Synthesis and Biological Activity of 3-(substitutedphenyl)-6-(4-methoxyphenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine: Part II

2020 ◽  
Vol 18 ◽  
Author(s):  
Niranjan Kaushik ◽  
Nitin Kumar ◽  
Anoop Kumar ◽  
Vikas Sharma
Keyword(s):  
Antifungal Activity ◽  
Opportunistic Infections ◽  
Fungal Infections ◽  
Mass Spectral Data ◽  
Triazole Derivatives ◽  
Mass Spectral ◽  
Fungal Strains ◽  
Antifungal Properties ◽  
Antifungal Potential ◽  
Spectral Data Analysis

Background: Fungal infections are opportunistic infections that become a serious problem to human health. Objective: Considering the antifungal potential of triazole nucleus, the study was carried out with the objective to synthesize some novel triazole derivatives with antifungal potential. Method: 1,2,4-triazole derivatives were synthesized via a two step reaction (reported earlier). The first step involves reaction of substituted benzoic acid with thiocarbohydrazide to form 4-amino-3-(substituted phenyl)-5-mercapto-1, 2, 4-triazole derivatives (1a-1k) while in second step, synthesized compounds (1a-1k) were then subsequently treated with substituted acetophenone to yield substituted (4-methoxyphenyl-7H-[1, 2, 4] triazolo [3, 4-b][1,3,4] thiadiazine derivatives (2a-2k). All synthesized compounds were characterized by IR, 1H NMR, and Mass spectral data analysis and were screened for their antifungal properties against different fungal strains i.e. Candida tropicalis (ATCC-13803, ATCC-20913), Candida albicans (ATCC-60193), Candida inconspicua (ATCC-16783) and Candida glabrata (ATCC-90030, ATCC-2001). Results: Compound 2d displayed better percentage inhibition (26.29%, 24.81%) than fluconazole (24.44%, 22.96%) against ATCC-16783, ATCC-2001 fungal strains respectively at 100µg/ml. Compound 2f also displayed better percentage inhibition (28.51%) against ATCC-90030 as compared to fluconazone (27.4%) at 200 µg/ml. Similarly, compounds 2e and 2j also exhibited better antifungal properties than fluconazole at 200µg/ml. Compound 2e was found most potent against ATCC13803 (30.37%) and ATCC-90030 (30.37%) fungal strains as compared to fluconazole (28.14%, 27.4%) at 200 µg/ml respectively whereas compound 2j exhibited better antifungal activity (28.51%) against ATCC-60193 than fluconazole (27.7%) at 200 µg/ml. Conclusion: The results were in accordance with our assertions for triazole derivatives, as all compounds displayed moderate to good antifungal activity.

scholarly journals Efficient Synthesis of Novel Thiazole Substituted Pyrrolidine Derivatives and their Antimicrobial Evaluation

2020 ◽  
Vol 32 (8) ◽  
pp. 2007-2012
Author(s):  
Mahendra B. Bodake ◽  
Ghanshyam R. Jadhav ◽  
Vijay J. Medhane ◽  
Avinash D. Bholay
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Spectral Data ◽  
1H Nmr ◽  
Efficient Synthesis ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Fungal Strains ◽  
Minimum Inhibitory Concentrations ◽  
Antimicrobial Evaluation

A series of new molecules containing pyrrolidine and thiazole moiety (4a-l) were designed and synthesized. The structures of the synthesized compounds were characterized by IR, 1H NMR and mass spectral data. All the synthesized compounds were screened for their antibacterial activity against strains of bacteria as well as antifungal activity against fungal strains. Minimum inhibitory concentrations (MICs) of all the synthesized compounds were determined. The screening of title compounds revealed that most of the tested compounds showed moderate to good microbial inhibitions

scholarly journals Impact of antifungal resistance in Australia

2007 ◽  
Vol 28 (4) ◽  
pp. 174 ◽  
Author(s):  
David Ellis ◽  
Tania Sorrell ◽  
Sharon Chen
Keyword(s):  
Antifungal Activity ◽  
Selection Pressure ◽  
Opportunistic Infections ◽  
Fungal Infections ◽  
Fungal Species ◽  
Antifungal Drugs ◽  
Drug Resistant ◽  
Populations At Risk ◽  
Complete Resistance ◽  
Major Increase

The last two to three decades have seen a major increase in invasive fungal infections (IFIs), a small, but increasing proportion of which are caused by pathogens with partial or complete resistance to antifungal drugs. The increase in IFIs has largely been associated with the increase in immunocompromised and critically ill patients. Opportunistic infections with relatively drug-resistant environmental fungi account for much of the resistance. In addition, amongst the only fungal species to colonise humans, Candida, two species that are resistant (C. krusei) or relatively resistant (C. glabrata) to fluconazole have emerged. In part this is explained by the selection pressure exerted by widespread use of fluconazole. Together with the introduction of new antifungal drugs with selective and/or variable antifungal activity, these changes have stimulated interest in understanding mechanisms and origins of resistance, the identification of resistance in the laboratory and its relationship to clinical outcomes, and in surveillance of clinical isolates and populations at risk of IFIs.

scholarly journals A numerical method for mass spectral data analysis

2005 ◽  
Vol 18 (12) ◽  
pp. 1412-1417 ◽  
Author(s):  
Anthony J. Kearsley ◽  
William E. Wallace ◽  
Javier Bernal ◽  
Charles M. Guttman
Keyword(s):  
Data Analysis ◽  
Numerical Method ◽  
Spectral Data ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Spectral Data Analysis

scholarly journals Synthesis and Antimicrobial Screening of Some Novel 2, 5-Disubstituted 1, 3, 4-oxadiazole Derivatives

2011 ◽  
Vol 8 (s1) ◽  
pp. S149-S154 ◽  
Author(s):  
P. Panneerselvam ◽  
G. Geete Ganesh
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antibacterial And Antifungal Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
E Coli ◽  
H Nmr ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
New Compounds

The syntheses of series of 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives are described. A total of twelve new compounds were synthesized and characterized by IR,1H-NMR and Mass spectral data. All newly synthesized compounds were screened for their antimicrobial activityi.e. antibacterial activity againstS. aureusandE. coliand antifungal activity against fungusA. nigar. CompoundsG5andG7exhibited significant both antibacterial and antifungal activity whileG2,G10andG3,G9showed antibacterial and antifungal activity respectively. These compounds were 2, 5-disubstituted 1, 3, 4-oxadiazole moiety at position two and five showed reasonable antibacterial and antifungal activity.

scholarly journals Antifungal activities of quince seed mucilage hydrogel decorated with essential oils of Nigella sativa, Citrus sinensis and Cinnamon verum

2021 ◽  
Author(s):  
Mehdi Mirzaii ◽  
Marzieh Yaeghoobi ◽  
Meysam Afzali ◽  
Neginsadat Amirkhalili ◽  
Majid Mahmoodi ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Side Effects ◽  
Essential Oils ◽  
Ultrasonic Treatment ◽  
Fungal Infections ◽  
Vitro Assay ◽  
Antifungal Activities ◽  
Antifungal Properties

Background and Objectives: Candidiasis and pityriasis versicolor are opportunistic fungal infections that are caused by Candida spp. and Malassezia spp. yeasts. Conventional drugs like azole and amino derivatives are known to treat fungal skin diseases. However, drawbacks like long-term side effects and drug resistance lead to investigate on antifungal properties of phytochemicals as an alternative to available synthetic drugs. Materials and Methods: The herbal nano hydrogel was successfully synthesized from Quince Seed extract followed by ultrasonic treatment and it has been formulated using a mixture of essential oils. We evaluated the antifungal in vitro assay for a mixture of essential oils in combination with herbal nano hydrogel against Candida albicans and Malasezia furfur strains by micro dilution method. Results: The results indicated that essential oils possess antifungal activity with the MIC value of 12.5 and 6.24 mg/ml against C. albicans and M. furfur, respectively. No fungicidal effect was reported for the herbal hydrogel before nanofabrication while it shown some antifungal activity after ultrasonic treatment for 5 and 10 minutes. As anticipated; the antifungal property of essential oil mixture was appreciably improved when it combined with herbal nano hydrogel where the highest level of inhibition was observed at concentration of 3.125 mg/ml for both strains. The loss in biological activity observed when the ultrasonic treatment on herbal nano hydrogel performed for longer time. Conclusion: The proposed plant-based nano formulation shown promising in vitro antifungal activities against C. albicans and M. furfur strains and its antifungal properties were comparable with commercially available agents like clotrimazole. The new formulation expected to be safe with minimum long-term side effects. Further investigations are underway to confirm the safety and the mechanism of the action of this new herbal formulation.

Antibacterial and antifungal two phenolic sesquiterpenes from Dysoxylum densiflorum

2020 ◽  
Vol 75 (1-2) ◽  
pp. 1-5
Author(s):  
Ni Komang T. Dharmayani ◽  
Tsuyoshi Yoshimura ◽  
Elvira Hermawati ◽  
Lia D. Juliawaty ◽  
Yana M. Syah
Keyword(s):  
Pathogenic Bacteria ◽  
Antifungal Agents ◽  
Inhibitory Concentration ◽  
Antibacterial Properties ◽  
Acetone Extract ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
Antifungal Properties ◽  
Antibacterial And Antifungal ◽  
Dysoxylum Densiflorum

AbstractA new phenolic sesquiterpene, dysoxyphenol (1), and the known sesquiterpene, 7R,10S-2-hydroxycalamenene (2), were isolated from the acetone extract of Dysoxylum densiflorum seeds. The structures of these compounds were determined based on physical, Nuclear Magnetic Resonance, and mass spectral data. Both compounds were evaluated for their antibacterial and antifungal properties against seven pathogenic bacteria and two wood-rotting fungi, respectively. The results showed that both compounds have significant antibacterial properties only against Bacillus subtilis (Minimum Inhibitory Concentration 28 μM), while in the antifungal evaluation compound 1 was found to be more active than compound 2. Therefore, compound 1 has promising antifungal properties that can be developed further for finding new antifungal agents.

scholarly journals Synthesis and antimicrobial activity of triazolyl analogs of diosgenin

2017 ◽  
Vol 6 (4) ◽  
pp. 227-233
Author(s):  
Masood-ur-Rahman ◽  
◽  
Khursheed Ahmad Bhat ◽  
Tabassum Ara ◽  
◽  
...  
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Bacterial Strains ◽  
Parent Molecule ◽  
Fungal Strains ◽  
Meta Position ◽  
Antifungal Potential ◽  
Beneficial Impact ◽  
Comparable Activity ◽  
Antibacterial And Antifungal

Novel and diverse triazoles of steroidal sapogenin-diosgenin were prepared using click chemistry approach. All the derivatives were subjected to antimicrobial screening to check their antibacterial and antifungal potential. All the tested analogs were inactive towards the tested bacterial strains, while as, some analogs displayed better activity towards the tested fungal strains. Of the synthesized analogs, Dgn-3 and Dgn-6 exhibited antifungal activity against Candida albicans with MICs of 12 and 16 µg/ml respectively, while as, Dgn-8 and Dgn-9 showed potency towards both the tested fungal strains: Candida albicans and Aspergillus fumigatus. The other derivatives showed almost comparable activity with that of the parent molecule. The structure-activity relationship (SAR) revealed that the analogs with electron withdrawing substituents (-NO2 and -CN) at meta position in R moieties along with analogs bearing bromo substituted R moieties seem to have beneficial impact on the antifungal activity.

Synthesis and Antimicrobial Screening of 2"-Amino-4"-[2-(4'-Chlorophenyl)-6-Methyl Imidazo[1, 2-a]Pyridine -3-yl]-6"-Aryl-4"-H-Pyran-3"-Carbonitrile

2015 ◽  
Vol 49 ◽  
pp. 149-154 ◽  
Author(s):  
V.V. Bhuva ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antibacterial Activity ◽  
Biological Activity ◽  
Antifungal Activity ◽  
Thin Layer ◽  
Moderate Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Layer Chromatography

3-Cyano-4,6-disubstituted 4H-pyrans are endowed with a variety of pharmacodynamic activities Looking to the interesting properties of cyanopyrans, it was considered worthwhile to synthesis some new 2"-amino-4"-[2-(4'-chlorophenyl) -6-methyl imidazo [1,2-a] pyridin-3-yl]-6"-aryl-4"-H-pyran-3"- carbonitrile ( 4a-4l ) have been synthesized. The products have been assayed for their biological activity against Gram +ve, Gram –ve bacteria and fungi. Some of the products showed moderate activity in concentration 50μg/mL. The structures of the products have been elucidated by IR, 1H-NMR, Mass spectral data, elemental analysis and thin layer chromatography.Keywords: Cyanopyrans; antibacterial activity; antifungal activity

scholarly journals A second generation fungerp analog SCY-247, shows potent in vitro activity against Candida auris and other clinically relevant fungal isolates

2020 ◽  
pp. AAC.01988-20
Author(s):  
Sherman Chu ◽  
Lisa Long ◽  
Rania Sherif ◽  
Thomas S. McCormick ◽  
Katyna Borroto-Esoda ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Second Generation ◽  
Fungal Infections ◽  
Parent Compound ◽  
Fungal Species ◽  
Antifungal Compound ◽  
Candida Auris ◽  
Fungal Cell ◽  
Antifungal Properties

Due to the increase of antifungal drug resistance and difficulties associated with drug administration, new antifungal agents for invasive fungal infections are needed. SCY-247 is a second-generation fungerp antifungal compound that interferes with the synthesis of the fungal cell wall polymer ß-(1,3)-D-glucan. We conducted an extensive antifungal screen of SCY-247 against yeast and mold strains compared with the parent compound ibrexafungerp (IBX, formerly SCY-078) to evaluate the in vitro antifungal properties of SCY-247. SCY-247 demonstrated similar activity to IBX against all of the organisms tested. Moreover, SCY-247 showed a higher percentage of fungicidal activity against the panel of yeast and mold isolates compared to IBX. Notably, SCY-247 showed considerable antifungal properties against numerous strains of Candida auris. Additionally, SCY-247 retained its antifungal activity when evaluated in the presence of synthetic urine, indicating that SCY-247 maintains activity and structural stability under environments with decreased pH levels. Finally, a time-kill study showed SCY-247 has potent anti-Candida, Aspergillus, and Scedosporium activity. In summary, SCY-247 has potent antifungal activity against various fungal species, indicating that further studies on this fungerp analog are warranted.

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