However, some derivatives are active at CB2, and they have also been found to have antibacterial, antifungal and antiparasitic actions, and have been investigated as lead compounds for the development of potential anti-cancer drugs. See also * Perrottetinene * Cis-THC ''cis''-Delta-9-Tetrahydrocannabinol ((-)-''cis''-Δ9-THC) is an isomer of tetrahydrocannabinol found in the ''Cannabis'' plant but in lower quantities than the more well-known ''trans'' isomer. Formation of cis-THC could take place in process o ... References Cannabinoids Benzopyrans Hydroxyarenes Heterocy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Phytocannabinoid
Cannabinoids () are several structural classes of compounds found primarily in the ''Cannabis'' plant or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary psychoactive compound in cannabis. Cannabidiol (CBD) is also a major constituent of temperate cannabis plants and a minor constituent in tropical varieties. At least 100 distinct phytocannabinoids have been isolated from cannabis, although only four (i.e., THCA, CBDA, CBCA and their common precursor CBGA) have been demonstrated to have a biogenetic origin. It was reported in 2020 that phytocannabinoids can be found in other plants such as rhododendron, licorice and liverwort, and earlier in Echinacea. Phytocannabinoids are multi-ring phenolic compounds structurally related to THC, but endocannabinoids are fatty acid derivatives. Nonclassical synthetic cannabinoids (cannabimimetics) include aminoalkylindoles, 1,5-diarylpyrazoles, quinolines, an ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antifungal
An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycosis such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and others. Such drugs are usually obtained by a doctor's prescription, but a few are available over the counter (OTC). The evolution of antifungal resistance is a growing threat to health globally. Routes of administration Ocular Indicated when the fungal infection is located in the eye. There is currently only one ocular antifungal available: natamycin. However, various other antifungal agents could be compounded in this formulation. Intrathecal Used occasionally when there's an infection of the central nervous system and other systemic options cannot reach the concentration required in that region for therapeutic benefit. Example(s): amphotericin B. Vaginal This may be used to treat some fungal in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Benzopyrans
4H-1-Benzopyran is an organic compound with the formula . It is one of two isomers of benzopyran, the other being 2H-1-benzopyran, which is more prevalent. It can be viewed as the fusion of a benzene ring to a heterocyclic pyran ring. Some benzopyrans have shown anticancerous activity '' in vitro''. The radical form of benzopyran is paramagnetic. The unpaired electron is delocalized over the whole benzopyran molecule, rendering it less reactive than one would expect otherwise. A similar example is the cyclopentadienyl radical. Commonly, benzopyran is encountered in the reduced state, in which it is partially saturated with one hydrogen atom, introducing a tetrahedral CH2 group in the pyran ring. Therefore, there are many structural isomers owing to the multiple possible positions of the oxygen atom and the tetrahedral carbon atom: Nomenclature According to current IUPAC The International Union of Pure and Applied Chemistry (IUPAC ) is an international federatio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoids
Cannabinoids () are several structural classes of compounds found primarily in the ''Cannabis'' plant or as synthetic compounds. The most notable cannabinoid is the phytocannabinoid tetrahydrocannabinol (THC) (delta-9-THC), the primary psychoactive compound in cannabis. Cannabidiol (CBD) is also a major constituent of temperate cannabis plants and a minor constituent in tropical varieties. At least 100 distinct phytocannabinoids have been isolated from cannabis, although only four (i.e., THCA, CBDA, CBCA and their common precursor CBGA) have been demonstrated to have a biogenetic origin. It was reported in 2020 that phytocannabinoids can be found in other plants such as rhododendron, licorice and liverwort, and earlier in Echinacea. Phytocannabinoids are multi-ring phenolic compounds structurally related to THC, but endocannabinoids are fatty acid derivatives. Nonclassical synthetic cannabinoids (cannabimimetics) include aminoalkylindoles, 1,5-diarylpyrazoles, quinolines, a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cis-THC
''cis''-Delta-9-Tetrahydrocannabinol ((-)-''cis''-Δ9-THC) is an isomer of tetrahydrocannabinol found in the ''Cannabis'' plant but in lower quantities than the more well-known ''trans'' isomer. Formation of cis-THC could take place in process of epimerization associated with acid-catalyzed cyclization of CBD to THC. It has similar psychoactive effects to ''trans''-Δ9-THC in tests on mice, but with only around 1/5th the potency. The equivalent Δ8 isomer is also known as a synthetic compound, but has not been isolated from ''Cannabis'' plant material. All four cis/trans isomers are known, though only the (6aR,10aR) and (6aS,10aR) enantiomers are psychoactive, while the others retain activity at targets such as GPR18 and GPR55. See also * Abeo-HHC acetate * Abn-CBD * CBD-DMH * Exo-THC * Iso-THC * HU-211 * Perrottetinene Perrottetinene is a naturally occurring cannabinoid compound found in liverworts from the family Radulaceae native to Japan, New Zealand and Costa Ri ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Perrottetinene
Perrottetinene is a naturally occurring cannabinoid compound found in liverworts from the family Radulaceae native to Japan, New Zealand and Costa Rica, namely '' Cladoradula perrottetii'', '' Radula marginata'' and ''Radula laxiramea'', along with a number of similar compounds. Its chemical structure closely resembles that of THC, the main active component of marijuana but with a ''cis'' rather than ''trans'' conformation and a bibenzyl tailchain instead of pentyl. The absolute configuration of perrottetinene was established in 2008 by an enantioselective total synthesis. Pharmacology In 2018, a study showed that perrottetinene is mild to moderately psychoactive through activation of the cannabinoid receptor 1. (-)-''cis''-Perrottetinene was found to have a binding affinity of 481 nM at CB1 and 225 nM at CB2, while the unnatural (-)-''trans''-perrottetinene was found to more active with binding affinities of 127 nM at CB1 and 126 nM at CB2, both acting as partial agonist ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lead Compound
A lead compound (, i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but may nevertheless have suboptimal structure that requires modification to fit better to the target; lead drugs offer the prospect of being followed by back-up compounds. Its chemical structure serves as a starting point for chemical modifications in order to improve potency, selectivity, or pharmacokinetic parameters. Furthermore, newly invented pharmacologically active moieties may have poor druglikeness and may require chemical modification to become drug-like enough to be tested biologically or clinically. Terminology Lead compounds are sometimes called developmental candidates. This is because the discovery and selection of lead compounds occurs prior to preclinical and clinical development of the candidate. Discovering lead compo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antiparasitic
Antiparasitics are a class of medications which are indicated for the treatment of parasitic diseases, such as those caused by helminths, amoeba, ectoparasites, parasitic fungi, and protozoa, among others. Antiparasitics target the parasitic agents of the infections by destroying them or inhibiting their growth; they are usually effective against a limited number of parasites within a particular class. Antiparasitics are one of the antimicrobial drugs which include antibiotics that target bacteria, and antifungals that target fungi. They may be administered orally, intravenously or topically. Overuse or misuse of antiparasitics can lead to the development of antimicrobial resistance. Broad-spectrum antiparasitics, analogous to broad-spectrum antibiotics for bacteria, are antiparasitic drugs with efficacy in treating a wide range of parasitic infections caused by parasites from different classes. Types Broad-spectrum * Nitazoxanide Antiprotozoals * Melarsoprol (for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antibacterial
An antibiotic is a type of antimicrobial substance active against bacteria. It is the most important type of antibacterial agent for fighting bacterial infections, and antibiotic medications are widely used in the treatment and prevention of such infections. They may either kill or inhibit the growth of bacteria. A limited number of antibiotics also possess antiprotozoal activity. Antibiotics are not effective against viruses such as the ones which cause the common cold or influenza. Drugs which inhibit growth of viruses are termed antiviral drugs or antivirals. Antibiotics are also not effective against fungi. Drugs which inhibit growth of fungi are called antifungal drugs. Sometimes, the term ''antibiotic''—literally "opposing life", from the Greek roots ἀντι ''anti'', "against" and βίος ''bios'', "life"—is broadly used to refer to any substance used against microbes, but in the usual medical usage, antibiotics (such as penicillin) are those produced ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hexahydrocannabinol
Hexahydrocannabinol (HHC) is a phytocannabinoid that has been reported as a trace component of ''Cannabis sativa''. It can also be synthesized by hydrogenation of tetrahydrocannabinol (THC). The synthesis and bioactivity of HHC was first reported in 1940 by Roger Adams. HHC is a psychoactive substance with effects reportedly similar to those of THC. HHC vaporizers have been openly sold at head shops and convenience stores since at least the early 2020s in North America and Europe. Pharmacology HHC has 2 diastereomers that only differ by the orientation of the 9-methyl group, unlike D9-THC and D8-THC which have the double bond position next to the 9-methyl group that prevents this. The 9-methyl group orientation is believed to be important for cannabinoid binding affinity. Research has found 9R-HHC to have a binding affinity of 15nM ± 0.8nM at CB1 and 13nM ± 0.4nM at CB2, while 9S-HHC has a binding affinity of 176nM ± 3.3nM at CB1 and 105nM ± 26nM at CB2. The same study ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cannabinoid Receptor 2
The cannabinoid receptor 2 (CB2), is a G protein-coupled receptor from the cannabinoid receptor family that in humans is encoded by the ''CNR2'' gene. It is closely related to the cannabinoid receptor 1 (CB1), which is largely responsible for the efficacy of endocannabinoid-mediated presynaptic-inhibition, the psychoactive properties of tetrahydrocannabinol (THC), the active agent in cannabis, and other phytocannabinoids (plant cannabinoids). The principal endogenous ligand for the CB2 receptor is 2-Arachidonoylglycerol (2-AG). CB2 was cloned in 1993 by a research group from Cambridge looking for a second cannabinoid receptor that could explain the pharmacological properties of tetrahydrocannabinol. The receptor was identified among cDNAs based on its similarity in amino-acid sequence to the cannabinoid receptor 1 (CB1) receptor, discovered in 1990. The discovery of this receptor helped provide a molecular explanation for the established effects of cannabinoids on the im ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
