Phosphorus–nitrogen compounds. Part 37. Syntheses and structural characterizations, biological activities of mono and bis(4-fluorobenzyl)spirocyclotetraphosphazenes

2017 ◽  
Vol 41 (13) ◽  
pp. 5818-5835 ◽  
Author(s):  
Gamze Elmas ◽  
Aytuğ Okumuş ◽  
Pelin Sevinç ◽  
Zeynel Kılıç ◽  
Leyla Açık ◽  
...  
Keyword(s):  
Biological Activities ◽  
Antimicrobial Activities ◽  
Nitrogen Compounds ◽  
Structural Characterizations

The syntheses, spectroscopic and crystallographic properties, in vitro cytotoxic and antimicrobial activities of the cyclotetraphosphazenes were investigated.

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone clubbed with 1,2,3-Triazoles

2020 ◽  
Vol 16 ◽  
Author(s):  
Adinath D. Badar ◽  
Shubham M. Sulakhe ◽  
Mahesh B. Muluk ◽  
Naziya N. M. A. Rehman ◽  
Prashant P. Dixit ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Biological Activities ◽  
Dna Gyrase ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Molecular Docking Study ◽  
Triazole Derivatives ◽  
Antibacterial And Antifungal

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities. Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives. Results: The compounds 5d, 5h, 5i and 5k have exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives have shown excellent binding affinity towards DNA gyrase. Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have been shown excellent binding affinity towards DNA gyrase.

scholarly journals Phytochemical Characterization and Evaluation of Biological Activities of Egyptian Carob Pods (Ceratonia siliqua L.) Aqueous Extract: In Vitro Study

Plants ◽  
2021 ◽  
Vol 10 (12) ◽  
pp. 2626
Author(s):  
Wael Sobhy Darwish ◽  
Abada El Sayed Khadr ◽  
Maher Abd El Naby Kamel ◽  
Mabrouk A. Abd Eldaim ◽  
Ibrahim El Tantawy El Sayed ◽  
...  
Keyword(s):  
Aqueous Extract ◽  
Biological Activities ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
Biologically Active ◽  
Phytochemical Analysis ◽  
Type I ◽  
Hypotonic Solution ◽  
Ceratonia Siliqua

Ceratonia siliqua (Carob) is an evergreen Mediterranean tree, and carob pods are potentially nutritive and have medicinal value. The present study was carried out to estimate the possible biological activities of phytochemical-characterized carob pod aqueous extract (CPAE). The phytochemical contents of CPAE were determined by using colorimetric methods and HPLC. In addition, the free radical scavenging properties and anti-diabetic, anti-hemolytic, and antimicrobial activities were estimated by using standardized in vitro protocols. The phytochemical analysis revealed that CPAE was rich in polyphenols, flavonoids, and alkaloids, where it contained a significant amount of gallic acid, catechin, and protocatechuic acid. Furthermore, CPAE exhibited strong antioxidant activity where it prevented the formation of 2, 2-Diphenyl-1-picryl hydrazyl, hydroxyl, and nitric oxide free radicals. Additionally, it had a potent inhibitory effect against digestive enzymes (amylase, maltase, sucrase, and lactase). Moreover, CPAE exhibited anti-Staph aureus, anti-Escherichia coli, anti-Candida albicans, and anti-herpes simplex type I virus (HSV-I). Finally, CPAE protected the erythrocyte membrane from hypotonic solution-induced hemolysis. Altogether, CPAE could be regarded as an interesting source of biologically active antioxidant, anti-diabetic, and antimicrobial preparation for a potential application in pharmaceutical and food supplement fields.

scholarly journals Secondary Metabolites from Gorgonian Corals of the Genus Eunicella: Structural Characterizations, Biological Activities, and Synthetic Approaches

Molecules ◽  
2019 ◽  
Vol 25 (1) ◽  
pp. 129
Author(s):  
Dario Matulja ◽  
Maria Kolympadi Markovic ◽  
Gabriela Ambrožić ◽  
Sylvain Laclef ◽  
Sandra Kraljević Pavelić ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Biological Activities ◽  
Structural Characteristics ◽  
Antimicrobial Activities ◽  
Chemical Structures ◽  
Gorgonian Corals ◽  
Synthetic Approaches ◽  
Further Development

Gorgonian corals, which belong to the genus Eunicella, are known as natural sources of diverse compounds with unique structural characteristics and interesting bioactivities both in vitro and in vivo. This review is focused primarily on the secondary metabolites isolated from various Eunicella species. The chemical structures of 64 compounds were divided into three main groups and comprehensively presented: a) terpenoids, b) sterols, and c) alkaloids and nucleosides. The observed biological activities of depicted metabolites with an impact on cytotoxic, anti-inflammatory, and antimicrobial activities were reviewed. The most promising biological activities of certain metabolites point to potential candidates for further development in pharmaceutical, cosmetic, and other industries, and are highlighted. Total synthesis or the synthetic approaches towards the desired skeletons or natural products are also summarized.

scholarly journals DESIGN AND SYNTHESIS OF NOVEL 1-((DIMETHYLAMINO)METHYL)-3-(4-(3-(SUBSTITUTE DPHENYL)-4-OXOTHIAZOLIDIN-2-YL)PHENYLIMINO)-5-NITROINDOLIN-2-ONES AS POTENT ANTITUBERCULAR AGENTS

2019 ◽  
pp. 200-207
Author(s):  
KOSARAJU LAHARI ◽  
RAJA SUNDARARAJAN
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
Proton Nuclear Magnetic Resonance ◽  
Design And Synthesis ◽  
Group Variation

Objective: Isatins have emerged as antimicrobial agents due to their broad spectrum of in vitro and in vivo antimicrobial activities. In addition, thiazolidinone also reported to possess various biological activities particularly antimicrobial activity. Due to the importance, we planned to synthesize compounds with isatin functionality coupled with thiazolidinone as possible antitubercular and antimicrobial agents which could furnish better therapeutic results. Methods: In vitro Mycobacterium tuberculosis method and agar streak dilution test are used to estimate antitubercular and antimicrobial potency of title analogs, respectively. Minimum inhibitory concentration of entire title compounds was determined against all tested microorganism such as M. tuberculosis, four Gram-positive, three Gram-negative bacteria, and two fungi. Results: A series of new thiazolidinone substituted Schiff and Mannich bases of 5-nitroisatins were designed and synthesized by a multistep synthesis from isatin. Structures of synthesized compounds are characterized using Fourier-transform infrared, proton nuclear magnetic resonance, mass spectroscopy, and bases of elemental analysis. Mild to good antitubercular and antimicrobial activity was showed by synthesized 5-nitroisatin analogs. The relationship between the biological activity and the functional group variation of the tested compounds was discussed. Conclusion: 3-(4-(3-(4-Aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethyl amino)methyl)-5-nitroindolin-2-one 6 and 3-(4-(3- (2-aminophenyl)-4-oxothiazolidin-2-yl)phenylimino)-1-((dimethylamino)methyl)-5-nitroindolin-2-one 13 were found to be the most potent compounds of this series which might be extended as a novel class of antimicrobial agents.

scholarly journals Chemical Composition and Biological Activities of the Essential Oil from Artemisia herba-alba Growing Wild in Tunisia

2013 ◽  
Vol 8 (3) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Ismail Amri ◽  
Laura De Martino ◽  
Aurelio Marandino ◽  
Hamrouni Lamia ◽  
Hanana Mohsen ◽  
...  
Keyword(s):  
Chemical Composition ◽  
Essential Oil ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Lepidium Sativum ◽  
Mediterranean Ecosystem ◽  
Bacterial Strains ◽  
Phytotoxic Activity ◽  
Main Components

Aromatic plants can interfere in the Mediterranean ecosystem, mainly by the introduction in the environment of volatile compounds. For this reason, we studied the chemical composition and the possible phytotoxic and antimicrobial activities of the essential oil extracted from leaves of Tunisian Artemisia herba-alba Asso. The chemical composition of the essential oil, obtained by hydrodistillation, was analyzed by GC and GC-MS. In all, 24 compounds were identified. The main components were camphor (39.1.%), chrysanthenone (15.0%) and cis-thujone (7.8%). The essential oil was evaluated for its in vitro phytotoxic activity against germination and initial radical growth of Raphanus sativus L., Lepidium sativum L., Sinapis arvensis L., Triticum durum L. and Phalaris canariensis L. seeds. The radicle elongation of the five seeds was affected to different extents by the oil, while germination was not affected. The oil, when tested against eight selected bacterial strains, showed low antimicrobial activity. The chemical composition of the oil of A. herba-alba can help in the chemosystematics of this complex genus. However, the recorded biological activities seem to be neither ecologically nor medicinally significant.

Phytochemical and Biological Activities of five Turanecio Hamzaoglu (Asteraceae) Species from Turkey

2017 ◽  
Vol 13 (1) ◽  
pp. 49-55
Author(s):  
Sevil Albayrak ◽  
Ahmet Aksoy ◽  
Abit Yasar ◽  
Lutfiye Yurtseven ◽  
Umit Budak
Keyword(s):  
Therapeutic Potential ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Natural Antioxidants ◽  
Antibacterial Activities ◽  
Antimicrobial Activities ◽  
In Vitro Assays ◽  
Methanolic Extracts ◽  
Promising Source

Objectives: In vitro biological activities of methanolic extracts of five Turanecio species have been studied. Materials and Methods: The phenolic compositions of the extracts were evaluated by the Folin- Ciocalteu assay and by HPLC analysis. Antioxidant activities were determined with two in vitro assays namely, DPPH (2,2-diphenyl-1-picrylhydrazyl) scavenging assay and phosphomolybdenum assay. The antimicrobial activities of the extracts were evaluated against 13 microorganisms. Results: T. hypochionaeus var. hypochionaeus was showed the highest DPPH inhibition with 88.84% at 100 μg·mL-1. All of the extracts were exerted high total antioxidant activities 128.00- 243.13 mg AAE g-1) and seem to be a promising source of natural antioxidants. The phenolic contents in the extracts varied from 26.17 to 60.99 mg·g-1 as gallic acid equivalent. Chlorogenic acid, caffeic acid and p- coumaric acid were the predominant constituents. The methanolic extracts revealed promising antibacterial activities against most bacteria. No activity was recorded against yeasts tested. Conclusion: The polyphenolic constituents appear to be responsible, at least in part, for the extract’s activities. The present study confirms that tested Turanecio species contains significant source of phenolics have antioxidant and antimicrobial activities and may have therapeutic potential.

scholarly journals Synthesis and Antimicrobial Activities of N-(Heteroaryl-substituted)-p-toluenesulphonamides

2014 ◽  
Vol 2014 ◽  
pp. 1-5
Author(s):  
Ozoh Chinwe Francisca ◽  
Okoro Uchechukwu Chris ◽  
Ugwu David Izuchukwu
Keyword(s):  
Biological Activities ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Gram Positive Bacteria ◽  
New Class ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
C Nmr

A new class of N-(heteroaryl-substituted)-p-toluenesulphonamides has been synthesized exhibiting antibacterial and antifungal properties. The condensation reaction of p-toluenesulphonyl chloride 1 with appropriate substituted amino pyridines 2a–g in acetone furnished N-(heteroaryl-substituted)-p-toluenesulphonamides 3a–g. These derivatives were characterized by IR, 1H-, and 13C-NMR spectroscopy and were screened in vitro against gram-positive bacteria, gram-negative bacteria, and fungi organisms using agar-diffusion method. Results indicated improved biological activities over reference drugs such as Tetracycline (TCN) and Fluconazole (FLU).

scholarly journals Antimicrobial, Antimalarial and Cytoxicity Activities of Constituents of a Bhutanese Variety of Ajania nubigena

2013 ◽  
Vol 8 (6) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Phurpa Wangchuk ◽  
Paul A. Keller ◽  
Stephen G. Pyne ◽  
John Korth ◽  
Samten ◽  
...  
Keyword(s):  
Biological Activities ◽  
Multidrug Resistant ◽  
Antimicrobial Activities ◽  
Major Constituent ◽  
Meoh Extract ◽  
Linalool Oxide ◽  
Pure Compounds ◽  
Cytotoxicity Activities ◽  
Multidrug Resistant Strain

An investigation of the essential oil (EO) and the crude MeOH extract of a Bhutanese variety of Ajania nubigena using GC/GC-MS and NMR found the following: a) one kg of the dried plant material contained 0.7% w/w EO; b) 44 of the 53 GC-FID peaks of the EO were identified with (3 R,6 R)-linalool oxide acetate (75.8 %) as the major constituent (chemotype II) and chamazulene as a new sub-chemotype; c) purification of the EO furnished ( 3R, 6R)-linalool oxide acetate (1), chamazulene (2), ( E)-2-(2,4-hexadiynylidene)-1,6-dioxaspiro[4,4]non-3-ene (3), and ( Z)-2-(2,4-hexadinylidene)-1,6-dioxaspiro[4,4]non-3-ene (4); d) from the crude MeOH extract, four flavonoid compounds: 1-(4-hydroxyphenyl)propan-1-one (5), oxyanin B (6), luteolin (7) (major) and the luteolin-7- O-β-D-glucoside (8) were isolated; e) among the EO and pure compounds tested for biological activities, compound 7 exhibited a broad range of moderate antiplasmodial, cytoxicity and antimicrobial activities; c) compound 8 showed significant in vitro antiplasmodial activity against P. falciparum strains TM4/8.2 and K1CB1 (multidrug resistant strain) and was identified as a potential antimalarial scaffold; and f) the in vitro antimicrobial and cytotoxicity activities were in alignment with the traditional medical uses of this plant and thus substantiate its use in Bhutanese traditional medicine.

Major biological activities and protein profiles of skin secretions of Lissotriton vulgaris and Triturus ivanbureschi

2018 ◽  
Vol 43 (6) ◽  
pp. 605-612 ◽  
Author(s):  
Mert Karış ◽  
Doğancan Şener ◽  
Hüsniye Tansel Yalçın ◽  
Ayşe Nalbantsoy ◽  
Bayram Göçmen
Keyword(s):  
Total Protein ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Protein Profiles ◽  
Skin Secretion ◽  
Active Components ◽  
Lissotriton Vulgaris ◽  
Hemolytic Effect ◽  
Skin Secretions

Abstract Objective The aim of this study was to determine the total protein amounts, protein profiles, in vitro cytotoxicities, antimicrobial activities and hemolytic effects of skin secretions of the Lissotriton vulgaris and Triturus ivanbureschi. Methods Skin secretions were obtained, clarified, supernatants snap-frozen then lyophilized. Total protein amounts were determined by BCA assay kit. Protein profiles were revealed by the SDS-PAGE. The cytotoxicity and antimicrobial activity were determined by using MTT assay and minimum inhibitory concentration (MIC) method. Hemolytic effects were measured on rabbit red blood cells. Results Lissotriton vulgaris and T. ivanbureschi skin secretions have totally 18 and 20 protein fractions. IC50 values were detected between 1.40 and 40.28 μg/mL. The MIC results were found between 7.8 and 250 μg/mL. Lissotriton vulgaris skin secretion showed low hemolytic effect while T. ivanbureschi skin secretion showed high hemolytic effect. Conclusion This study is the first report showing the potential of L. vulgaris and T. ivanbureschi skin secretions for cytotoxicity, antimicrobial and hemolytic activity as an alternative therapeutic approach for traditional uses. Further studies need to focus on purification of the active components from these skin secretions and mode of action on cancer cell lines and microorganisms as anti-agents.

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