Материалы II студенческой межфакультетсткой конференции первокурсников по биоорганической химии
Pyrrole Jad Ahmad, group 3. Scientific adviser is Tishakova Tatyana
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- Бұл бет үшін навигация:
- Barbituric acid
- Imidazole
- PURINE Outmane Belbachir, group 3. Scientific adviser is Tishakova Tatyana.
- QUINOLINE P ranav Sharma, group 3. Scientific adviser is Tishakova Tatyana.
- MORPHINE Sara ben Hassen, group 3. Scientific adviser is Tishakova Tatyana.
- THIAZOLE Zainab Riyaz, group 3. Scientific adviser is Tishakova Tatyana.
PyrroleJad Ahmad, group 3. Scientific adviser is Tishakova Tatyana.Pyrrole is a heterocyclic aromatic organic compound, a five-membered ring with the formula C4H4NH. It is a colourless volatile liquid that darkens readily upon exposure to air. Substituted derivatives are also called pyrroles, e.g., N-methylpyrrole, C4H4NCH3.Porphobilinogen, a trisubstituted pyrrole, is the biosynthetic precursor to many natural products such as heme. Pyrroles are components of more complex macrocycles, including the porphyrins of heme, the chlorins, bacteriochlorins, chlorophyll, porphyrinogens. Pyrrole has very low basicity compared to conventional amines and some other aromatic compounds like pyridine. This decreased basicity is attributed to the delocalization of the lone pair of electrons of the nitrogen atom in the aromatic ring. Pyrrole is a very weak base with a pKaH of about –1 to –2. Protonation results in loss of aromaticity, and is, therefore, unfavorable. The uses of pyrrole 1) Pyrrole and its derivatives are widely used as an intermediate in synthesis of pharmaceuticals, medicines, agrochemicals, dyes, photographic chemicals, perfumes and other organic compounds. For example, chlorophyll, heme are the derivatives which are made by four pyrrole ring formation of porphyrin ring system. 2) They are used as catalysts for polymerization process, corrosion inhibitors, preservatives, and as solvents for resins and terpenes. 3) They are used as the standard of chromatographic analysis. 4) At last, they are also used in organic synthesis and the pharmaceutical industry. Pyrrole Disorder is known by many different names including the commonly used names of Pyroluria, Kryptopyrroles, and the lesser used names of Kryptopyrroluria, Pyrroluria, Pyrolle Disorder, Mauve Factor and Hemepyrrole. Pyrrole Disorder can best be described as the abnormal synthesis and metabolism of the oxygen carrying molecule in your blood, called haemoglobin. All cells in your body produce waste or by-products and the by-product of haemoglobin is a metabolite called hydroxyhemopyrrolin-2-one (HPL) also known as Pyrrole. This metabolite was originally thought to be a Kryptopyrrole but further studies have proven this not the case. People who suffer from Pyrrole Disorder produce excessive amounts of HPL which, binds to or inhibits the nutrients; Zinc 1-7, vitamin B6 1-7, Biotin 8, and the Omega 6 Fat GLA from reaching their targets within your body. This effectively renders these nutrients unavailable.
Jennifer Ileka, group 3. Scientific adviser is Tishakova Tatyana.Barbituric acid or malonylurea or 6-hydroxyuracil is an organic compound based on a pyrimidine heterocyclic skeleton. It is an odorless powder soluble in water. Barbituric acid is the parent compound of barbiturate drugs, although barbituric acid itself is not pharmacologically active. The compound was discovered by the German chemist Adolf von Baeyer on December 4, 1864, the feast ofSaint Barbara (who gave the compound its namesake), by combining urea and malonic acid in a condensation reaction.[1] Pharmaceutical and medical use Barbiturates are a group of drugs derived from barbituric acid that act as depressants to the central nervous system. These drugs are often used for medical purposes as sedatives or anesthetics.Barbiturates are actually known as CNS depressants or central nervous system depressants. Barbiturates are derivatives of barbituric acid. Barbiturates have both physical and mental addiction. Currently, Barbiturates have been greatly substituted by benzodiazepines, a psychoactive drug used in general medical practices such as, for treating anxiety and insomnia. This is because benzodiazepines are extensively less dangerous in overdose. On the other hand, barbiturates are still used in generalanesthesia, as well as for epilepsy. Barbiturates comprise a greater danger than alcohol or heroin. If it is used under medical supervision, barbiturates are remarkably safe and effective. They are widely used and widely distributed legally, but more widely abused and misused illegally. Owing to the number of fatal accidents from their misuse they are now largely replaced by tranquillizers. ImidazoleKhalil Jaddouh, group 3. Scientific adviser is Tishakova Tatyana.Imidazoles are well known heterocyclic compounds having important feature of a variety of medicinal agents. Imidazole is a planar 5-membered ring. It is a highly polar compound with dipole moment of 3.61 D. It is highly soluble in water and also is soluble in other polar solvents. It exists in two equivalent tautomeric forms because the proton can be located on either of the two nitrogen atoms. Due to the presence of a sextet of π-electrons the compound is classified as aromatic. It consists of a pair of electrons from the protonated nitrogen atom and one from each of the remaining four atoms of the ring. Imidazole is amphoteric, i.e., it can function as both an acid and as a base. The literature surveys depicts that Imidazole derivatives shows various pharmacological activities such as anti viral, anti inflammatory and analgesic, anti depressant, anti fungal and anti-bacterial, anti cancer, anti tubercular and antileishmanial activity. Anti viral activity: Chronic infection with the Hepatitis C Virus (HCV) is a major cause for developing cirrhosis and hepatocellular carcinoma. A series of novel compounds, 5-alkynyl-1-beta-D-ribofuranosylimidazole-4- carboxamides have been synthesized and identified as broad-spectrum antiviral agents. 5-Ethynyl-1-beta-D-ribofuranosylimidazole-4-carboxamide (EICAR) 1, the most potent congener of the group, showed antiviral potency about 10-to 100-fold superior than that of ribavirin, 212. EICAR is an antiviral drug for the treatment of pox-, toga-, arena-, reo-, orthomyxo and paramyxovirus infections.
Purines and pyrimidines make up the two groups of nitrogenous bases, including the two groups of nucleotide bases. Two of the fourdeoxyribonucleotides and two of the four ribonucleotides, the respective building-blocks of DNA and RNA, are purines. There are many naturally occurring purines. Two of the five bases in nucleic acids, adenine (2) and guanine (3), are purines. In DNA, these bases form hydrogen bonds with their complementary pyrimidines thymine and cytosine, respectively. This is called complementary base pairing. In RNA, the complement of adenine is uracil instead of thymine. Other notable purines are hypoxanthine (4), xanthine (5), theobromine (6), caffeine (7), uric acid (8) and isoguanine (9). Aside from the crucial roles of purines (adenine and guanine) in DNA and RNA, purines are also significant components in a number of other important biomolecules, such as ATP, GTP, cyclic AMP, NADH, and coenzyme A. Purine (1) itself, has not been found in nature, but it can be produced by organic synthesis. They may also function directly as neurotransmitters, acting upon purinergic receptors. Adenosine activates adenosine receptors. Metabolism Many organisms have metabolic pathways to synthesize and break down purines. Purines are biologically synthesized as nucleosides (bases attached to ribose). Accumulation of modified purine nucleotides is defective to various cellular processes, especially those involving DNA and RNA. To be viable, organisms possess a number of (deoxy)purine phosphohydrolases, which hydrolyze these purine derivatives removing them from the active NTP and dNTP pools. Deamination of purine bases can result in accumulation of such nucleotides as ITP, dITP, XTP and dXTP.[5] Defects in enzymes that control purine production and breakdown can severely alter a cell’s DNA sequences, which may explain why people who carry certain genetic variants of purine metabolic enzymes have a higher risk for some types of cancer. Sources
Purines are found in high concentration in meat and meat products, especially internal organs such as liver and kidney. In general, plant-based diets are low in purines.[6]Examples of high-purine sources include: sweetbreads, anchovies, sardines, liver, beef kidneys, brains, meat extracts (e.g., Oxo, Bovril), herring, mackerel, scallops, game meats, beer (from the yeast) and gravy. A moderate amount of purine is also contained in beef, pork, poultry, other fish and seafood, asparagus, cauliflower, spinach, mushrooms, green peas, lentils, dried peas, beans, oatmeal, wheat bran, wheat germ, and hawthorn.[7] Higher levels of meat and seafood consumption are associated with an increased risk of gout, whereas a higher level of consumption of dairy products is associated with a decreased risk. Moderate intake of purine-rich vegetables or protein is not associated with an increased risk of gout.[8]
target structures and evaluated their biological activities. The present review provides an in depth view of work done so far on quinolines and its biological activities covering anticancer, antimycobacterial, antimicrobial, anticonvulsant, antiinflamatory and cardiovascular activities. Anticancer Quinoline derivatives fused with various heterocycles haves displayed potent anticancer activity targeting different sites like topoisomerase I, telomerase, farnasyl transferase, Src tyrosine kinase, protein kinase CK-II etc. Indole fused 10H-indolo[3,2-b]quinoline bearing bis-dimethylaminoethyl chain have been synthesized and evaluated for anticancer activity by Vittorio Caprio et al. [15] and compound was found to be act on telomerase with IC50 16M . Intercalation with double stranded DNA is important target for cytotoxicity Yuzi Mikata et al. [16] reported the synthesis of new derivatives of 2-phenyl quinoline having [(2 aminoethyl)aminomethyl] group and compound showed ability to intercalate into double stranded DNA. Antimycobacterial Activity Tuberculosis (TB) has become a global health problem because of lack of proper therapeutic agents for its remedy. There is another serious and alarming problem due to the resurgence of TB especially for the synergy with global human immunodeficiency virus (HIV) and the emergence of multi-drug-resistant (MDR) strains. Thus, there is an urgent need for developing new anti-tubercular drugs which will effectively kill MDR strains, less toxic, shortened duration of therapy, rapid mycobactericidal mechanism of action in the intracellular environment. In this direction various quinoline containing molecules have been synthesized tested for anti-TB activity all over the world. MORPHINESara ben Hassen, group 3. Scientific adviser is Tishakova Tatyana.Morphine is an opioid analgesic drug, a recreational drug, and the main psychoactive chemical in opium. In clinical medicine, morphine is regarded as the gold standard, or benchmark, of analgesics used to relieve intense pain and suffering.[2] Like other opioids, such as oxycodone, hydromorphone, and diacetylmorphine (heroin), morphine acts directly on the central nervous system (CNS) to relieve pain. Morphine has a high potential for addiction; tolerance and psychological dependence develop rapidly, although physiological dependence may take several months to develop. Tolerance to respiratory depression and euphoria develops more rapidly than tolerance to analgesia, and many chronic pain patients are therefore maintained on a stable dose for years. However, its effects can also reverse fairly rapidly, worsening pain through hyperalgesia. Morphine is the most abundant opiate found in opium, the dried latex from unripe seedpods of Papaver somniferum (the opium poppy). Morphine was the first active ingredient purified from a plant source. It is one of at least fifty alkaloids of several different types present in opium, poppy straw concentrate, and other poppy derivatives. The primary source of morphine is chemical extraction from opium. Morphine is primarily used to treat both acute and chronic severe pain. It is also used for pain due to myocardial infarction and for labor pains.[5] There are however concerns that morphine may increase mortality in the setting of non ST elevation myocardial infarction.[6] Morphine has also traditionally been used in the treatment of the acute pulmonary edema.[5] A 2006 review however found little evidence to support this practice.[7] Immediate release morphine is beneficial in reducing the symptom of acute shortness of breath due to both cancer and non-cancer causes.[8][9] In the setting of breathlessness at rest or on minimal exertion from conditions such as advanced cancer or end-stage cardio-respiratory diseases, regular, low-dose sustained release morphine significantly reduces breathlessness safely, with its benefits maintained over time.[10][11] Its duration of analgesia is about 3–4 hours when administered via the intravenous, subcutaneous, or intramuscular route and 3–6 hours when given by mouth.[12] Morphine is also used in slow release formulations for opiate substitution therapy (OST) in Austria, Bulgaria, and Slovenia, for addicts who cannot tolerate the side effects of using either methadone or buprenorphine, or for addicts who are "not held" by buprenorphine or methadone. It is used for OST in many parts of Europe although on a limited basis.[13] histidineRautia Matheus, group 3. Scientific adviser is Tishakova Tatyana.HISTIDINE: Is the a-amino acid with an imidazole functional group. It is one of the 22 proteinogenic amino acids.Histidine is an essential amino acid in humans and other mammals. CHEMICAL PROPERTIES The imidazole side chain of histidine has a PKa of approximately 6.0.This means that, at physiologically relevant PH value, relatively small shifts in PH will change its average change. Below PH 6, the imidazole ring is mostly protonated as described by the Hendrson-Hasselbalch equation. When protonated, the imidazole ring bears two NH bonds and has a positive charge. The positive charge is equally distributed between both Nitrogen and can be represented with two equally important resonance structures. AROMATICITY The imidazole ring of Histidine is aromatic at all PH value. It contains six Pi electrons, four from two double bonds and two from a Nitrogen Ione pair. It can form Pi staking interactions, but is complicated by the positive charge. USES OF HISTIDINE
SIDE EFFECTS OF HISTIDINE
CONCLUSION
REFERENCES 1. www.webmd.com//ingredientmono-467 histidine 2. Br.J.pharmacol>157(1) may 2009
Medical Function : The thiazole ring is notable as a component of the vitamin thiamine (B1). Sulfur of the thiazole is derived from cysteine. In anaerobic bacteria, the CN group is derived from dehydroglycine. Pharmacological Function: An antifungal medication is a pharmaceutical fungicide used to treat and prevent mycoses such as athlete's foot, ringworm, candidiasis (thrush), serious systemic infections such as cryptococcal meningitis, and other. Thiazole antibiotics Siomycin A and thiostrepton induce apoptosis in human cancer cells [2], [3] and act as proteasome inhibitors [4]. It has been demonstrated before that combination of two proteasome inhibitors lactacystin and MG132 synergized against prostate cancer cells in vitro [5]. Additionally, synergy was demonstrated by combining bortezomib with curcumin (which demonstrates proteasomal inhibitory activity in addition to other effects) against multiple myeloma cells [6]. Similarly, we have demonstrated that combination of thiostrepton and bortezomib demonstrated strong synergy against prostate cancer [7]. In this study we confirmed that co-treatment of various tumor cell lines of different origin with sub-lethal concentrations of proteasome inhibitors thiostrepton and bortezomib reveals a strong synergy as demonstrated by induction of apoptosis, combination index values and long-term clonogenic assay. Antitumor activity: The synthesis of several new ethyl 2-substituted aminothiazole-4-carboxylate analogs have been described and the prepared compounds were tested for their in vitro antitumor activity against 60 human tumor cell lines by the National Cancer Institute (NCI) and showed potential anticancer activity. Ethyl 2-[3-(diethylamino)-propanamido]-thiazole-4-carboxylate 22 exhibited remarkable activity against RPMI-8226 leukemia cell line with GI50 value of 0.08 μM and a broad spectrum activity against all the tumor cell lines used with GI50 (MG-MID) value of 38.3 μM.
Ответственные за выпуск: Лукьянова Л. В., Тишакова Т. С. жүктеу/скачать 3.18 Mb. Достарыңызбен бөлісу:
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