scholarly journals The Methylene-Cycloalkylacetate (MCA) Scaffold in Terpenyl Compounds with Potential Pharmacological Activities

Molecules ◽  
2019 ◽  
Vol 24 (11) ◽  
pp. 2120 ◽  
Author(s):  
Ignacio E. Tobal ◽  
Alejandro M. Roncero ◽  
Rosalina F. Moro ◽  
David Díez ◽  
Isidro S. Marcos
Keyword(s):  
Neurite Outgrowth ◽  
Bioactive Compounds ◽  
Pharmacological Activities ◽  
Synthetic Derivatives ◽  
Derivatives Of

Recently, the methylene-cycloakylacetate (MCA) scaffold has been reported as a potential pharmacophore for neurite outgrowth activity. In this work, natural diterpenes that embed MCA fragments are reviewed, as they are major components of Halimium viscosum: ent-halimic acid, the prototype for these bioactive compounds. Herein, structures, sources, and activities for the natural diterpenes, as well as their synthetic derivatives of interest, are reviewed.

Synthetic derivatives of pulchrol: An antiparasitic natural product

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
P Terrazas ◽  
O Sterner
Keyword(s):  
Natural Product ◽  
Synthetic Derivatives ◽  
Derivatives Of

A Comprehensive Review on the Therapeutic Versatility of Imidazo [2,1-b]thiazoles

2020 ◽  
Vol 27 (40) ◽  
pp. 6864-6887 ◽  
Author(s):  
Mohd Adil Shareef ◽  
Irfan Khan ◽  
Bathini Nagendra Babu ◽  
Ahmed Kamal
Keyword(s):  
Literature Review ◽  
Medicinal Chemistry ◽  
Therapeutic Agents ◽  
Present Review ◽  
Thiazole Derivatives ◽  
Pharmacological Activities ◽  
Comprehensive Review ◽  
Derivatives Of

Background:: Imidazo[2,1-b]thiazole, a well-known fused five-membered hetrocycle is one of the most promising and versatile moieties in the area of medicinal chemistry. Derivatives of imidazo[2,1-b]thiazole have been investigated for the development of new derivatives that exhibit diverse pharmacological activities. This fused heterocycle is also a part of a number of therapeutic agents. Objective:: To review the extensive pharmacological activities of imidazo[2,1-b]thiazole derivatives and the new molecules developed between 2000-2018 and their usefulness. Method:: Thorough literature review of all relevant papers and patents was conducted. Conclusion:: The present review, covering a number of aspects, is expected to provide useful insights in the design of imidazo[2,1-b]thiazole-based compounds and would inspire the medicinal chemists for a comprehensive and target-oriented information to achieve a major breakthrough in the development of clinically viable candidates.

Flavones and Their Analogues as Bioactive Compounds – An Overview

2019 ◽  
Vol 16 (4) ◽  
pp. 377-391 ◽  
Author(s):  
B.S. Jayashree ◽  
H. Venkatachalam ◽  
Sanchari Basu Mallik
Keyword(s):  
Biological Activity ◽  
Free Radical ◽  
Bioactive Compounds ◽  
Antioxidant Properties ◽  
Radical Scavenging ◽  
Cost Effective ◽  
Free Radical Scavenging ◽  
Polyphenolic Compounds ◽  
Pharmacological Activities ◽  
Poor Solubility

Flavonoids constitute a large group of polyphenolic compounds that are known to have antioxidant properties, through their free radical scavenging abilities. They possess a chromone (γ- benzopyrone) moiety, responsible for eliciting many pharmacological activities. Even though, natural flavonoids are highly potent, owing to their poor solubility, they are less used. Therefore, attempts have been made to improve their stability, solubility, efficacy and kinetics by introducing various substituents on the flavone ring. For nearly the last two decades, flavones were synthesized in our laboratory by simple, convenient and cost-effective methods, with the knowledge of both synthetic and semi-synthetic chemistry. In this direction, it was considered worthwhile to present an overview on the synthesized flavonoids. This review creates a platform for highlighting various modifications done on the flavone system along with their biological activity.

Synthesis, Cytotoxicity and Antioxidant Activity of New Analogs of RC-121 Synthetic Derivatives of Somatostatin

2019 ◽  
Vol 18 (10) ◽  
pp. 1417-1424 ◽  
Author(s):  
Emilia Naydenova ◽  
Diana Wesselinova ◽  
Svetlana Staykova ◽  
Ivan Goshev ◽  
Ljubomir Vezenkov
Keyword(s):  
Antioxidant Activity ◽  
Antioxidant Capacity ◽  
Cell Line ◽  
Cancer Cell ◽  
Cancer Cell Line ◽  
Colorectal Cancer Cell Line ◽  
Cervical Cancer Cell Line ◽  
Synthetic Derivatives ◽  
Derivatives Of

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.

scholarly journals Cyanobacteria—From the Oceans to the Potential Biotechnological and Biomedical Applications

Marine Drugs ◽  
2021 ◽  
Vol 19 (5) ◽  
pp. 241
Author(s):  
Shaden A. M. Khalifa ◽  
Eslam S. Shedid ◽  
Essa M. Saied ◽  
Amir Reza Jassbi ◽  
Fatemeh H. Jamebozorgi ◽  
...  
Keyword(s):  
Bioactive Compounds ◽  
Biomedical Applications ◽  
Large Scale ◽  
Biological Activities ◽  
Scale Production ◽  
Pharmacological Activities ◽  
Large Scale Production ◽  
Marine Products ◽  
Hiv 1 ◽  
Successful Phase

Cyanobacteria are photosynthetic prokaryotic organisms which represent a significant source of novel, bioactive, secondary metabolites, and they are also considered an abundant source of bioactive compounds/drugs, such as dolastatin, cryptophycin 1, curacin toyocamycin, phytoalexin, cyanovirin-N and phycocyanin. Some of these compounds have displayed promising results in successful Phase I, II, III and IV clinical trials. Additionally, the cyanobacterial compounds applied to medical research have demonstrated an exciting future with great potential to be developed into new medicines. Most of these compounds have exhibited strong pharmacological activities, including neurotoxicity, cytotoxicity and antiviral activity against HCMV, HSV-1, HHV-6 and HIV-1, so these metabolites could be promising candidates for COVID-19 treatment. Therefore, the effective large-scale production of natural marine products through synthesis is important for resolving the existing issues associated with chemical isolation, including small yields, and may be necessary to better investigate their biological activities. Herein, we highlight the total synthesized and stereochemical determinations of the cyanobacterial bioactive compounds. Furthermore, this review primarily focuses on the biotechnological applications of cyanobacteria, including applications as cosmetics, food supplements, and the nanobiotechnological applications of cyanobacterial bioactive compounds in potential medicinal applications for various human diseases are discussed.

scholarly journals Pharmacological Insights into Halophyte Bioactive Extract Action on Anti-Inflammatory, Pain Relief and Antibiotics-Type Mechanisms

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3140
Author(s):  
Rocco Giordano ◽  
Zeinab Saii ◽  
Malthe Fredsgaard ◽  
Laura Sini Sofia Hulkko ◽  
Thomas Bouet Guldbæk Poulsen ◽  
...  
Keyword(s):  
Pain Relief ◽  
Bioactive Compounds ◽  
Biomedical Applications ◽  
Medicinal Products ◽  
Salt Tolerant ◽  
Salicornia Europaea ◽  
Pharmacological Activities ◽  
Sustainable Resources ◽  
Anti Inflammatory ◽  
Significant Attention

The pharmacological activities in bioactive plant extracts play an increasing role in sustainable resources for valorization and biomedical applications. Bioactive phytochemicals, including natural compounds, secondary metabolites and their derivatives, have attracted significant attention for use in both medicinal products and cosmetic products. Our review highlights the pharmacological mode-of-action and current biomedical applications of key bioactive compounds applied as anti-inflammatory, bactericidal with antibiotics effects, and pain relief purposes in controlled clinical studies or preclinical studies. In this systematic review, the availability of bioactive compounds from several salt-tolerant plant species, mainly focusing on the three promising species Aster tripolium, Crithmum maritimum and Salicornia europaea, are summarized and discussed. All three of them have been widely used in natural folk medicines and are now in the focus for future nutraceutical and pharmacological applications.

The synthesis of the isomeric N-methyl derivatives of murexine

1981 ◽  
Vol 34 (8) ◽  
pp. 1739 ◽  
Author(s):  
CC Duke ◽  
JV Eichholzer ◽  
JK Macleod
Keyword(s):  
Imidazole Ring ◽  
The Other ◽  
Pharmacological Activities ◽  
Tautomeric Forms ◽  
Methyl Derivatives ◽  
Paramagnetic Ions ◽  
Nucella Emarginata ◽  
Derivatives Of

The two isomeric N-methyl derivatives of murexine have been synthesised by independent routes and shown to be different from an 'N- methylmurexine' reportedly isolated from the mollusc Nucella emarginata. 1H n.m.r. studies have shown a marked difference in the extent of binding to paramagnetic ions of the two N-methyl derivatives of murexine in water while pharmacological results show substantially different pharmacological activities of the two isomers. Both results can be rationalized in terms of the observed activities being associated with the presence of one or the other of the tautomeric forms of the imidazole ring.

Semi-synthetic Derivatives of Heliomycin with an Antiproliferative Potency

2018 ◽  
Vol 13 ◽  
Author(s):  
A. E. Shchekotikhin ◽  
Georgy Y. Nadysev ◽  
Alexander S. Tikhomirov ◽  
Lyubov G. Dezhenkova
Keyword(s):  
Synthetic Derivatives ◽  
Derivatives Of

scholarly journals A Review on Ethnopharmacological Applications, Pharmacological Activities, and Bioactive Compounds ofMangifera indica(Mango)

2017 ◽  
Vol 2017 ◽  
pp. 1-24 ◽  
Author(s):  
Meran Keshawa Ediriweera ◽  
Kamani Hemamala Tennekoon ◽  
Sameera Ranganath Samarakoon
Keyword(s):  
Amino Acids ◽  
Bioactive Compounds ◽  
Mangifera Indica ◽  
Fruit Peel ◽  
Pharmacological Activities ◽  
Phytochemical Constituents ◽  
Pharmacological Potential ◽  
Diverse Plant ◽  
Different Parts ◽  
Comprehensive Study

Mangifera indica(family Anacardiaceae), commonly known as mango, is a pharmacologically, ethnomedically, and phytochemically diverse plant. Various parts ofM. indicatree have been used in traditional medicine for the treatment of different ailments, and a number of bioactive phytochemical constituents ofM. indicahave been reported, namely, polyphenols, terpenes, sterols, carotenoids, vitamins, and amino acids, and so forth. Several studies have proven the pharmacological potential of different parts of mango trees such as leaves, bark, fruit peel and flesh, roots, and flowers as anticancer, anti-inflammatory, antidiabetic, antioxidant, antibacterial, antifungal, anthelmintic, gastroprotective, hepatoprotective, immunomodulatory, antiplasmodial, and antihyperlipemic. In the present review, a comprehensive study on ethnopharmacological applications, pharmacological activities, and bioactive compounds ofM. indicahas been described.

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