In the present investigation, the synthesis and antimicrobial evaluation of 1,2,4-triazolo [3,4-b][1,3,4] thiadiazine including different pharmacophores are aimed at. In this study, a series of 6-aryl-3- (3,4 -dialkoxyphenyl)-7H -[1,2,4]triazolo [3,4-b][1,3,4] thiadiazine (7a-7k) was synthesized by condensing 4-amino-5-(3,4-dialkoxyphenyl)-4H-[1,2,4]- triazole-3-thiol (6) with various aromatic carboxylic acids in the presence of phenacyl bromides through one-pot reaction. Eleven fused heterocyclic derivatives were successfully synthesized. The structures of these newly synthesized compounds were characterized by IR, 1H NMR and mass spectroscopic studies. All the synthesized compounds were screened for their antimicrobial evaluation. Some of the compounds exhibited promising antimicrobial activity. From the present study it may be concluded that synthesized compounds are fruitful in terms of their structural novelty and marked biological activities. These compounds could be further modified to develop potential and safer antifungal agents.
In the field of heterocyclic medicinal chemistry, especially five-membered ring
structures containing a nitrogen atom, imidazole core is an imperative aromatic heterocycle which
is usually present in naturally occurring products and synthetic bioactive molecules. The
occurrence of imidazole moiety in therapeutic compounds may be beneficial in terms of improving
water-soluble properties due to its two nitrogen atoms which leads to the creation of hydrogen
bonds. The imidazole nucleus has also been recognized as an important isostere of triazole,
pyrazole, thiazole, tetrazole, oxazole, amide etc. for the purpose of designing and development of
various biologically active molecules. Moreover, imidazole core as an attractive binding site could
interact with diverse cations and anions as well as biomolecules through different reactions in the
human biological system thus displaying extensive biological activities. This effort thoroughly
provides a wide-ranging assessment in current drug discovery and developments of imidazolebased
analogues in the entire series of synthetic medicinal chemistry as antibacterial and
antifungal, anticancer, anti-tubercular, analgesic and anti-inflammatory, anti-neuropathic,
antihypertensive, anti-allergic, anti-parasitic, antiviral, antidepressant, anti-obesity and so on,
altogether with their prospective approaches in diagnostic and pathological field. It is expected
that the present review will be supportive on behalf of new opinions in the search for rational
strategies of more efficacious and less toxic medicinal agents and drugs containing imidazole core.
Background:
Oxadiazole core displays various pharmacological properties among five membered nitrogen
heterocyclic compounds specially 1,3,4-oxadiazole containing molecules have occupied a particular place in the field of
synthetic medicinal chemistry as surrogates (bioisosteres) of carboxylic acids, carboxamides and esters. Moreover, they are
having widespread kind of applications in numerous zones as polymers, as luminescence producing materials and as
electron-transporting materials and corrosion inhibitors.
Methods:
This write up contains comprehensive and extensive literature survey on chemical reactivity and biological
properties associated with 1,3,4-oxadiazole containing compounds.
Results:
This review summarises 1,3,4-oxadiazole moiety in numerous compounds with reported pharmacological activity
such as antiviral, analgesic and anti-inflammatory, antitumor, antioxidant, insecticidal and anti-parasitic etc. Nevertheless,
ring opening reactions of the 1,3,4-oxadiazole core have also made great attention, as they produce new analogues
containing aliphatic nitrogen atom and to other ring system.
Conclusion:
In relation to occurrence of oxadiazoles in biologically active molecules, 1,3,4-oxadiazole core emerges as an
structural subunit of countless significance and usefulness for the development of new drug aspirants applicable to the
treatment of many diseases. It concludes that 1,3,4-oxadiazole core compounds are more efficacious and less toxic medicinal
agents with respect to new opinions in the search for rational strategies.
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