scholarly journals Biological Activity of Naturally Derived Naphthyridines

Molecules ◽  
2021 ◽  
Vol 26 (14) ◽  
pp. 4324
Author(s):  
Gabriela Chabowska ◽  
Ewa Barg ◽  
Anna Wójcicka

Marine and terrestrial environments are rich sources of various bioactive substances, which have been used by humans since prehistoric times. Nowadays, due to advances in chemical sciences, new substances are still discovered, and their chemical structures and biological properties are constantly explored. Drugs obtained from natural sources are used commonly in medicine, particularly in cancer and infectious diseases treatment. Naphthyridines, isolated mainly from marine organisms and terrestrial plants, represent prominent examples of naturally derived agents. They are a class of heterocyclic compounds containing a fused system of two pyridine rings, possessing six isomers depending on the nitrogen atom’s location. In this review, biological activity of naphthyridines obtained from various natural sources was summarized. According to previous studies, the naphthyridine alkaloids displayed multiple activities, i.a., antiinfectious, anticancer, neurological, psychotropic, affecting cardiovascular system, and immune response. Their wide range of activity makes them a fascinating object of research with prospects for use in therapeutic purposes.

2021 ◽  
Vol 9 (5) ◽  
pp. 1036
Author(s):  
Dongmei Lyu ◽  
Levini A. Msimbira ◽  
Mahtab Nazari ◽  
Mohammed Antar ◽  
Antoine Pagé ◽  
...  

Terrestrial plants evolution occurred in the presence of microbes, the phytomicrobiome. The rhizosphere microbial community is the most abundant and diverse subset of the phytomicrobiome and can include both beneficial and parasitic/pathogenic microbes. Prokaryotes of the phytomicrobiome have evolved relationships with plants that range from non-dependent interactions to dependent endosymbionts. The most extreme endosymbiotic examples are the chloroplasts and mitochondria, which have become organelles and integral parts of the plant, leading to some similarity in DNA sequence between plant tissues and cyanobacteria, the prokaryotic symbiont of ancestral plants. Microbes were associated with the precursors of land plants, green algae, and helped algae transition from aquatic to terrestrial environments. In the terrestrial setting the phytomicrobiome contributes to plant growth and development by (1) establishing symbiotic relationships between plant growth-promoting microbes, including rhizobacteria and mycorrhizal fungi, (2) conferring biotic stress resistance by producing antibiotic compounds, and (3) secreting microbe-to-plant signal compounds, such as phytohormones or their analogues, that regulate aspects of plant physiology, including stress resistance. As plants have evolved, they recruited microbes to assist in the adaptation to available growing environments. Microbes serve themselves by promoting plant growth, which in turn provides microbes with nutrition (root exudates, a source of reduced carbon) and a desirable habitat (the rhizosphere or within plant tissues). The outcome of this coevolution is the diverse and metabolically rich microbial community that now exists in the rhizosphere of terrestrial plants. The holobiont, the unit made up of the phytomicrobiome and the plant host, results from this wide range of coevolved relationships. We are just beginning to appreciate the many ways in which this complex and subtle coevolution acts in agricultural systems.


2021 ◽  
Vol 22 (1) ◽  
Author(s):  
Magdalena Woźniak ◽  
Anna Kwiatkowska ◽  
Elżbieta Hołderna-Kędzia ◽  
Katarzyna Sosnowska ◽  
Lucyna Mrówczyńska ◽  
...  

Introduction. Propolis, also known as bee glue, is a resinous material collected by honeybees with numerous biological properties, including antibacterial, antifungal, antioxidant and anticancer effects. Due to its health-promoting properties, propolis is a component of many products, including dietary supplements, cosmetics and healthy food. Aim. The aim of the study was to determine the antibacterial, antifungal and antioxidant activity of propolis extracts, as well as to compare the biological activity of propolis extracts, depending on the solvent used – ethyl alcohol or propylene glycol. Material and methods. Two propolis extracts were used in the research – the first was prepared in ethyl alcohol, and the second in propylene glycol. The antimicrobial activity of the examined extracts was determined against S. aureus, E. coli and C. albicans. The antioxidant activity was determined on the basis of the evaluation of their antiradical activity in the DPPH· test and Fe2+ chelating activity. Moreover, the total content of phenolic compounds and flavonoids in the tested extracts was determined using the colorimetric method. Results. The tested propolis extracts, regardless of the solvent used (ethyl alcohol or propylene glycol), showed high antibacterial (against S. aureus), antifungal (against C. albicans) and antioxidant (antiradical activity in the DPPH· test and ferrous iron chelating potency in the ferrozine test) activity. Moreover, both tested extracts were characterized by a high and similar content of bioactive compounds – phenolic compounds and flavonoids. Conclusions. The results of the conducted tests showed that the solvent used did not affect determined biological activity and the content of bioactive substances in the tested propolis extracts.


2021 ◽  
Vol 37 (5) ◽  
pp. 1158-1166
Author(s):  
S.Syed Shafi ◽  
R. Rajesh ◽  
R. Subaash ◽  
S.Senthil kumar

Recently, heterocyclic compounds play important role in drug industries. The benzothiazole (BTA) is a bicyclic compound in heterocyclic because of their biological properties. In this paper the synthesis and characterization of benzothiazole were reported. The chemical structures of synthesized compounds were established based on spectral data of 1HNMR, 13CNMR, and IR. The mass of the novel compounds was established with the help of the LCMS test. The formation of the crystal was confirmed by powder XRD and the sharp peaks show the purity and crystalline nature of the samples. The photoluminescence spectra explain the optical property of the compound. The biological studies of synthesized compounds show that compound 5c possesses good antibacterial activity and compound 5d has good antifungal activity.


2018 ◽  
Vol 73 (3) ◽  
pp. 83-95
Author(s):  
KATARZYNA OLESIŃSKA

Sesquiterpene lactones are secondary metabolites commonly found in higher plants as well as mosses, lichens, and fungi. Currently, over 5000 of such compounds have been identified with a majority isolated from Asteraceae plants. They are characterised by different chemical structures associated with the presence of various carbon pathways and functional groups, which exert an impact on their pharmacological activity. These colourless substances are soluble in fats, alcohols, or water. They are often bitter ingredients regarded as bitter compounds. They are accumulated mainly in leaves, flower parts and seeds; less frequently, they are present in roots. Sesquiterpene lactones exhibit multidirectional biological activity: some of them have anticancer, anti-inflammatory, antidiabetic, analgesic, antiparasitic, antifungal, and bacteriostatic effects. Therefore, high hopes are placed on the medical and pharmaceutical use of these substances. Lactone compounds are also regarded as a potential source of new active substances used in agriculture to combat plant pathogens


2019 ◽  
Vol 11 (15) ◽  
pp. 1979-1998 ◽  
Author(s):  
Mehmet Gümüş ◽  
Mehmet Yakan ◽  
İrfan Koca

Thiazoles have attracted much synthetic interest due to their wide variety of biological properties and are important members of heterocyclic compounds. In recent years, studies on the synthesis of thiazole compounds have been increasing because of the properties of this core. In particular, the hybrid structures in which the thiazole ring and the other nuclei are linked have gained popularity. Hybrid structures are formed by the combination of different groups of chemical reactivity and biological activity characteristics. In this review, we highlight recent developments related to hybrid structures containing a thiazole core, recently developed as anticancer, antibacterial, anti-inflammatory, analgesic, anti-tubercular, antialzheimer and antidiabetic compounds.


2019 ◽  
Vol 65 (2) ◽  
pp. 99-102 ◽  
Author(s):  
Yu.V. Butina ◽  
T.V. Kudayarova ◽  
E.A. Danilova ◽  
M.K. Islyaikin

The work is devoted to predicting and studying biological properties of N-substituted analogs of 3,5-diamino-1,2,4-thiadiazole, which, in their turn, include in the composition of many drugs that exhibit a wide range of pharmacological actions. For searching of new alternative drugs with an antibacterial activity, but lacking resistance of microorganism strains to them, a computer screening of 2N-alkyl-substituted 5-amino-3-imino-1,2,4-thiadiazolines previously synthesized by us was carried out. The prediction of the spectrum of biological activity, as well as the determination of the probable toxicity of these compounds, was performed using the freely available computer programs PASS, Anti-Bac-Pred, and GUSAR. The study of the antibacterial activity in vitro against gram-positive (Staphylococcus aureus, Staphylococcus saprophyticus, Staphylococcus epidermidis) and gram-negative (Escherichia coli, Pseudomonas aeruginosae) bacterial strains was performed by the disco-diffusion method. Experimental data roughly correspond to the predictions.


2021 ◽  
Author(s):  
Lali Tabatadze ◽  
Neli Sidamonidze ◽  
Darejan Gulbani ◽  
Darejan Iremashvili

Carbohydrate derivatives are distinguished with wide range of biological activity which is proven by successful usage of preparations made of Carbohydrate based in different branches of pharmaceutical chemistry. As a result of research of Carbohydrate compounde, the relationship between unique structure and its chemical and biological properties has been studied. Input of bulk liphophilic adamantine moiety in the proved medications or biologically active molecule in most cases is improved molecule’s biological characteristic, drug’s lipopilycity and prolonged actin is enhanced, and at the same time toxicity and side negative effects is reduced.We studied the reactions of acetylaryl glycosides with phenylsulfonyl chloride in the presence of a benzoyl peroxide catalyst. A new sulfur-containing glucoside was synthesized: Hepta-O-acetyl-1-O-(2-chloro-3-phenyl thio propyl)-β-D-maltose. The bactericidal properties of β-O-(2-chloro-3-phenyl thio propyl)-D-maltose of the obtained product after deacetylation were studied. With the help of the com­­pu­ter program PASS (Prediction of Activity Spectra for Substance) onlaines were able to predict the range of activity of substances. The obtained result established correlations on bactericidal properties between biological activity and the intended biological activity. The structure of the synthesized compounds was determined by physico-chemical research methods.


2020 ◽  
Vol 20 (3) ◽  
pp. 196-218
Author(s):  
Rajiv K. Tonk ◽  
Sandhya Bawa ◽  
Deepak Kumar

Cinnoline or Benzo-pyridazine has its place in the family of fairly well-known benzfuseddiazine heterocycles. Because of its natural occurrence and synthetic exploration, cinnoline compounds validated its thought-provoking bioactivity through a number of research publications and patents during last few decades. A creative consideration has been rewarded to the synthesis of cinnoline based heterocyclic compounds, mostly due to their wide range of diverse pharmacological activities. The present review covers the principle approaches to the synthesis of cinnoline nucleus and almost all biological properties of 115 cinnoline derivatives reported during the last 65 years from natural and synthetic origin with 140 references.


2019 ◽  
Vol 16 (1) ◽  
pp. 17-37 ◽  
Author(s):  
Jaskirat Kaur ◽  
Divya Utreja ◽  
Ekta ◽  
Nisha Jain ◽  
Shivali Sharma

Background:Heterocyclic compounds containing nitrogen have been known to possess a very important role in the field of medicinal chemistry. Indole and its derivatives displayed a wide range of biological properties such as anti-inflammatory, analgesic, anti-microbial, anti-convulsant, antidepressant, anti-diabetic, antihelmintic and anti-allergic activities etc. The diverse biological activities exhibited by compounds containing indole moiety has provided the impetus to explore its anti-microbial activity in order to save the valuable life of patients. </P><P> Objective: The review focuses on the advances in the synthesis of indole derivatives and antimicrobial properties exhibited by them.Conclusion:A great deal of work has been done in order to synthesize indole derivatives and to evaluate antimicrobial potential, as indicated by the review. The information provided in this article may be helpful for the researchers for the development of efficient antimicrobial drugs.


2020 ◽  
Vol 07 ◽  
Author(s):  
Archana Dhakar ◽  
Archana Rajput ◽  
Ghazala Khanum ◽  
Dau D. Agarwal

Background,Objective: : spiro[indoline-3,4′-pyrano[2,3-c]pyrazoles] derivatives are an important heterocyclic compounds. These compounds shows wide range of biological properties and exhibits varied pharmaceutical applications. Pyranopyrazoles, which are basically fused heterocyclic compounds and act as vasodilators, hypertensive, hypoglycaemic, and anticancer agents. Methods: An efficient and micelle-promoted surfactant catalyzed synthesis of spiro[indoline-3,4′-pyrano[2,3-c]pyrazoles] derivatives have been achieved via one-pot four-component reaction of hydrazine hydrate (phenyl hydrazine), ethyl acetoacetate, malononitrile (ethyl cyanoacetate) and isatin under thermal conditions (at 60°C) in water as a solvent. Results: Sodium lauryl sulphate (SLS) used has been found to be an efficient and green catalyst. The compounds reported during this work were obtained in excellent yield, in a short duration of time and ease of work up. They were purified by recrystalization from ethanol, and also the synthesized compounds were characterized by various spectroscopic techniques. Conclusion: The method offers several advantages such as safe, cost-effective and catalyst easily recovered and reused for a minimum of five cycles, that confirms its good stability. Short reaction times, high yield and usage of eco-friendly catalyst and solvent are the key features of this methodology.


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