Материалы II студенческой межфакультетсткой конференции первокурсников по биоорганической химии


PYRROLE Otaigbe Peace Augustine, group 9. Scientific adviser is Tishakova Tatyana



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PYRROLE

Otaigbe Peace Augustine, group 9. Scientific adviser is Tishakova Tatyana.


Pyrrole is a heterocyclic aromatic organic compound, a five-membered ring with the formula C4H4NH. Pyrroles are components of more complex macrocycles, including the porphyrins of heme, the chlorins, bacteriochlorins, chlorophyll and porphyrinogens.

Medical implications of pyrrole

Pyrroles are synthesized during hemoglobin production in the body. They can be thought of as a byproduct of hemoglobin, when hemoglobin is synthesized in the spleen. While it is normal for some pyrroles to be produced as a hemoglobin byproduct, certain individuals tend to produce an excess. Pyrroles have an affinity for binding to and causing a high depletion of 2 critical nutrients: Vitamin B-6 and Zinc. In the instance of an increasing production of pyrroles, the pyrroles have an affinity for binding to aldehydes such as B-6. Increased pyrrole production will also tend to deplete zinc’s activities. Below are some of the activities of vitamin B-6 and zinc increased pyrrole will deplete.

Vitamin B-6 is critical for several biological and metabolic functions:



  • Neurotransmitter synthesis

  • Gene expression

  • Synthesis of hemoglobin

  • Histamine production

  • Metabolism of amino acids, lipids and glucose

  • Methylation status

Some of the activities that zinc are involved in:

  • DNA & RNA synthesis

  • Gene expression

  • Nervous system function

  • Immune function & immune signaling such as cell apoptosis

  • Neuronal transmission

  • Brain function

Conclusion

Hetero cyclic compound containing pyrrole plays most important role in the field of clinical therapeutics. It shows wide range of activities for medication purpose. The various substituted pyrrole are having significant antihypertensive activity, antineoplastic and Non-steroidal anti-inflammatory drug, some modified are found to be effective as tricyclic antidepressant dissociative anesthetic, antibacterial properties and antipsychotic. Whereas some of the derivatives of pyrrole are found to be effective as analgesic, antipsychotic, Antiarrhythmic and sedative hypnotics.



IMATINIB

Stacia Goodlit, group 9. Scientific adviser is Tishakova Tatyana.


Introduction

Heterocyclic compounds make up majority of organic chemistry. It is a branch of a group of compounds known as cyclic compounds which has two branches Carbocyclic and Heterocyclic. Carbocyclic are those which contain only carbon atoms in the ring, while heterocyclics differ in that the ring contains atleast one other atom besides that of carbon. Heterocyclics are either aliphatic or aromatic. Heterocyclics are present in a wide variety of drugs, most vitamins, many natural products, biomolecules, and biologically active compounds, including antitumor, antibiotic, anti-inflammatory, antidepressant, antimalarial and many more.



Quinazoline is the heterocyclic of focus it is composed of two aromatic rings, to be more specific a benzene ring and a pyrimidine ring therefore it carries the formula C8H6N2. Derivatives of Quinazoline are known as quinazolines and many of them are biologically active substances. One example of such is Imanitib.

Imatinib:

Imatinib / Imatinibmysilate is marketed by Novartis under the brand name (Gleevec / Glivec)



Molecular Formula : C
29H31N7O 

IUPAC NAME:

4-[(4-methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide

It is a quinazoline derived drug which inhibits tyrosine Kinase. It is used in the treatment of multiple cancers most notably Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML)…a specific chromosomal abnormality that is associated with CML. Like all tyrosine-kinase inhibitors, imatinib works by preventing a tyrosine kinase enzyme, in this case BCR-Abl, from phosphorylating subsequent proteins and initiating the signalling cascade necessary for cancer development, thus preventing the growth of cancer cells and leading to their death by apoptosis. Because the BCR-Abl tyrosine kinase enzyme exists only in cancer cells and not in healthy cells, imatinib works as a form of targeted therapy only cancer cells are killed through the drug's action. In this regard, imatinib was one of the first cancer therapies to show the potential for such targeted action, and is often cited as a paradigm for research in cancer therapeutics.



Benzodiazepine

Tafadzwa .C. Mhizha, group 9. Scientific adviser is Tishakova Tatyana.


A benzodiazepine (often abbreviated "BZD") is a psychoactive drug whose core chemical structure is the fusion of a benzene ring and a diazepine ring. Examples include: diazepam, lorazepam, chlordiazepoxide, oxazepam, temazepam, nitrazepam, loprazolam, lormetazepam, clobazam and clonazepam. The first such drug, chlordiazepoxide (Librium), was discovered accidentally by Leo Sternbach in 1955, and made available in 1960 by Hoffmann–La Roche, which has also marketed the benzodiazepine diazepam (Valium) since 1963.

Benzodiazepines enhance the effect of the neurotransmitter gamma-aminobutyric acid (GABA) at the GABAA receptor, resulting in sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety), euphoric, anticonvulsant, and muscle relaxant properties; also seen in the applied pharmacology of high doses of many shorter-acting benzodiazepines are amnesic-dissociative actions. These properties make benzodiazepines useful in treating anxiety, insomnia, agitation, seizures, muscle spasms, alcohol withdrawal and as a premedication for medical or dental procedures. A dose of a benzodiazepine is often given as a pre-med to reduce anxiety before an operation. A large dose is commonly given as a sedative during medical procedures that may cause anxiety or discomfort. The medicine not only reduces anxiety but also has an amnestic effect. Therefore a patient is less likely to remember the details of his or her surgery due to being administered with benzodiazepine.

Benzodiazepines are categorized as short-, intermediate-, or long-acting. Short- and intermediate-acting benzodiazepines are preferred for the treatment of insomnia; longer-acting benzodiazepines are recommended for the treatment of anxiety.

However, despite its wide and various beneficial uses, benzodiazepines should not be used regularly as they may become addictive. Once a patient’s body becomes used to benzodiazepines as a source of relief and help , it becomes used to functioning with the help of this drug and has difficulties functioning without it later on in the future , resulting in restlessness and withdrawal symptoms.




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