Application of heterocyclic compounds
Application of heterocyclic compounds
In
an organic chemistry, largest families of organic compounds are belongs in the
heterocyclic compounds. In ourdaily life important of heterocyclic compounds
are of very essential. It has broad range of application in medicinal chemistry
and in agrochemicals products.
Applications
of the heterocyclic compounds in detail are following below;
1.
Medicinal
chemistry:
Heterocycles have been found a key structural in medical chemistry
and also they are frequently found in large percent in biomolecules such as
enzyme, vitamins, natural products and biological active compounds including
antifungal, anti-inflammatory, antibacterial, antioxidant, anti-convulsant,
anti-allergic, enzyme inhibitors, herbicidal activity, anti-HIV, anti-diabetic,
anticancer activity, insecticidal agents.
·
Antifungal
activity:
It is substances or medications that used to treats the fungal
infection which is most commonly located on the skin, hair and nails. There are
some common fungal infections such as ringworm and athlete's foot, etc. The
effect of antifungal medicine either by killing the fungal cells due to
affecting on the substances of the cell membrane which is lead to cells
components leak out and cell die.
Anotherway by preventing the growth and reproduction of the fungal
cells.
Molnaretal have
synthesized a series of dipicolinic acid derivatives, some of it show
antifungal activity against fungal strains called Aspergillusflavus,
Aspergillusochraceus, Fusariumgraminearum and Fusariumverticilioides.
Chitraetal have
synthesized indole 3-acetic acid based biopolymeric hydrogels, this compounds
also show activity against fungal infections and tested of several type of
fungi including, Aspergillus fumigates, Rhizopusoryzae and Candida albicans at
different concentrations using ketoconazole as positive control and Dimethyl
Sulfoxide (DMSO) as negative control for antifungal activity.
·
Anti-inflammatory
activity:
Is a term referring to the substances that used to treatment or
reduces inflammations or swelling. Analgesic makes up about half of anti-inflammatory
drugs. Relieving pain by reducing inflammation as opposed to opioids which
affect the central nervous system, to block painsignaling to the brain. The
most common anti-inflammatory drugs are aspirin and ibuprofen and naproxen,
this type of anti-inflammatory calledNon-steroidal Anti-inflammatory Drug
(NSAIDs), this term recognizes these drugs from steroids. The mechanism of
actions of these drugsincludes inhibiting the activity of Cyclooxygenase (COX)
enzymes. The activity of these enzymes is in the metabolism of arachidonic
acid.Isoenzymes of cyclooxygenase may be the target of certain NSAIDs.
Sawhney and Bhutani
have prepared some novel 2-(2-benzothiazolyl)-6-aryl-4, 5-dihydro-3(2
H)-pyridazinone and found that they possessedlow to moderate anti-inflammatory
activity.
Ghattasetal have synthesized some of
4,6-Diamino-3-cyano-2-methylthiopyridine derivatives and proved this compounds
have anti-inflammatory by carrageenan-induced pawoedema standard method in
rats,
·
Antibacterial
activity:
Antibacterial or antibiotics is a term that used to describe the
drugs which are used for prevention or treatment of bacterial infections,
either by killing or inhibit the growth of bacteria. The antiprotozoal activity
also related to some of the antibiotics. Antibiotics do not effective against
viral infections such as the common cold or influenza. The emergence of resistant
organisms may happen if the using of antibiotics was inappropriate. The
classification of antibiotics is according to the mechanisms of actions or
chemical structural. Aromatic heterocyclic derivatives represent an important
part of antibiotics chemical structure such as β-lactam derivatives, and there
are a lot of chemists’ have been synthesis many compounds have this type of
activity and tested it on several types of bacteria. We will review some of
this works in recent two years.
Abbas and Zimam have
been synthesized some new pyrimidine and 1,2,3,4-tetrazole derivatives based on
sulfadiazine and tested these compounds on two types of bacteria Streptococcus
spp., (Gram-positive bacteria) and Porphyromonasgingivalis (Gram-negative
bacteria).
2.
In cancer
therapy:
The technology and reasoning behind drug design are closely
interrelated to the pre mediated inclusion of heterocyclic fragments with
explicit physicochemical characteristics. Effectiveness and discernment through
bio isosteric substitutions, lipophilicity, polarity, and aqueous solubility
can eventually be modified to the point of changing and conditioning the
possible mechanisms of action of heterocyclic drugs in an effort to attain
molecularly targeted therapeutic agents. Regardless of their flexibility and
effectiveness, as for any other therapeutics, there are many issues obstructing
broader application and auxiliary expansion of such compounds into market
drugs. Treatment of cancer is perhaps most widely suffering health care event
due to the inherent confines regarding foremost therapeutic routes of
chemotherapy, attendant side effects and toxicity to unaffected healthy cells.
Such venomous effects may be skirted by selective targeted drug delivery
approaches directly into malignant cells. With respect to this, nanostructure
based delivery tools are the most attractive solutions associated with various
cancer chemotherapy hindrances. In order to circumvent the poor physicochemical
characteristics of many therapeutic heterocyclic compounds including their
pharmacokinetic and dynamic properties and advance their use towards clinical
translation, numerous formulation development studies have been conducted using
various nanostructured systems. The nanostructured heterocyclic compounds are
capable enough to bind and/or encapsulate with targeting carrier and allows the
exploit of improved cell permeability and retaining effect appropriate for
malignant targeting. This facilitates for an accumulated concentration of
therapeutic agent at the tumor site with a resultant increase in efficiency
while decreasing the unwanted side effects and avoids effecting healthy cells.
The surface nanocarriers may be conjugated with extra targeting moieties to
enhance the selectivity towards malignant tissues with specific overexpressed
receptors, and/or other biomarkers. Nanostructured carrier systems include
polymeric nanoparticles, liposomes; albumin bound metallic nanoparticles, and
dendrimers. Regardless of widespread nanomaterials are in use, encapsulated
nanostructures such as polymeric nanoparticles and liposomal formulations are
found to be serving most favourable with more than 30 nano formulations in ongoing
clinical trials.
3.
In Agrochemistry:
the different roles of heterocyclic scaffolds in crop protection
agents and the major possibilities for their synthesis are take place. An overview
is given of the significance of heterocycles in crop protection chemistry,
which is enormous as more than two-thirds of all agrochemicals launched to the
market within the last 20 years belong to this huge group of chemicals.
The chemistry of heterocycles is an important branch of organic
chemistry. This is due to the fact that a large number of natural products, e.
g. hormones, antibiotics, vitamins, etc. are composed of heterocyclic
structures. Often, these compounds show beneficial properties and are therefore
applied as pharmaceuticals to treat diseases or as insecticides, herbicides or
fungicides in crop protection. This volume presents important agrochemicals. A
valuable one-stop reference source for researchers in academia and industry as
well as for graduate students with career aspirations in the agrochemical
chemistry. The agrochemicals or agrochemistry deals with theamino acids;
bioisosteres; fungicides; herbicides; heterocycles; heterocyclization;
insecticides; multicomponent reactions; propesticides.
4.
In
industries:
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