Synthesis of 1,3,4-Oxadiazole derivatives with its Antifungal Activity Evaluation

Author(s):  
Anuja Patil ◽  
Mohite Shriniwas

Azole exhibits wide range of pharmacological properties. there is limited number of drugs are available to treat microbial infection that too have serious toxic effects the existing drugs has been suffering from the development of resistance and thus newer drugs are required with better activity profile. In this paper synthesis of 1,3,4- oxadiazole derivative with precursor salicylic acid and perform an antifungal activity.

2021 ◽  
Vol 10 (1) ◽  
Author(s):  
Luce Mattio ◽  
Giorgia Catinella ◽  
Marcello Iriti ◽  
Lisa Vallone

Stilbenoids (resveratrol and its derivatives) are secondary metabolites produced by plants as defence mechanism to microbial infection. These compounds are known for their anti-inflammatory action and health benefits in preventing a wide range of disorders (e.g. cancer and cardiovascular diseases). However, their antimicrobial properties are less investigated. A series of 8 stilbenoid compounds were synthesized and their antifungal activity against 19 wild strains of filamentous fungi and yeasts (isolated from the environment and food) was tested in vitro. Using an agar diffusion assay, compounds were tested at the concentration of 100 μg/ml on filamentous fungi and yeasts at 104 CFU/ml. The results showed that tested derivatives possess moderate antifungal activity: in particular, monomeric stilbenoids 3’-hydroxy-pterostilbene and piceatannol, and dimeric stilbenoids (±)-trans-δ-viniferin and pallidol were active against mycotoxigenic fungi.


2020 ◽  
Vol 17 (7) ◽  
pp. 780-794
Author(s):  
Nurhayatun S. Abdul Razak ◽  
Joazaizulfazli Jamalis ◽  
Subhash Chander ◽  
Roswanira Abdul Wahab ◽  
Deepak P. Bhagwat ◽  
...  

Coumarin and oxadiazole moieties ubiquitously occur in a wide range of natural products and are valued for their varied and beneficial pharmacological activities. Herein, this review focuses on various documented techniques used by researchers to synthesize an assortment of biologically active coumarin-oxadiazole scaffolds. Also, the common techniques discussed are used to establish the wide-range of biological activities of the synthesized coumarin and oxadiozole derivatives, including; antioxidant, anthelmintic, antimicrobial, anti-tuberculosis, analgesic, anti-inflammatory, cytotoxicity and anticonvulsant. Additionally, the current, well-established drugs synthesized using coumarin-oxadiazole scaffolds are typically dispensed in regular clinical practice are also highlighted in this review paper.


2019 ◽  
Author(s):  
Chem Int

Coumarin and its derivatives are widely spread in nature. Coumarin goes to agroup as benzopyrones, which consists of a benzene ring connected to a pyronemoiety. Coumarins displayed a broad range of pharmacologically useful profile.Coumarins are considered as a promising group of bioactive compounds thatexhibited a wide range of biological activities like anti-microbial, anti-viral,antiparasitic, anti-helmintic, analgesic, anti-inflammatory, anti-diabetic, anticancer,anti-oxidant, anti-proliferative, anti-convulsant, and antihypertensiveactivities etc. The coumarin compounds have immense interest due to theirdiverse pharmacological properties. In particular, these biological activities makecoumarin compounds more attractive and testing as novel therapeuticcompounds.


2020 ◽  
Vol 24 (5) ◽  
pp. 473-486 ◽  
Author(s):  
Ligia S. da Silveira Pinto ◽  
Thatyana R. Alves Vasconcelos ◽  
Claudia Regina B. Gomes ◽  
Marcus Vinícius N. de Souza

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.


2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Luca Barbieri ◽  
Ioritz Sorzabal Bellido ◽  
Alison J. Beckett ◽  
Ian A. Prior ◽  
Jo Fothergill ◽  
...  

AbstractIn this work, we introduce a one-step strategy that is suitable for continuous flow manufacturing of antimicrobial PDMS materials. The process is based on the intrinsic capacity of PDMS to react to certain organic solvents, which enables the incorporation of antimicrobial actives such as salicylic acid (SA), which has been approved for use in humans within pharmaceutical products. By combining different spectroscopic and imaging techniques, we show that the surface properties of PDMS remain unaffected while high doses of the SA are loaded inside the PDMS matrix. The SA can be subsequently released under physiological conditions, delivering a strong antibacterial activity. Furthermore, encapsulation of SA inside the PDMS matrix ensured a diffusion-controlled release that was tracked by spatially resolved Raman spectroscopy, Attenuated Total Reflectance IR (ATR-IR), and UV-Vis spectroscopy. The biological activity of the new material was evaluated directly at the surface and in the planktonic state against model pathogenic bacteria, combining confocal laser scanning microscopy, electron microscopy, and cell viability assays. The results showed complete planktonic inhibition for clinically relevant strains of Staphylococcus aureus and Escherichia coli, and a reduction of up to 4 orders of magnitude for viable sessile cells, demonstrating the efficacy of these surfaces in preventing the initial stages of biofilm formation. Our approach adds a new option to existing strategies for the antimicrobial functionalisation of a wide range of products such as catheters, wound dressings and in-dwelling medical devices based on PDMS.


2021 ◽  
Vol 9 (4) ◽  
pp. 839
Author(s):  
Muhammad Rafiullah Khan ◽  
Vanee Chonhenchob ◽  
Chongxing Huang ◽  
Panitee Suwanamornlert

Microorganisms causing anthracnose diseases have a medium to a high level of resistance to the existing fungicides. This study aimed to investigate neem plant extract (propyl disulfide, PD) as an alternative to the current fungicides against mango’s anthracnose. Microorganisms were isolated from decayed mango and identified as Colletotrichum gloeosporioides and Colletotrichum acutatum. Next, a pathogenicity test was conducted and after fulfilling Koch’s postulates, fungi were reisolated from these symptomatic fruits and we thus obtained pure cultures. Then, different concentrations of PD were used against these fungi in vapor and agar diffusion assays. Ethanol and distilled water were served as control treatments. PD significantly (p ≤ 0.05) inhibited more of the mycelial growth of these fungi than both controls. The antifungal activity of PD increased with increasing concentrations. The vapor diffusion assay was more effective in inhibiting the mycelial growth of these fungi than the agar diffusion assay. A good fit (R2, 0.950) of the experimental data in the Gompertz growth model and a significant difference in the model parameters, i.e., lag phase (λ), stationary phase (A) and mycelial growth rate, further showed the antifungal efficacy of PD. Therefore, PD could be the best antimicrobial compound against a wide range of microorganisms.


AMB Express ◽  
2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Razmik Sargsyan ◽  
Arsen Gasparyan ◽  
Gohar Tadevosyan ◽  
Hovik Panosyan

AbstractDue to wide range of secondary metabolites, lichens were used from antiquity as sources of colorants, perfumes and medicaments. This research focuses on exploring the antioxidant, antimicrobial and cytotoxic activities of methanol, ethanol, acetone extracts and aqueous infusions of corticolous lichens sampled from Armenia. Methanol, ethanol and acetone extracts from all tested lichens were active against Gram-positive bacterial strains. The most effective solvent to retrieve antimicrobial compounds was methanol. Aqueous infusions of tested lichens didn’t show any significant antibacterial and antifungal activity. The highest antimicrobial activity was observed for methanol extract of Ramalina sinensis. The minimum inhibitory concentration of methanol extract of Ramalina sinensis were 0.9–1.8 mg mL− 1. Pseudevernia furfuracea demonstrated antifungal activity (Ø 12 mm). Methanol extract of Parmelia sulcata demonstrated largest 1,1-diphenyl-2-picryl-hydrazil (DPPH) radical scavenging activity (71 %). The cytotoxicity was measured on human HeLa (cervical carcinoma) cell lines using microculture tetrazolium test assay. The IC50 values estimated for methanol extracts of Peltigera praetextata, Evernia prunastri, Ramalina sinensis and Ramalina farinacea species in HeLa cell line were within 1.8–2.8 mg mL− 1 and considered as non-cytotoxic. Obtained results suggest that studied lichens can be prospective in biotechnologies as alternative sources of antimicrobial and antioxidant substances.


Molecules ◽  
2020 ◽  
Vol 25 (5) ◽  
pp. 1059 ◽  
Author(s):  
Khadija El Hazzam ◽  
Jawhar Hafsa ◽  
Mansour Sobeh ◽  
Manal Mhada ◽  
Moha Taourirte ◽  
...  

Saponins are an important group found in Chenopodium quinoa. They represent an obstacle for the use of quinoa as food for humans and animal feeds because of their bitter taste and toxic effects, which necessitates their elimination. Several saponins elimination methods have been examined to leach the saponins from the quinoa seeds; the wet technique remains the most used at both laboratory and industrial levels. Dry methods (heat treatment, extrusion, roasting, or mechanical abrasion) and genetic methods have also been evaluated. The extraction of quinoa saponins can be carried out by several methods; conventional technologies such as maceration and Soxhlet are the most utilized methods. However, recent research has focused on technologies to improve the efficiency of extraction. At least 40 saponin structures from quinoa have been isolated in the past 30 years, the derived molecular entities essentially being phytolaccagenic, oleanolic and serjanic acids, hederagenin, 3β,23,30 trihydroxy olean-12-en-28-oic acid, 3β-hydroxy-27-oxo-olean-12en-28-oic acid, and 3β,23,30 trihydroxy olean-12-en-28-oic acid. These metabolites exhibit a wide range of biological activities, such as molluscicidal, antifungal, anti-inflammatory, hemolytic, and cytotoxic properties.


2017 ◽  
Vol 55 (1) ◽  
pp. 258-264 ◽  
Author(s):  
Salama A. Ouf ◽  
Sobhi M. Gomha ◽  
Mohamed M. Ewies ◽  
Ihab A. A. Sharawy

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