http://www.3dchem.com Molecule of the Month Updates en-gb Sat, 4 Feb 2012 00:00:00 GMT Copyright: (C) Karl Harrison http://www.3dchem.com 12 http://www.3dchem.com/molecules.asp?id=475http://www.3dchem.com/molecules.asp?id=475Streptolydigin is an antibiotic which works by blocking nucleic acid chain elongation by binding to the polymerase, thus stopping RNA polymerase activity inside a cell. Specifically, it inhibits the assembly of the RNA polymerase II transcription complex and DNA polymerase III transcription. It is active against a number of gram positive bacteria.Sat, 16 Apr 2011 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=476http://www.3dchem.com/molecules.asp?id=476Temocillin is a β-lactamase resistant carboxypenicillin. introduced by Beecham, marketed by Eumedica Pharmaceuticals as primarily for the treatment of multiresistant Gram negative bacteria, such as Salmonella and Escherichia coli. It is not active against Gram positive bacteria or bacteria with altered penicillin-binding proteins. The common dosage is 2g intravenously every 12 hours. Wed, 16 Mar 2011 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=474http://www.3dchem.com/molecules.asp?id=474Scopolamine is a tropane alkaloid drug with muscarinic antagonist effects. Scopolamine causes central nervous system depression characterized by amnesia, fatigue and reduction in rapid eye movement sleep. It is among the secondary metabolites of plants from Solanaceae (nightshade) family of plants. Scopolamine exerts its effects by acting as a competitive antagonist at muscarinic acetylcholine receptors, specifically M1 receptors; it is thus classified as an anticholinergic, anti-muscarinic drug. Although scopolamine is often portrayed in the media as a dangerous drug, its anticholinergic properties give it some legitimate medical applications in very minute doses. As an example, in the treatment of motion sickness, the dose, gradually released from a transdermal patch, is only 330 micrograms (µg) per day.Wed, 16 Feb 2011 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=473http://www.3dchem.com/molecules.asp?id=473Phencyclidine is a recreational, dissociative drug formerly used as an anesthetic agent, exhibiting hallucinogenic and neurotoxic effects. Developed in 1926, it was first patented in 1952 by the Parke-Davis pharmaceutical company and marketed under the brand name Sernyl. In chemical structure, PCP is an arylcyclohexylamine derivative, and, in pharmacology, it is a member of the family of dissociative anesthetics. PCP works primarily as an NMDA receptor antagonist, which blocks the activity of the NMDA receptor and, like most antiglutamatergic hallucinogens, is significantly more dangerous than other categories of hallucinogens. Users tend to demonstrate symptoms that mimic schizophrenia such as delusions, hallucinations, paranoia and disordered thinking. The full extent of the pharmacology of this compound in the human central nervous system is not fully understood; it binds to many different receptor sites. Sat, 15 Jan 2011 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=472http://www.3dchem.com/molecules.asp?id=472Naphyrone is a stimulant drug and has been reported as a novel designer drug with effects similar to recently controlled drugs like mephedrone, that acts as a triple reuptake inhibitor. This drug is chemically related to pyrovalerone which used to be prescribed to treat lethargy and fatigue, but was discontinued because of concerns over potential for misuse. Pyrovalerone is already a Class C drug.Wed, 15 Dec 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=471http://www.3dchem.com/molecules.asp?id=471Myristicin is a phenylpropene, a natural organic compound present in small amounts in the essential oil of nutmeg and to a lesser extent in other spices such as parsley and dill. Myristicin is a naturally occurring insecticide and acaricide with possible neurotoxic effects on neuroblastoma cells. It has psychoactive properties at doses much higher than used in cooking. Myristicin is a weak inhibitor of monoamine oxidase. Raw nutmeg produces anticholinergic-like symptoms, attributed to myristicin and elemicin.Mon, 15 Nov 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=470http://www.3dchem.com/molecules.asp?id=470Methylone is an entactogen and stimulant of the phenethylamine, amphetamine, and cathinone classes. It was originally patented by Peyton Jacob and Alexander Shulgin in 1996 as an antidepressant. Methylone is a close structural analogue of MDMA, differing by the addition of a β-ketone group.Fri, 15 Oct 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=469http://www.3dchem.com/molecules.asp?id=469Methedrone is a stimulant and entactogen drug of the phenethylamine, amphetamine, and cathinone chemical classes. It is a triple reuptake/release/reversible MAO inhibitor. It is closely related to para-methoxymethamphetamine (PMMA), methylone and mephedrone, and likely has a similar pharmacological profile. It may still be legal in some countries, but its sale has been banned in Sweden and the UK. Its prior availability via the internet led to increased use of the drug.Wed, 15 Sep 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=468http://www.3dchem.com/molecules.asp?id=468Methamphetamine, methylamphetamine, N-methylamphetamine, desoxyephedrine, and colloquially as "meth" or "crystal meth", is a psychostimulant of the phenethylamine and amphetamine class of drugs. It increases alertness, concentration, energy, and in high doses, can induce euphoria, enhance self-esteem, and increase libido. Methamphetamine has high potential for abuse and addiction by activating the psychological reward system via triggering a cascading release of dopamine and norepinephrine in the brain. Methamphetamine is FDA approved for the treatment of ADHD and exogenous obesity, marketed in the USA under the trademark name DesoxynSun, 15 Aug 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=467http://www.3dchem.com/molecules.asp?id=467Mephedrone, also known as 4-methylmethcathinone (4-MMC), or 4-methylephedrone, is a synthetic stimulant and entactogen drug of the amphetamine and cathinone classes. Slang names include meph, drone, and MCAT. It is reportedly manufactured in China and is chemically similar to the cathinone compounds found in the khat plant of eastern Africa. Mephedrone was first synthesised in 1929 but did not become widely known until it was rediscovered in 2003. By 2007 mephedrone was reported to be available for sale on the internet, by 2008 law enforcement agencies had become aware of the compound and by 2010 it had been reported in most of Europe, becoming particularly prevalent in the United Kingdom. It comes in the form of tablets or a powder, which users can swallow, snort or inject, producing similar effects to MDMA, amphetamines and cocaine. As well as producing the intended stimulant effects, negative side effects occur when mephedrone is used, with teeth grinding the most common. The metabolism of mephedrone has been studied in rats and humans, and the metabolites can be detected in urine after usage. Nothing is known about the potential neurotoxicity of mephedrone, but scientists have suggested possible dangers associated with its use based on its similarity to other drugs. Several people have died after consuming mephedrone, but some deaths that the media attributed to the drug were later determined to have been caused by other factors.Thu, 15 Jul 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=466http://www.3dchem.com/molecules.asp?id=466Lofentanil is one of the most potent opioid analgesics known and is an analogue of fentanyl, which was developed in 1960. It is most similar to the highly potent opioid carfentanil (4-carbomethoxyfentanyl), only slightly more potent. Lofentanil can be described as 3-methylcarfentanil, or 3-methyl-4-carbomethoxyfentanyl. While 3-methylfentanyl is considerably more potent than fentanyl itself, lofentanil is only slightly stronger than carfentanil. This suggests that substitution at both the 3 and 4 positions of the piperidine ring introduces steric hindrance which prevents μ-opioid affinity from increasing much further. As with other 3-substituted fentanyl derivatives such as ohmefentanyl, the stereoisomerism of lofentanil is very important, with some stereoisomers being much more potent than others.Tue, 15 Jun 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=465http://www.3dchem.com/molecules.asp?id=465Gramicidin S or Gramicidin Soviet is an antibiotic effective against some Gram positive and Gram negative bacteria as well as some fungi. It is a derivative of gramicidin, produced by the Gram positive bacterium Bacillus brevis. Gramicidin S is a cyclodecapeptide, constructed as two identical pentapeptides joined head to tail, formally written as cyclo(-Val-Orn-Leu-D-Phe-Pro-)2. An interesting point is that it utilizes two amino acids uncommon in peptides: ornithine as well as the unnatural stereoisomer of phenylalanine. Gramicidin S has historically been employed as a topical antibiotic for the treatment of infections from superficial wounds. It exhibits strong antibiotic activity against a broad spectrum of Gram negative and Gram-positive bacteria and against several pathogenic fungi. Like Gramicidin D, Gramicidin S causes hemolysis at low concentrations, thus is not an effective drug for the treatment of systemic infections. Additionally, Gramicidin S has been employed as a spermicide and therapeutic for genital ulcers caused by sexually transmitted diseaseSat, 15 May 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=464http://www.3dchem.com/molecules.asp?id=464Fosfomycin (also known as phosphomycin and phosphonomycin) is a broad-spectrum antibiotic produced by certain Streptomyces species. Fosfomycin is indicated in the treatment of urinary tract infections, where it is usually administered as a single oral megadose. The drug is well tolerated and has a low incidence of harmful side-effects. However, development of bacterial resistance under therapy is a frequent occurrence and makes fosfomycin unsuitable for sustained therapy of severe infections. Additional uses have been proposed. The global problem of advancing antimicrobial resistance has led to a renewed interest in its use more recently.Thu, 15 Apr 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=463http://www.3dchem.com/molecules.asp?id=463Dimenhydrinate is an over-the-counter drug used to prevent nausea and motion sickness. It is most commonly used as pills, although it is also available in liquid form and in suppositories. Chemically, dimenhydrinate is a salt of two drugs: diphenhydramine, and 8-chlorotheophylline, a chlorinated derivative of theophylline.Mon, 15 Mar 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=462http://www.3dchem.com/molecules.asp?id=462Clindamycin is an antibiotic. It is usually used to treat infections with anaerobic bacteria but can also be used to treat some protozoal diseases, such as malaria. It is a common topical treatment for acne and can be useful against some methicillin-resistant Staphylococcus aureus (MRSA) infections.Mon, 15 Feb 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=461http://www.3dchem.com/molecules.asp?id=461Ceftobiprole (band names Zeftera or Zevtera) is a 5th generation cephalosporin antibiotic with activity against methicillin-resistant Staphylococcus aureus, penicillin-resistant Streptococcus pneumoniae, Pseudomonas aeruginosa, and Enterococci. It was discovered by Basilea Pharmaceutica and was developed by Johnson & Johnson Pharmaceutical Research and Development. It has been shown to be statistically non-inferior to the combination of vancomycin and ceftazidime for the treatment of skin and soft tissue infections.Fri, 15 Jan 2010 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=460http://www.3dchem.com/molecules.asp?id=460Ceftaroline fosamil (brand name Teflaro) is an advanced generation cephalosporin antibiotic. It is active against methicillin-resistant Staphylococcus aureus (MRSA) and Gram positive bacteria. It retains the activity of later generation cephalosporins having broad spectrum activity against Gram negative bacteria. It is currently being investigated for community-acquired pneumonia and complicated skin and skin structure infection. Ceftaroline is being developed by Forest Laboratories, under a license from Takeda. Ceftaroline has received approval from the U.S. Food and Drug Administration for the treatment of community-acquired bacterial pneumonia and acute bacterial skin infections on October 29, 2010.[6] In vitro studies show that it has a similar spectrum to ceftobiprole, the only other fifth-generation cephalosporin to date, although no head to head clinical trials have been conducted. Currently, ceftaroline and ceftobiprole are on an unnamed subclass of cephalosporins by the Clinical and Laboratory Standards Institute (CLSI).Tue, 15 Dec 2009 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=459http://www.3dchem.com/molecules.asp?id=459Atropine is a tropane alkaloid extracted from deadly nightshade (Atropa belladonna), jimsonweed (Datura stramonium), mandrake (Mandragora officinarum) and other plants of the family Solanaceae. It is a secondary metabolite of these plants and serves as a drug with a wide variety of effects. The name comes from the original use in deadly nightshade (Atropa belladonna) as a way of dilating women's pupils to make them beautiful. As such both Atropine and deadly nightshade derive names from Atropos, one of the three Fates who, according to Greek mythology, chose how a person was to die. Mandragora (mandrake) was described by Theophrastus in the fourth century B.C. for treatment of wounds, gout, and sleeplessness, and as a love potion. By the first century A.D. Dioscorides recognized wine of mandrake as an anaesthetic for treatment of pain or sleeplessness, to be given prior to surgery or cautery. The use of Solanaceae containing tropane alkaloids for anesthesia, often in combination with opium, persisted throughout the Roman and Islamic Empires and continued in Europe until superseded by the use of ether, chloroform, and other modern anesthetics. Atropine extracts from the Egyptian henbane were used by Cleopatra in the last century B.C. to dilate her pupils, in the hope that she would appear more alluring. In the Renaissance, women used the juice of the berries of Atropa belladonna to enlarge the pupils of their eyes, for cosmetic reasons; "bella donna" is Italian for "beautiful lady". This practice resumed briefly in the late nineteenth- and early twentieth-century in Paris. The mydriatic effects of atropine were studied among others by the German chemist Friedlieb Ferdinand Runge (1795–1867). In 1831, the pharmacist Mein succeeded the pure crystalline isolation of atropine. The substance was first synthesized by German chemist Richard Willstätter in 1901.Sun, 15 Nov 2009 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=458http://www.3dchem.com/molecules.asp?id=458Bisphenol A, commonly abbreviated as BPA, is an organic compound with two phenol functional groups. It is a difunctional building block of several important plastics and plastic additives. With an annual production of 2–3 million tonnes, it is an important monomer in the production of polycarbonate. It is prepared by the condensation of acetone (hence the suffix A in the name) with two equivalents of phenol. The reaction is catalyzed by an acid, such as hydrochloric acid (HCl) or a sulfonated polystyrene resin. Sat, 10 Oct 2009 00:00:00 GMT http://www.3dchem.com/molecules.asp?id=457http://www.3dchem.com/molecules.asp?id=457Trazodone is a psychoactive drug of the piperazine and triazolopyridine chemical classes that has antidepressant, anxiolytic, and hypnotic properties. It has been advertised that its therapeutic benefits become noticeable within the first week of administration. Trazodone has considerably less prominent side effects in comparison to most of the tricyclic antidepressants and tetracyclic antidepressants. Trazodone was originally discovered and developed in Italy in the 1960s by Angelini research laboratories as a second-generation antidepressant. It was developed according to the mental pain hypothesis, which was postulated from studying patients and which proposes that major depression is associated with a decreased pain threshold.Sat, 12 Sep 2009 00:00:00 GMT