scholarly journals Synthesis, Characterization, Swiss ADME and Antimicrobial Activity of Copper (II) Complex with 2-Sulfanilamidopyrimidine: Through DFT Spectroscopic with Profound Biological Implications

Author(s):  
Mohd. Washid Khan ◽  
Ravi Prakash Mishra ◽  
Bhavesh Patel ◽  
Shradha Patel ◽  
Sujit Gupta ◽  
...  

Sulphadiazine and their copper metal complexes are dexterous ligands, which are condensation products of primary amines with carbonyl compounds gaining importance day by day in the present scenario. Spectral characterization and examination of the potential antimicrobial and antioxidant activity of the synthesized complex were performed. The imine Cu(II) complex is characterized by FTIR and UV/Vis spectroscopy. The Stoichiometric M:L ratio was determined by Joe and Jones method. These compounds and their copper metal complex are very important in various biological systems and their medicinal and pharmaceutical fields. Schiff foundations show beneficial natural functions such as anti-inflammatory, analgesic, antimicrobial, anticonvulsant, antitubercular, anticancer, antioxidant, anthelmintic, and antiglycation. The present review summarizes information on the diverse biological activities and also highlights the recently synthesized numerous Schiff bases and their metal complex  as potential bioactive core.

2013 ◽  
Vol 2013 ◽  
pp. 1-14 ◽  
Author(s):  
Anu Kajal ◽  
Suman Bala ◽  
Sunil Kamboj ◽  
Neha Sharma ◽  
Vipin Saini

Schiff bases are condensation products of primary amines with carbonyl compounds gaining importance day by day in present scenario. Schiff bases are the compounds carrying imine or azomethine (–C=N–) functional group and are found to be a versatile pharmacophore for design and development of various bioactive lead compounds. Schiff bases exhibit useful biological activities such anti-inflammatory, analgesic, antimicrobial, anticonvulsant, antitubercular, anticancer, antioxidant, anthelmintic, antiglycation, and antidepressant activities. Schiff bases are also used as catalysts, pigments and dyes, intermediates in organic synthesis, polymer stabilizers, and corrosion inhibitors. The present review summarizes information on the diverse biological activities and also highlights the recently synthesized numerous Schiff bases as potential bioactive core.


2021 ◽  
Vol 18 (4) ◽  
pp. 352-361
Author(s):  
Achut R. Shinde ◽  
Dyanoba B. Muley

Background: Plethora of literature reported hitherto, depicts impending biological activities for spirochromones. This fact encouraged us for the exploration of the synthesis of new substituted spirochromones and their evaluation of their bioactivities. Objective: To synthesize different substituted spirochromones derivatives from a spirochromones salt using (R)-pyroglutamic acid as catalyst and their evaluation for antimicrobial and antioxidant activities. Methods: Herein, Aldol cascade method was used for the syntheses of spirochromone derivatives from its salt. A mild protocol is developed for the syntheses of spirochromones derivatives by using (R)-pyroglutamic acid as catalyst. Further, the derivatives and its precursor salt were screened for antimicrobial and antioxidant activity. The antioxidant potentials of the synthesized compounds were checked by DPPH and hydroxyl free radical scavenging assay. Consequently, in vitro antimicrobial activities were performed by well diffusion assay against gram negative bacterium (E. coli) and gram positive bacterium (S. aureus). Results: In the present work, 10 synthesized derivatives are obtained in harmonious yield from a precursor spirochromones salt using (R)-pyroglutamic acid as catalyst. Amongst the studied compounds, 6a depicted maximum antimicrobial activity against the screened microorganisms along with maximum antioxidant activity. Albeit, the synthesized motifs showed moderate to good antioxidant and antimicrobial activities. Conclusion: A mild protocol was developed for the synthesis of spirochromone derivatives from their precursor spirochromones salt by using (R)-pyroglutamic acid as catalyst, which showed moderate to good antimicrobial and antioxidant activity.


2020 ◽  
Vol 16 ◽  
Author(s):  
Mojgan Alizadeh ◽  
Akram Arianfar ◽  
Ameneh Mohammadi

Objective: Ziziphora clinopodioides is an edible medicinal plant belongs to the Labiatae family that widespread all over Iran. It used as culinary and also in cold and cough treatments in Iran. The aim of present work was to evaluate the effect of different timeframes during the hydrodistillation on essential oil composition, antimicrobial and antioxidant activity. Materials and Methods: The essential oil of Z. clinopodiodes was extracted via hydrodistillation with Clevenger apparatus. The fractions of essential oil were captured at 6 times from the beginning of the distillation: (10, 20, 60, 120, 180 and 240 min). The fractions of essential oil were analyzed by GC/MS and their antibacterial, antifungal and antioxidant activities were studied by Disk - well diffusion and DPPH methods respectively. Results: Six distillation times and whole essential oil were captured during the hydrodistillation. Essential oil yield dropped off significantly during distillation progressed (1.0% for 10 min and 0.025 for 240 min). 1,8 Cineol, Isomenthone, Pulegone, Piperitenone and Citronellic acid were major compounds in fractions and they were affected by distillation times. Pulegone was major compound in all of essential oils. In antioxidant activity assay, whole essential oil was stronger than was stronger than positive control and fractions of essential oil, because of higher levels of Isomenthone, Piperitenone and Citronellic acid. Strongest antimicrobial activity against S. aureus, E. coli and C. albicans was observed from 10 min fraction. Conclusion: Our results indicated that distillation time can create essential oils with specific properties and we can achieve to more efficient essential oil in short times.


Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3170
Author(s):  
Wafaa M. Elkady ◽  
Mariam H. Gonaid ◽  
Miriam F. Yousif ◽  
Mahmoud El-Sayed ◽  
Hind A. N. Omar

Active components from natural sources are the current focus in most pharmacological research to provide new therapeutic agents for clinical use. Essential oils from the Pinus species have been traditionally used in medicine. This study aimed to investigate the chemical profile of two Pinus species, Pinus halepensis L. and Pinus pinea Mill, from different altitudes in Libya and study the effect of environmental conditions on the biological activities of essential oils. A clevenger apparatus was used to prepare the essential oils by hydrodistillation. Analyses were done using GC/MS. Anthelmintic and antimicrobial activities were tested against the earthworm Allolobophora caliginosa, gram-positive bacteria, gram-negative bacteria, and fungi. Different chemical profiles were observed among all tested essential oils, and terpenes were the most dominant class. All studied essential oils from the Pinus species exhibited a remarkable anthelmintic activity compared to the standard piperazine citrate drug. Pinus halepensis from both altitudes showed broad-spectrum antimicrobial activity against all tested microorganisms, while Pinus pinea was effective against only Escherichia coli. From these findings, one can conclude that there are variations between studied species. The essential oil compositions are affected by environmental factors, which consequently affect the anthelmintic and antimicrobial activity.


2019 ◽  
Vol 377 (6) ◽  
Author(s):  
Samson Afewerki ◽  
Armando Córdova

AbstractThe concept of merging enamine activation catalysis with transition metal catalysis is an important strategy, which allows for selective chemical transformations not accessible without this combination. The amine catalyst activates the carbonyl compounds through the formation of a reactive nucleophilic enamine intermediate and, in parallel, the transition metal activates a wide range of functionalities such as allylic substrates through the formation of reactive electrophilic π-allyl-metal complex. Since the first report of this strategy in 2006, considerable effort has been devoted to the successful advancement of this technology. In this chapter, these findings are highlighted and discussed.


AMB Express ◽  
2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Hend M. Tag ◽  
Amna A. Saddiq ◽  
Monagi Alkinani ◽  
Nashwa Hagagy

AbstractHaloferax sp strain NRS1 (MT967913) was isolated from a solar saltern on the southern coast of the Red Sea, Jeddah, Saudi Arabia. The present study was designed for estimate the potential capacity of the Haloferax sp strain NRS1 to synthesize (silver nanoparticles) AgNPs. Biological activities such as thrombolysis and cytotoxicity of biosynthesized AgNPs were evaluated. The characterization of silver nanoparticles biosynthesized by Haloferax sp (Hfx-AgNPs) was analyzed using UV–vis spectroscopy, transmission electron microscopy (TEM), X-ray diffraction (XRD), and Fourier-transform infrared spectroscopy (FTIR). The dark brown color of the Hfx-AgNPs colloidal showed maximum absorbance at 458 nm. TEM image analysis revealed that the shape of the Hfx-AgNPs was spherical and a size range was 5.77- 73.14 nm. The XRD spectra showed a crystallographic plane of silver nanoparticles, with a crystalline size of 29.28 nm. The prominent FTIR peaks obtained at 3281, 1644 and 1250 cm− 1 identified the Functional groups involved in the reduction of silver ion reduction to AgNPs. Zeta potential results revealed a negative surface charge and stability of Hfx-AgNPs. Colloidal solution of Hfx-AgNPs with concentrations ranging from 3.125 to 100 μg/mL was used to determine its hemolytic activity. Less than 12.5 μg/mL of tested agent showed no hemolysis with high significant decrease compared with positive control, which confirms that Hfx-AgNPs are considered non-hemolytic (non-toxic) agents according to the ISO/TR 7405-1984(f) protocol. Thrombolysis activity of Hfx-AgNPs was observed in a concentration-dependent manner. Further, Hfx-AgNPs may be considered a promising lead compound for the pharmacological industry.


2021 ◽  
Vol 10 (1) ◽  
pp. 882-892
Author(s):  
Sami Bawazeer ◽  
Abdur Rauf ◽  
Taufiq Nawaz ◽  
Anees Ahmed Khalil ◽  
Muhammad Sameem Javed ◽  
...  

Abstract Requirements for developing new methodologies to biosynthesize nanoparticles are increasing day by day. The typical chemical synthesis of nanoparticles has raised concerns regarding environmental safety and adverse impact on human health. Therefore, there is an urgent need to develop green synthesized nanoparticles that are considered to be safe, ecofriendly, and cost-effective as compared to chemical approaches. Hence, in this study, we synthesized and characterized pomegranate peel extract-based gold nanoparticles (PP-AuNPs) through UV-visible spectroscopy, FT-IR, and AFM microscopy. Furthermore, the biological activities like analgesic, muscle relaxant, and sedative properties of synthesized PP-AuNPs were also determined. The change of color to dark ruby indicates the formation of AuNPs. The surface plasma resonance (SPR) peak in the absorption spectra was shown at 525 nm by using (UV-Vis) spectroscopy. A single distinctive peak implied the shape of nanoparticles to be spherical. AFM images revealed that the biosynthesized nanoparticles were spherical in shape. Furthermore, the images confirm the uniform distribution of PP-AuNPs with particle sizes ranging from 4 to 16 nm. Different classes of phytochemicals were preliminarily identified in extracts. The analgesic effect of extracts (70.04%) and PP-AuNPs (81.98%) demonstrated a significant (p < 0.001) percent reduction in writhing at a dose of 100 and 15 mg·kg−1, respectively. A mild muscle relaxant effect was noted against both the tested samples while a significant sedative effect was observed for both samples; however, PP-AuNPs weres more sedative compared to the extract. Pomegranate peel extracts and synthesized PP-AuNPs were found to possess significant analgesic, muscle relaxant, and sedative properties.


2021 ◽  
Vol 2 (2) ◽  
Author(s):  
Eti Nurwening Sholikhah ◽  
Maulina Diah ◽  
Mustofa ◽  
Masriani ◽  
Susi Iravati ◽  
...  

Pycnarrhena cauliflora (Miers.) Diels., local name sengkubak, is one of indigenous plants from West Kalimantan that has been used as natural flavor. Pycnorrhena cauliflora is one of species of Menispermaceae family which is rich in bisbenzylisoquinoline alkaloids. This alkaloids are known to have various biological activities including antiprotozoal, antiplasmodial, antifungal and antibacterial activities. This study aimed to investigate antimicrobial activity of  the P. cauliflora (Miers.) Diels. methanolic extracts against gram-positive and gram-negative bacteria. The methanolic extract of P. cauliflora (Miers.) Diels., root, leaf and stem were prepared by maceration. The disk-diffusion method was then used to determine the antimicrobial activity of the extracts against Streptococcus pyogenes, S. mutants, Staphylococcus aureus, S. epidermidis, Salmonella typhi, Shigella flexneri, Pseudomonas aeruginosa and Escherichia coli after 18-24 h incubation at 37 oC. Amoxicillin was used as positive control for gram-positive bacteria and ciprofloxacin was used as gram-negative bacteria. The inhibition zones were then measured in mm. Analysis were conducted in duplicates. The results showed in general the methanolic extracts of P. cauliflora (Miers.) Diels. root (inhibition zone diameter= 10-23 mm) were more active than that leaf (0-15 mm) and stem (0-17 mm) extracts against gram-positive bacteria. The zone inhibition diameter of amoxicillin as positive control was 8-42 mm. In addition, the methanolic extracts of P. cauliflora (Miers.) Diels. root (12-17 mm) were also more active than that leaf (0-12 mm) and stem (0-12 mm) extracts against gram-negative bacteria. The zone inhibition diameter of ciprofloxacin as positive control was 33-36 mm. In conclusion, the methanolic extract of P. caulifloria (Miers.) Diels. root is the most extract active against both gram-positive and gram-negative bacteria. Further study will be focused to isolate active compounds in the methanolic extract of the root.


2017 ◽  
Vol 37 (4) ◽  
pp. 368-378 ◽  
Author(s):  
Jusciêne B. Moura ◽  
Agueda C. de Vargas ◽  
Gisele V. Gouveia ◽  
João J. de S. Gouveia ◽  
Juracy C. Ramos-Júnior ◽  
...  

ABSTRACT: Cladonia substellata Vainio is a lichen found in different regions of the world, including the Northeast of Brazil. It contains several secondary metabolites with biological activity, including usnic acid, which has exhibited a wide range of biological activities. The aim of this study was to evaluate the in vitro antimicrobial activity of the organic extract of C. substellata and purified usnic acid. Initially, Staphylococcus spp., derived from samples of skin and ears of dogs and cats with suspected pyoderma and otitis, were isolated and analyzed. In antimicrobial susceptibility testing against Staphylococcus spp., 77% (105/136) of the isolates were resistant to the antimicrobials tested. In the assessment of biofilm production, 83% (113/136) were classified as producing biofilm. In genetic characterization, 32% (44/136) were positive for blaZ, no isolate (0/136) was positive for the mecA gene, and 2% (3/136) were positive for the icaD gene. The in vitro antimicrobial activity of the organic extract of C. substellata and purified usnic acid against Staphylococcus spp. ranged from 0.25mg/mL to 0.0019mg/mL, inhibiting bacterial growth at low concentrations. The substances were more effective against biofilm-producing bacteria (0.65mg/mL-0.42mg/mL) when compared to non-biofilm producing bacteria (2.52mg/mL-2.71mg/mL). Usnic acid and the organic extract of C. substellata can be effective in the treatment of pyoderma and otitis in dogs and cats caused by Staphylococcus spp.


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