scholarly journals Synthesis and Antimicrobial Studies of Some New 3-Isoxazoline Substituted Phthalazine Methylsulfonyl Oxadiazoles

2011 ◽  
Vol 8 (3) ◽  
pp. 1022-1029 ◽  
Author(s):  
A. M. Sridhara ◽  
K. R. Venugopala Reddy ◽  
J. Keshavayya ◽  
D. S. Ambika ◽  
Sanathkumar Goud ◽  
...  

A series of new 3-isoxazoline substituted phthalazine methylsulfonyl-oxadiazoles were prepared from methyl 2-(4-oxo-3,4-dihydrophthalazin-1-yl) acetate. The structure of synthesized compounds were characterized by spectral data and screened for their antimicrobial activities against various bacteria and fungi strains. Several of these compounds showed antimicrobial activity.

2021 ◽  
Vol 62 (1) ◽  
Author(s):  
Junpeng Li ◽  
Shuping Hu ◽  
Wei Jian ◽  
Chengjian Xie ◽  
Xingyong Yang

AbstractAntimicrobial peptides (AMPs) are a class of short, usually positively charged polypeptides that exist in humans, animals, and plants. Considering the increasing number of drug-resistant pathogens, the antimicrobial activity of AMPs has attracted much attention. AMPs with broad-spectrum antimicrobial activity against many gram-positive bacteria, gram-negative bacteria, and fungi are an important defensive barrier against pathogens for many organisms. With continuing research, many other physiological functions of plant AMPs have been found in addition to their antimicrobial roles, such as regulating plant growth and development and treating many diseases with high efficacy. The potential applicability of plant AMPs in agricultural production, as food additives and disease treatments, has garnered much interest. This review focuses on the types of plant AMPs, their mechanisms of action, the parameters affecting the antimicrobial activities of AMPs, and their potential applications in agricultural production, the food industry, breeding industry, and medical field.


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.


Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2793 ◽  
Author(s):  
Ameen Abu-Hashem

Substituted-6-methyl-1-thioxo-1,2-dihydro-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-ones (5a,b) were synthesized from condensation of visnagenone (2a) or khellinone (2b) with 6-amino-thiouracil (3) in dimethylformamide or refluxing of (4a) or (4b) in dimethylformamide. Hence, compounds (5a,b) were used as the starting materials for preparing many new heterocyclic compounds such as; furo[3,2-g]pyrimido[1,6-a]quinazoline (6a,b), furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazolinone (7a,b), substituted-benzylidene-furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazoline-3,5-dione (8a–f), 3-oxo-furo[3,2-g]pyrimido[1,6-a]quinazoline-pentane-2,4-dione (9a,b), 1-(pyrazole)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (10a,b), 2-(oxo or thioxo)-pyrimidine-furo[3,2-g]pyrimido[1,6-a]quinazolinone (11a–d), 1-(methylthio)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (12a,b), 1-(methyl-sulfonyl)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (13a,b) and 6-methyl-1-((piperazine) or morpholino)-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-one (14a–d). The structures of the prepared compounds were elucidated on the basis of spectral data (IR, 1H-NMR, 13C-NMR, MS) and elemental analysis. Antimicrobial activity was evaluated for the synthesized compounds against Gram-positive, Gram-negative bacteria and fungi. The new compounds, furothiazolo pyrimido quinazolines 8a–f and 11a–d displayed results excellent for growth inhibition of bacteria and fungi.


2008 ◽  
Vol 25 (No. 2) ◽  
pp. 81-89 ◽  
Author(s):  
A. Adiguzel ◽  
H. Ozer ◽  
H. Kilic ◽  
B. Cetin

The present work reports the <i>in vitro</i> antimicrobial activities of the essential oil and methanol extract from <i>Satureja hortensis</i> as well as the content of its essential oil. The chemical composition of hydrodistilled essential oil of Satureja hortensis was analysed by means of GC-MS. Thirty constituents were identified. The main constituents of the oil were thymol (40.54%), &gamma;-terpinene (18.56%), carvacrol (13.98%), and <i>p</i>-cymene (8.97). The essential oil of <i>Satureja hortensis</i> exhibited the activity against 25 bacteria, 8 fungi, and a yeast, <i>C. albicans</i>; exerting the Minimum Inhibitory Concentration values (MIC) ranging from 15.62 to 250 &micro;l/ml. Similarly, methanol extract of the plant also showed antimicrobial activity.


2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Awol Mekonnen ◽  
Berhanu Yitayew ◽  
Alemnesh Tesema ◽  
Solomon Taddese

In this study, thein vitroantimicrobial activities of four plant essential oils (T. schimperi,E. globulus,R. officinalis, andM. Chamomilla) were evaluated against bacteria and fungi. The studies were carried out using agar diffusion method for screening the most effective essential oils and agar dilution to determine minimum inhibitory concentration of the essential oils. Results of this study revealed that essential oils ofT. schimperi,E. globulus, andR. officinaliswere active against bacteria and some fungi. The antimicrobial effect ofM. chamomillawas found to be weaker and did not show any antimicrobial activity. The minimum inhibitory concentration values ofT. schimperiwere<15.75 mg/mL for most of the bacteria and fungi used in this study. The minimum inhibitory concentration values of the other essential oils were in the range of 15.75–36.33 mg/mL against tested bacteria. This study highlighted the antimicrobial activity of the essential oil ofE. globulus,M. chamomilla,T. Schimperi, andR. officinalis. The results indicated thatT. schimperihave shown strong antimicrobial activity which could be potential candidates for preparation of antimicrobial drug preparation.


2007 ◽  
Vol 72 (4) ◽  
pp. 321-329 ◽  
Author(s):  
Sohel Mostahar ◽  
Sayed Alam ◽  
Azizul Islam

Two new 2'-oxygenated flavones have been synthesized via chalcone precursors and the biocidal activity of these two flavones, along with the corresponding chalcones against microbes (bacteria and fungi) and brine shrimp nauplii were investigated. Both the flavones (compounds 6 and 7) and their corresponding chalcones (compounds 4 and 5) showed good activity against all the tested bacterial and fungal strains. The LC50 values of compounds 4-7 were found to be 2.31, 0.94, 1.39 and 0.58 ?gmL -1, respectively. The synthesized compounds were characterized using UV-Vis, IR, 1H-NMR and 13C-NMR spectral data, together with elemental analysis. .


2010 ◽  
Vol 62 (3) ◽  
pp. 633-641 ◽  
Author(s):  
Pirbalouti Ghasemi ◽  
Parvin Jahanbazi ◽  
Shekoofeh Enteshari ◽  
Fatemeh Malekpoor ◽  
Behzad Hamedi

The major aim of this study was to determine the antimicrobial activity of the extracts of eight plant species which are endemic in Iran. The antimicrobial activities of the extracts of eight Iranian traditional plants, including Hypericum scabrum, Myrtus communis, Pistachia atlantica, Arnebia euchroma, Salvia hydrangea, Satureja bachtiarica, Thymus daenensis and Kelussia odoratissima, were investigated against Escherichia coli O157:H7, Bacillus cereus, Listeria monocytogenes and Candida albicans by agar disc diffusion and serial dilution assays. Most of the extracts showed a relatively high antimicrobial activity against all the tested bacteria and fungi. Of the plants studied, the most active extracts were those obtained from the essential oils of M. communis and T. daenensis. The MIC values for active extract and essential oil ranged between 0.039 and 10 mg/ml. It can be said that the extract and essential oil of some medicinal plants could be used as natural antimicrobial agents in food preservation. .


Author(s):  
J.V. Guna ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit

2- Methoxy – 6 - {4' - [(4'''- Chlorophenyl) (phenyl) methyl amino] phenyl} - 4 - aryl nicotinonitrile (3a-3l) and 2-Amino-6-{4'-[(4'''-Chlorophenyl)(phenyl)methyl amino]phenyl}-4-aryl nicotinonitrile (4a-4l) have been synthesized. The products have been assayed for their antimicrobial activity against Gram +ve, Gram -ve bacteria and fungi. The structure of the products has been elucidated by IR, 1H-NMR, mass spectral data, elemental analysis and thin layer chromatography.


Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 4009 ◽  
Author(s):  
Alsaedi ◽  
Farghaly ◽  
Shaaban

A novel series of pyrazolo[1,5-a]pyrimidine ring systems containing phenylsulfonyl moiety have been synthesized via the reaction of 2-(phenylsulfonyl)-1-(4-(phenylsulfonyl) phenyl)ethan-1-one, 2-benzenesulfonyl-1-(4-benzenesulfonyl-phenyl)-3-dimethylamino-propenone and 3-(dimethylamino)-1-(4-(phenylsulfonyl)phenyl)prop-2-en-1-one each with various substituted aminoazopyrazole derivatives in one pot reaction strategy. The proposed structure as well as the mechanism of their reactions were discussed and proved with all possible spectral data. The results of antimicrobial activities of the new sulfone derivatives revealed that several derivatives showed activity exceeding the activity of reference drug. Contrary to expectations, we found that derivatives containing one sulfone group are more effective against all bacteria and fungi used than those contain two sulfone groups.


2009 ◽  
Vol 55 (12) ◽  
pp. 1381-1391 ◽  
Author(s):  
Aline B.M. Vaz ◽  
Rubens C. Mota ◽  
Maria Rosa Q. Bomfim ◽  
Mariana L.A. Vieira ◽  
Carlos L. Zani ◽  
...  

The purpose of this study was to examine antimicrobial activity of endophytic fungi isolated from the leaves, stems, and roots of 54 species of Orchidaceae collected in a Brazilian tropical ecosystem. In total, 382 filamentous fungi and 13 yeast isolates were obtained and cultured to examine the production of crude extracts. Thirty-three percent of the isolates displayed antimicrobial activity against at least one target microorganism. The multivariate statistical analyses conducted indicate that the extracts of endophytic fungi isolated from leaves of terrestrial orchids in semideciduous forest were more active against Escherichia coli , whereas extracts of endophytic fungi from roots of rupicolous orchids collected in rock fields were more active against Candida krusei and Candida albicans . Among the fungi that were screened in the study, 22 isolates held their antimicrobial activities after replication and were therefore selected for assessment of the minimum inhibitory concentration (MIC), which ranged from 62.5 to 250 µg/mL and 7.8 to 250 µg/mL against bacteria and fungi, respectively. One isolate of Alternaria sp. and one isolate of Fusarium oxysporum presented the strongest antibacterial activity. Three Fusarium isolates, Epicoccum nigrum , and Sclerostagonospora opuntiae showed the greatest MIC values against the pathogenic yeasts. This study is the first survey investigating the bioactive potential of endophytic fungi associated with tropical Orchidaceae species present in Brazilian ecosystems.


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