Nitrogen Heterocyclic Importance in Chemistry

2021-06-06 08:12:13
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Heterocyclic compounds involve the organic compounds that contains a ring structure that institute atoms like nitrogen. The rings appear to be either simple aromatic or even non-aromatic rings. Heterocyclic chemistry is very important since it accounts for one third of the recent publications. Heterocyclic compounds are very much distributed in nature and they are essential for life. They are known to play vital role in the metabolism of all living cells. Some of the heterocyclic compounds are natural for example the antibiotics, penicillin and alkaloids. The most known or the majority are synthetic heterocyclic which uses pharmaceutical applications like anti-cancer agents. For instance, cationic N-heterocyclic carbine (NHC) complexes are capable of disrupting mitochondrial functions as well as TrxR inhibition. Also, N-heterocyclic complexes are can interfere with the mitochondrial membrane potentials causing induction of apoptosis14,18.

Nitrogen that contains heterocyclic are the key compounds of biological or even medicine interests to chemists. Nitrogen heterocyclic obtains application in the pharmaceutical research, drug discovery and in the agricultural science. For instance, N-heterocyclic carbine-Amine Pt(II) complexes has been of paramount importance to the pharmacists in the development of platinum-based anticancer drug20.

Histamine can be used in the local response to immune and also act as neurotransmitter. It is involved in the allergic reaction and can liberate skin cells on injury and also participate in the regulation of gastric acid secretion. As a drug to combat cancer and viruses, the nitrogen heterocyclic has been made to explore on the use of analogues of the nucleosides. Analogues can be made with the structure of the heterocyclic nitrogenous base and the figure can interfere in the replicative cycle of a virus like in the place of nucleoside.

It has necessitated the production of some drugs like zidovudine which is a nucleoside analog reverse that transcriptase inhibitor. In additional it is useful in the formation of a useful drug that is used for treatment of herpes simplex and herpes zoster viral infections due to high selectivity and low cytotoxicity.

Nitrogen heterocyclic have been an attractive target for synthesis over some years. It has been found in various natural products and have been identified as products of chemical and biological importance. It has been used in different studies to synthesis numerous alkaloids. They have been important as a precursor to the many biological active compound while at the same time focusing on a tremendous amount of attention in developing approaches that could be used to functionalize the systems.

Due to the therapeutic and pharmacological properties, the heterocyclic nitrogen has emerged as an integral backbone for a lot of existing drugs25. Most of the organic that contains nitrogen indicate better biological activity compared to the non-nitrogen compounds. Most of the heterocyclic compounds involve essential amino acids, B12 and E vitamin, hemoglobin, photosynthesis pigment, chlorophyll pigment, thyamine, co-enzyme, riboflavin, DNA among others. All these compounds play a crucial role in the metabolism of living things and therefore deemed important.

Pyrazoles

Pyrazoles belong to a heterocyclic group of compounds that has two adjacent nitrogens in a five-membered ring system25. Pyrazole and its derivatives are commonly used in medical and pesticide chemistry as well as bioactivities. In the medical field, pyrazole and its derivatives portray anti-inflammatory, antitumor, herbicidal, antimicrobial, selective enzyme inhibitory, antibacterial and anticancer properties16, 17,23. Pyrazole and its derivatives are significant due to their wide spectrum of application, novel model of action, favorable profiles to humans as well as low toxicity toward mammalian cells.

The Important Role of Pyrazoles As Anticancer and Antimicrobial and The Important in

Pharmacology

1-mythyl-1,4-dihydroindeno[1,2-c] pyrazoles affects the bindings and conformations of its substituents within the tubulin. It also has hydrogen bonding features the plays a significant role in the anticancer potency of the indenopyrazole derivatives26. When a series of 7-substituted 1-methyl-1,4-dihydroimdeno[1,2-c] pyrazoles (6a-p) are evaluated and synthesized in a cellular and tubulin inhibition, they form a new class of antitumor agents as tubulin polymerization inhibitors thus are idea as anticancer1, 13. Besides, 6n and 6a have significantly low nanomolar potency against a set of cancer cell lines hence provides appropriate inhibition of tubulin polymerization at the tubulin colchicine binding sites.

As Liu et.al1 indicates, in the G2/M phase of the cell cycle, 6a arrested most cells, disrupting the cellular microtubules a well as inducing A549 cell apoptosis. Hence, it is evident the 7-substituted 1-methyl-1,4-dihydroindeno[1,2-c] pyrazoles (6a-p) provides tubulin polymerization inhibition at the colchicine site. As a potential anticancer, pyrazoles has the advantage of suppressing tumor growth by about 59.1% at a dose of 50mg/kg (ip), with minimal toxicity.

Other derivatives of pyrazoles such as dihydropyrano[2,3-c] pyrazoles are crucial in pharmacology because they have pharmacological and biological properties and are thus referred to as antimicrobial.2 Dihydropyrano[2,3-c] pyrazoles are also significant in pharmacology due to their wide applicability as intermediates in medicinal chemistry.

Combretastatin have been used as antimitotic agents but later applied as Vascular Disrupting Agents (VDAs). Specifically, combretastatin A-4 (CA4) was indicated to have the capability to cause selective tumor vascular collapse given nontoxic doses.5 The 12 pyrazole-based analogs of CA4 are potential anticancer agents.

Other pyrazoles derivatives such as proteasome inhibitors with pyrazoles scaffolds play an imperative role as anticancer agents16. Proteasomes play an important role in cell survival and proliferation and were thus approved by Food and Drugs Association (FDA) in 2003 as anticancer agents. 6,16 Proteasomes are also crucial in pharmacology as they were utilized in making of the drugs necessary for the treatment of relapsed multiple myeloma (MM).

Drugs That Has Pyrazole Skeleton in Their Structure and The Important of Them as Anticancer and Antimicrobial or Pharmacology

Cancer fighting Drugs Structure

Colchicine

Teniposide

Podophyllotoxin

5, 11-dimethyl-5H-indolo[2,3-b]quinoline (I DiMIQ)

Cisplatin (Tetramethylxantin-8-ylidenePtII Complex)

Figure SEQ Figure \* ARABIC 1: Drugs that have pyrazole skeleton in their structure

Drugs that have pyrazole skeleton a helpful because medical chemists can use the MCR approach to generate systematic SAR data19. Besides, they can be used together with other aromatic and heteroaromatic amines to help in the preparation of anticancer drugs. Drugs that contains pyrazoles skeleton are crucial in pharmacology because they can act as intermediaries and converted to other substituted forms of pyrazoles drug that can terminated the activities of cancellous cells.

Structures of Four Known Natural Products That Has Pyrazole Skeleton and The Important of Them as Anticancer

Natural Products Structure

Tryptophan-rich catonic antimicrobial polymers

IEMA

Arginine

Tryptophan

Lysine

Figure SEQ Figure \* ARABIC 2:structures of four known natural products that has pyrazole skeleton

The structure of natural products is diverse such that it can portray multiple biological activities. The chemotherapeutic drugs that are derived from natural product is about 60%18. Natural products that have pyrazoles skeleton in their structures are crucial in antimicrobial because of their reduced prevalence of resistance and their ability to bind as a way of disrupting membrane function. Similarly, the natural products containing pyrazoles skeleton in their structure are of paramount importance in pharmacology because they provide hope for the possibility of the development of drugs that can help to overcome the antibiotic resistance that is currently being experienced in the health systems3, 18. Podophyllotoxin for instance, is a natural product containing pyrazole and which has been of great use in pharmacology, especially in preparation of cancer fighting drugs such as etoposide, etoposide phosphate and teniposide18.

Pyrazole Known Synthesis That Has Four Equations (Reactions)

Pyrazole known Synthesis Structure

Pyrimidine synthesis

Figure SEQ Figure \* ARABIC 3: Pyrazole Known Synthesis That Has Four Equations

Pyrimidine synthesis is crucial in antimicrobial as it uses Dihydroorotate dehydrogenase (DHODase) during the formation reactions. Pyrimidine is a critical target for the antibacterial therapy due to the fact that H. Pylori solely depends on the biosynthesis of the pyrimidines.4

Acid Important in Chemistry and Pharmacology

Acids are chemical agents that are able to release hydrogen ions when they are added into the water. Their chemistry allows them to be one of the most important classes of molecule in nature and science. Acid have been identified to be important in the discovery of drugs under various guidelines and scrutinization of their properties. All the acids are required to release hydrogen ions into the solutions and the amount will be able to determine whether the acid was weak or strong. Weak acids include acetic acid and citric acid while the strong acid involves hydrochloric acid and sulfuric acid. Moreover, some molecules can act as acids for instance the adenosine triphosphate which is used in the building of body energy and amino acids which is used as the building block of protein.

Berkelic acid for example has properties such as nano-molar activity against OVCAR-3 against an ovarian cancer cell line21. The basic function of lactic acid is to prompt the muscles to produce energy for the mitochondria. In the pharmacology context, however, lactic acidic is used to dissociate hydrogel allowing effective separation of boronate ester as well as bridging the gap between stabilized complex between the lactic acid and boronic acid substituent. Of most importance in the fact that lactic acid exists in cancer cells hence a cross-linked hydrogel portrays a stimuli-responsive matrix for the controlled release of gossypol22. Pharmacologists are able to use the properties of acid to determine how it affect them, for example some drugs with acidic properties like aspirin increases the chances of stomach bleeding if the condition becomes adverse.

Salicylic acid has been a natural remedy which was used to provide pain relief. Salicylic is made from the synthesis of salicin. Acid has been used to form drugs like aspirin which act as analgesic, antipyretic and anti-inflammatory drug. It allows the prevention of aggregation of platelets and it is also indicated that it can prevent stroke. It is therefore a preferred drug treatment that is responsible for rheumatoid arthritis treatment and also in the treatment of osteoarthritis.

Carboxylic acid make up a series of fatty acids that is extremely useful for human. The omega -6 and omega-3 are essential fatty acids not produced in the body and they help to maintain the cell membrane and control nutrients with direct rush into the blood stream. In the pharmaceutical industry, organic acids are used in many drugs like phenacetin28. Acetic acids can be used in making vinegar and sodium salts. Most acids are used in the industries to manufacture fertilizers, dyes, paints and man-made fibers.

The Structure of Five Known Drugs with Their Structure That Has Acid in Their Structure and The Important of Them as Anticancer and Antimicrobial

Drug Structure

Heparin

1Methyl-1,4- dihydroindeno...

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