ChemInform Abstract: Utility of Octadecyl Amine in the Synthesis of Various Nitrogen Heterocycles: A Preliminary Investigation on Their Surface and Biological Activities.

ChemInform ◽  
2016 ◽  
Vol 47 (43) ◽  
Author(s):  
Refat El-Sayed ◽  
Saleh A. Ahmed
Molecules ◽  
2020 ◽  
Vol 25 (15) ◽  
pp. 3508
Author(s):  
Carme Masdeu ◽  
Maria Fuertes ◽  
Endika Martin-Encinas ◽  
Asier Selas ◽  
Gloria Rubiales ◽  
...  

Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in the fields of synthetic organic chemistry and play an important role in the field of medicinal chemistry, as many of them have a wide range of biological activities. In this review, a wide range of synthetic protocols for the construction of this scaffold are presented. For example, Friedländer, Skraup, Semmlere-Wolff, and hetero-Diels-Alder, among others, are well known classical synthetic protocols used for the construction of the main 1,5-naphthyridine scaffold. These syntheses are classified according to the nature of the cycle fused to the 1,5-naphthyridine ring: carbocycles, nitrogen heterocycles, oxygen heterocycles, and sulphur heterocycles. In addition, taking into account the aforementioned versatility of these heterocycles, their reactivity is presented as well as their use as a ligand for metal complexes formation. Finally, those fused 1,5-naphthyridines that present biological activity and optical applications, among others, are indicated.


2019 ◽  
Vol 8 (3) ◽  
pp. 21-24
Author(s):  
Anandika Suryavanshi ◽  
Anand Murari Saxena

The present study was carried out for the determination of bioactive compounds from different extracts of Terminalia catappa and Rumex vesicarius. The plants are mines of several bioactive compounds also called as phytochemical compounds. These bioactive compounds are responsible for imparting such a potential medicinal property in the plants. The medicinal plant contains various types of bioactive compounds including phenols, alkaloids, terpenoids, tannins, glycosides, flavonoids etc. These bioactive compounds take part in various metabolic pathways and impart their effect. Terminalia catappa and Rumex vesicarius are such medicinal plants which are being used for medicinal purposes for long time. Both of them are rich source of potential bioactive compounds and hence carry out several biological activities effective for the treatment of various diseases. Hence the study focuses on determining the types of bioactive compounds they acquire. For this the leaves of T. catappa and dry stems of R. vesicarius were used for the extraction using different solvents with soxhlet method. The extract of different solvents was analyzed for the phytochemical test. The results obtained revealed that the type of solvents is crucial in determining the type of bioactive compounds to be present in extract. The results showed that ethanol and methanol are good solvent choice for extraction for these two plants. The results concludes that the presence of such potential and effective bioactive compounds in their extract makes them important medicinal plants and are hence employed for several researches and also used for treatment of various kinds of diseases.


2010 ◽  
Vol 5 (5) ◽  
pp. 1934578X1000500
Author(s):  
Ilef Limem-Ben Amor ◽  
Nidhal Salem ◽  
Emmanuel Guedon ◽  
Jean-Marc Engasser ◽  
Leila Chekir-Ghedrira ◽  
...  

Flavonoid hydroxylation is one way to increase the biological activities of these molecules and the number of hydroxyl groups needed for polymerization, esterification, alkylation, glycosylation and acylation reactions. These reactions have been suggested as a promising route to enhance flavonoid solubility and stability. In our preliminary study we hydroxylated naringenin (the first flavonoid core synthesized in plants) with recombinant E. coli harboring flavanone 3 hydroxylase (F3H). We demonstrated that recombinant E. coli harboring the F3H from Petroselinum crispum, can convert naringenin to dihydrokaempferol. The whole cell hydroxylase activity was often influenced by the stability of the plasmid harboring the cloned gene and the biomass yield. When the composition of the growth media became richer the amount of formed product decreased about twofold; the naringenin bioconversion yield in LB media was 70% and decreased to 33% in TB. However, the enrichment of culture media increased the biomass yield nearly threefold in LB media, only 0.5 g/L of bacteria was formed, but in TB there was 1.6 g/L. Thus, LB constitutes the best medium for naringenin bioconversion using the recombinant E. coli harboring the F3H; this allows for maximum bioconversion yield and plasmid stability when compared with the fourth tested culture medium. Consequently, E. coli harboring F3H from Petroselinum crispum can be used to produce flavonoids hydroxylated in position 3 that can serve in additional reactions like polymerization, glycosylation, and acylation,


Nutrients ◽  
2018 ◽  
Vol 10 (10) ◽  
pp. 1369 ◽  
Author(s):  
Ali El-Far ◽  
Soad Al Jaouni ◽  
Weikun Li ◽  
Shaker Mousa

The focus on nanotechnology for improved bioavailability and drug delivery is of increasing importance for control of different human diseases. Therefore, numerous nanoformulations have been developed for the oral bioavailability of different drugs. This review introduces applications of nanomedicine to enhance the biological activities of thymoquinone (TQ) to control different diseases in several in vivo studies as a preliminary investigation for human disease treatment with nano-TQ. Nano-TQ effectively augments the anticancer roles of doxorubicin by upregulation of P53 and downregulation of Bcl2 and potentiates paclitaxel’s apoptosis in MCF-7 breast cancer cells. Moreover, nano-TQ protects against diabetes, inflammation, CNS, and hepatotoxicity, mainly by enhancement of organs’ antioxidant status. We summarize the pros and cons of several FDA approved nanoparticle-based therapeutics and discuss the roadblocks in clinical translation, along with potential nano-TQ strategies to overcome these roadblocks. From this review, we can conclude that nano-TQ may be considered as a promising nutraceutical for human health.


Marine Drugs ◽  
2021 ◽  
Vol 19 (9) ◽  
pp. 514
Author(s):  
Kevin Seipp ◽  
Leander Geske ◽  
Till Opatz

Nitrogen heterocycles are essential parts of the chemical machinery of life and often reveal intriguing structures. They are not only widespread in terrestrial habitats but can also frequently be found as natural products in the marine environment. This review highlights the important class of marine pyrrole alkaloids, well-known for their diverse biological activities. A broad overview of the marine pyrrole alkaloids with a focus on their isolation, biological activities, chemical synthesis, and derivatization covering the decade from 2010 to 2020 is provided. With relevant structural subclasses categorized, this review shall provide a clear and timely synopsis of this area.


2021 ◽  
Vol 17 (1) ◽  
pp. 011-025
Author(s):  
Ugochukwu Moses Okezie ◽  
Peter Maduabuchi Eze ◽  
Festus Basden Chiedu Okoye ◽  
Charles Okechukwu Esimone

Endophytic fungi have demonstrated a harmless relationship living within the internal tissues of several plant hosts and at the same time produce diverse important bioactive compounds having a wide range of pharmaceutical applicability. In this study, nine endophytic fungi, eight from Cassava leaf: Clg1, Clg2, Clr4, Clr5, Clr6, Clr7, Clr9 and one from Cassava mid-rib: CRs3 with distinct cultural features were isolated from healthy leaves of Manihot utilisima and axenic cultures were fermented on sterile rice medium for 21 days. The antimicrobial and antioxidant activities of the fungal crude extracts were evaluated. Chemical analyses of the metabolic profiles of each fungal extract revealed the presence of nine known compounds with established biological activities. Each fungal extract exhibited antimicrobial activities against at least one Gram positive and Gram negative bacteria with an inhibition zone that ranged from 2 – 6 mm. Clg2 and CRs3 fungal extracts demonstrated moderate potential to scavenge free radical with an inhibition of 58 and 60% respectively. Septicine, cyclo(prolylvalyl), pentenedioc acid, neurolenin B, rubrofusarin, p-Hydroxybenzoic acid, protocatechuic acid, citreoisocoumarin, palitantin and pestalio pyrone were the compounds detected in the fungal fermentation products. Our findings reveal that M. utilisima leaves harbor endophytic fungi with unique chemodiversity of bioactive secondary metabolites needed for development of new drugs.


ChemInform ◽  
2003 ◽  
Vol 34 (44) ◽  
Author(s):  
H. M. Hirpara ◽  
V. A. Sodha ◽  
A. M. Trivedi ◽  
B. L. Khatri ◽  
A. R. Parikh

Marine Drugs ◽  
2020 ◽  
Vol 18 (1) ◽  
pp. 54 ◽  
Author(s):  
Xu ◽  
Yuan ◽  
Li ◽  
Li

Nitrogen heterocycles have drawn considerable attention due to of their significant biological activities. The marine fungi residing in extreme environments are among the richest sources of these basic nitrogen-containing secondary metabolites. As one of the most well-known universal groups of filamentous fungi, marine-derived Aspergillus species produce a large number of structurally unique heterocyclic alkaloids. This review attempts to provide a comprehensive summary of the structural diversity and biological activities of heterocyclic alkaloids that are produced by marine-derived Aspergillus species. Herein, a total of 130 such structures that were reported from the beginning of 2014 through the end of 2018 are included, and 75 references are cited in this review, which will benefit future drug development and innovation.


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