Synthesis and Antimicrobial activity of Piperazine analogues containing [1, 3, 4] Thiadiazole ring

Author(s):  
Kottakki Naveen Kumar ◽  
Karteek Rao Amperayani ◽  
Uma Devi Parimi

A new series of piperazine-1, 3, 4-thiadiazole has been synthesized, purified and characterized with the help of their analytical and spectral data. Structures of the synthesized compounds were confirmed by IR, 1H NMR and mass spectroscopy. The potential antimicrobial effects of the synthesized compounds were investigated using Vibrio cholera and Bacillus subtilis. The newly synthesized compounds exhibited capable activities against Vibrio cholera and Bacillus subtilis and it showed minimum inhibitory concentration. In this study, few compounds showed appreciable antibacterial activity. The compound PT6 shows highly significant antibacterial and good inhibition as compared to the standard drug.

10.17158/232 ◽  
2012 ◽  
Vol 18 (1) ◽  
Author(s):  
Judee N. Nogodula ◽  
Jessa Marie D. Draug ◽  
Maryjane S. Jamero

Taro (Colocasia esculenta) plant is commonly available and popularly used as food and alternative medicine. To prove its medicinal value, the study explored its secondary metabolites from aqueous-ethanolic leaf extract. Specifically, this investigation aimed to classify its acute dermal toxicity and antibacterial activity, determine its Minimum Inhibitory Concentration (MIC), and identify the equipotency with the standard drug and mutagenic activity. Phytochemical screening of tannins, alkaloids, saponins, cardenolides and bufadienolides, flavonoids, polyphenol compounds and anthraquinones was performed. Five healthy female rabbits were used for toxicity test based on OECD guidelines 404. Kirby-Bauer method was employed for antibacterial activity (susceptibility and potency tests) using Methicillin-Resistant Staphylococcus aureus ATCC 43300, Clinical Isolate Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli. A two-fold agar dilution was applied for Minimum Inhibitory Concentration and Ames test was employed for direct mutagenicity assay using Salmonella typhimurium TA98. Results showed that leaf extract has no anthraquinone and it is categorized as non toxic up to allowable dose of 5000 mg/kg. The findings showed a significant difference on the mean zones of inhibition between Vancomycin and plant extract against S. aureus and between tetracycline and the extract towards E.coli. The MRSA and P. aeruginosa showed no significant differences. The MIC of extract is effective to MRSA and S. aureus at 105.26 and 50 mg/mL respectively. However, E. coli and P. aeruginosa are resistant up to the 105.26 mg/mL. Potency test revealed a non-comparability in strength between the extract and Azithromycin using Gram-negative bacteria. However, the extract showed comparable strength with the standard drug using MRSA and S. aureus. Ames test revealed a mutagenic activity using Salmonella typhimurium TA98.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Biswanath Chakraborty ◽  
Suchandra Chakraborty ◽  
Chandan Saha

The antibacterial activity of Murrayaquinone A (10), a naturally occurring carbazoloquinone alkaloid, and 6-methoxy-3,7-dimethyl-2,3-dihydro-1H-carbazole-1,4(9H)-dione (11), a synthetic carbazoloquinone, both obtained during the development of the synthesis of Carbazomycin G, having unique quinone moiety, was studied against Gram-positive (Bacillus subtilisandStaphylococcus aureus) and Gram-negative (Escherichia coliandPseudomonassp.) bacteria. Compound10showed antibacterial activities against both ofEscherichia coliandStaphylococcus aureuswhereas compound11indicated the activity againstStaphylococcus aureusonly. Both compounds10and11exhibited minimum inhibitory concentration (MIC) of 50 μg mL−1againstStaphylococcus aureus.


2017 ◽  
Vol 5 (04) ◽  
pp. 34-38
Author(s):  
Monika Gupta ◽  
Baljeet Kaur ◽  
Shailender Pratap Singh ◽  
Vivek Kumar Gupta

Thiadiazole is a heterocyclic compound containg both two nitrogen atom and one sulfur atom as a part of the aromatic five-membered ring. The imidazo [2,1-b]-1,3,4-thiadiazole ring system is the core skeleton of well known immunomodulator levamisole. The synthesis and antimicrobial activity of nine 6-Phenyl-2- substituted imidazo [2,1-b]-1,3,4-thiadiazole derivatives were reported against Gram +ve bacteria Bacillius subtilis (MTCC 121), Staphyloccus aureus (MTCC 87), Gram –ve bacteria Pseudomonas aeruginosa (MTCC 424), Escherichia coli (MTCC 40), and fungal strains Candida albicans (MTCC 183), Fusarium solani (MTCC 2935), Fusarium oxyporium (MTCC 2840). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The synthesized compound (6) and (5b) had moderate antibacterial activity especially with Gram negative Escherichia coli (MTCC 40) where (5a) and (5f) had good antibacterial activity. The structures of the synthesized compounds were established by IR, NMR and Mass spectral studies.


Marine Drugs ◽  
2019 ◽  
Vol 17 (3) ◽  
pp. 158 ◽  
Author(s):  
Walter Balansa ◽  
Ute Mettal ◽  
Zerlina Wuisan ◽  
Anuchit Plubrukarn ◽  
Frans Ijong ◽  
...  

Sponges are a well-known bioresource for bioactive compounds. In this study, antibacterial activity-guided fractionation of the extract from an Indonesian marine Dactylospongia elegans sponge led to the discovery of four merosesquiterpenoids, namely, a new sesquiterpenoid aminoquinone nakijiquinone V (1), along with illimaquinone (2), smenospongine (3), and dyctioceratine C (4). The structure of compound 1 was elucidated by 1D and 2D NMR as well as by LC-HRESIMS data analysis. Compounds 2–4 showed moderate to low antimicrobial activity against Bacillus megaterium DSM32 with a minimum inhibitory concentration (MIC) of 32 μg/mL, 32 μg/mL, and 64 μg/mL, respectively. Furthermore, compounds 2 and 3 both inhibited Micrococcus luteus ATCC 4698 with a MIC of 32 μg/mL. In conclusion, the isolated merosesquiterpenoids, which are known for their cytotoxic effects, showed antibacterial activity and prompt future structure activity relationship (SAR) studies concerning the various bioactivities observed for this group of natural products.


Author(s):  
Phan Vu Hai ◽  
Hoang Thi Hong Van ◽  
Nguyen Van Chao ◽  
Nguyen Dinh Thuy Khuong ◽  
Thuong Thi Thanh Le ◽  
...  

The chives and ginger’s bulbs were extracted by ethanol 96%, 72%, 48% within 5, 10 and 15 days for each concentration (15, 30 and 45 days in total, respectively). The solidified extract then was used for antibacterial activity against E. coli and Salmonella spp. isolated from fecal of chickens with diarrhoea. The results showed that both ginger and chive, which socked and leached for greater than 30 days gave better antibacterial ability. Extracts diluted at concentrations of 5 µg/µl, 7.5 µg/µl and 10 µg/µl of ginger and chive bulbs are resistant to both bacteria. Compared with antibiotics, E. coli was resistant to amoxicillin, whereas Salmonella spp. was resistant to gentamicin and amoxicillin. The minimum inhibitory concentration (MIC) of chives extract (30 days) was 16-63 (31-125) mg/ml and ginger extract (30 days) was 16-80 (2-4) mg/ml; overall, the results indicated that both extract had bacteriostatic/bactericidal effects on E. coli and Salmonella spp.


2017 ◽  
Author(s):  
Ardianti Febriana

AbstrakTumbuhan sarang semut (Myrmecodia pendens Merr. & L. M. Perry) secara empiris digunakan sebagai obat yang memiliki aktivitas antibakteri. Namun, belum pernah diteliti mengenai aktivitas antibakteri tersebut. Penelitian ini dilakukan untuk mengetahui aktivitas antibakteri umbi batang sarang semut (Myrmecodia pendens Merr. & L. M. Perry) terhadap bakteri Gram negatif dan Gram positif yaitu Pseudomonas aeruginosa dan Staphylococcus aureus, menentukan konsentrasi hambat tumbuh minimum (KHTM), dan nilai banding ak- tivitas antibakterinya terhadap tetrasiklin-HCl. Hasil pengujian aktivitas antibakteri umbi batang sarang semut menunjukkan bahwa ekstrak umbi batang sarang semut memiliki ak- tivitas antibakteri terhadap kedua bakteri tersebut. Konsentrasi hambat tumbuh minimum (KHTM) ekstrak umbi batang sarang semut (Myrmecodia pendens Merr. & L. M. Perry) terhadap Pseudomonas aeruginosa terletak pada konsentrasi 0,83 % , sedangkan pada Staph- ylococcus aureus terletak pada konsentrasi 0,8 %. Hasil uji banding ekstrak umbi batang sarang semut (Myrmecodia pendens Merr. & L. M. Perry) dengan tetrasiklin-HCl terhadap Pseudomonas aeruginosa dan Staphylococcus aureus berturut-turut sebesar 1 : 6,709 x 10-4 dan 1 : 1,038 x 10-5. Penapisan fitokimia menunjukkan bahwa ekstrak umbi batang sarang semut (Myrmecodia pendens Merr. & L. M. Perry) mengandung flavonoid dan polifenol.Kata kunci: Myrmecodia pendens Merr. & L. M. Perry, Aktivitas antibakteri, Pseudomo- nas, StaphylococcusABSTRACTThe ant plant (Myrmecodia pendens Merr. & L. M. Perry) is one of plant applied as tradi- tional medicine. Empirically, the tuber of the ant plant have antibacterial activity. However, the examination of antimicrobial activity from extract of the tuber has never been reported. The research was done to know the activity of antimcrobial againts Gram positive and Gram negatif bacteria such as Pseudomonas aeruginosa and Staphylococcus aureus, to determine Minimum Inhibitory Concentration (MIC) of the tuber, and comparative value antibacterial activity with tetracycline-HCl. The result revealed that the tuber of the ant plant (Myrmeco-dia pendens Merr. & L. M. Perry) has antibacterial activity againts those bacteria. The Min- imum Inhibitory Concentration of extract from the tuber of ant plant to Pseudomonas aeru- ginosa was in range 8,2x103-8,3x103 ppm of concentration, and to Staphylococcus aureus was in range 7,5x103-8x103 ppm of concentration. Comparative value of extract from the tuber of ant plant with tetracycline-HCl againts Pseudomonas aeruginosa and Staphylococ- cus aureus were respective 1:.6.709 x 10-4 and :1.038 x 10-5. Phytochemical screening showed that the extract of the tuber contains flavonoid and polifenol.Keywords: Myrmecodia pendens Merr. & L. M. Perry, Antibacterial activity, Pseudomonas, Staphylococcus


2016 ◽  
Vol 78 (6-8) ◽  
Author(s):  
Noor Izzatie Munira Kamaruddin ◽  
Nor Azah Mohamad Ali ◽  
Muhd Fauzi Safian ◽  
Zaidah Zainal Ariffin

Polyalthia stenopetala essential oils were extracted by hydrodistillation from the leaves and were analyzed using gas chromatography-flame ionization detector (GC-FID) and gas chromatography/mass spectrometry (GC/MS) system. Thirty one compounds were identified from the analysis. The most abundant components in the leaves oil are curzerene (37.56%) followed by viridiflorol (11.59%), germacrene B (3.77%) and aromadendrene (4.01%). The antimicrobial activity of the oil essential oils was determined with disk diffusion method and minimum inhibitory concentration (MIC) assay. Four bacteria, Staphylococcus aureus (ATCC 25923), Bacillus subtilis (ATCC 6633), Escherichia coli (ATCC 25922) Psedomonas aeruginosa (ATCC 10145) and two yeasts, Candida albicans (ATCC 10231) and Saccharomyces cerevisiae (ATCC 4098) were selected. The crude oil shows the most reactivity against B. subtilis (ATCC 6633) and C. albicans (ATCC 10231) with an inhibitory zone of 11mm. The minimum inhibitory concentration (MIC) of sample against Staphylococcus aureus (ATCC 25923), Bacillus subtilis (ATCC 6633), Escherichia coli (ATCC 25922) Psedomonas aeruginosa (ATCC 10145) and Candida albicans (ATCC 10231) in range of 0.5 mg/ml – 1.0 mg/ml which can categorized as strong.


INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (02) ◽  
pp. 36-43
Author(s):  
U. S. Mishra ◽  
◽  
P. N Murthy ◽  
A. K. Mahapatra

The present study focuses on, screening the anti-bacterial activities of methanol and chloroform extracts of the dried stem barks of Ziziphus xylopyrus. The anti-bacterial activities were evaluated against fifteen different bacterial strains by detecting minimum inhibitory concentration and zone of inhibition. The minimum inhibitory concentration (MIC) values were compared with control and zones of inhibition (ZOI) were compared with standard ciprofloxacin at concentration of 100 and 200 μg/mL. Among the two extracts, the methanolic extract showed better antibacterial activity compared to chloroform extract . The MIC values for different bacterial strains obtained were within the range of 100-300 μg/mL. The ZOI values showed that there was a little differences in the ZOI values between the standard and methanol extract within the range of 0.5 to 1mm. This was comparable with the standard drug. Anatomical, proximate analysis and chromatographic studies were also carried out to fulfill the botanical quality control standards.


2011 ◽  
Vol 140 ◽  
pp. 426-430
Author(s):  
Xing Feng ◽  
Lei Wang ◽  
Mei Ling Tao ◽  
Qing Zhou

Objective: To study antimicrobial activity of aqueous extract of maize silk. Methods: Choose Staphylococcus aureus, Pseudomonas aeruginosa, Bacillus cereus, Bacillus coli and Candida albicans as detected germs. Using methods of agar plated diffusions and tube continuous dilution to detect antimicrobial activity and minimum inhibitory concentration of aqueous extract of maize silk. Results:(1) Aqueous extract of maize silk has antimicrobial activity against bacteria such as Staphylococcus aureus and Bacillus subtilis, and the diameter of bacteriostatic circle is 17 and 28 millimeter; Candida albicans is also inhibited by aqueous extract and its diameter of bacteriostatic circle is 24 millimeter.(2)The antimicrobial activity against Staphylococcus aureus and Bacillus subtilis is 500mg/ml and 62.5mg/ml.The minimum inhibitory concentration to Candida albicans is 125mg/ml.(3) aqueous extract of maize silk has no antimicrobial activity on Pseudomonas aeruginosa and Bacillus coli. Conclusion: Staphylococcus aureus, Bacillus subtilis and Candida albicans can be inhibited by aqueous extract of maize silk.


2012 ◽  
Vol 77 (5) ◽  
pp. 619-626 ◽  
Author(s):  
Dejan Godjevac ◽  
Ljubodrag Vujisic ◽  
Ivan Vuckovic ◽  
Vlatka Vajs ◽  
Marina Sokovic ◽  
...  

The investigation of chemical composition and antimicrobial activity of the essential oil of Galatella linosyris was presented. Chemical analysis (GC/MS, NMR) showed that sabinene (40%), ?-pinene (35.5%), ?-pinene (4.5%), limonene (4%), ?-muurolene (4%), and E-Caryophyllene (3.3%) were dominant components in this oil. The microdilution assays was used to evaluate minimum inhibitory concentration (MIC) and minimum bactericidal/fungicidal concentration (MBC, MFC). G. linosyris essential oil exhibited better antifungal than antibacterial activity.


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