scholarly journals Synthesis of New Hispolon Derived Pyrazole Sulfonamides for Possible Antitubercular and Antimicrobial Agents

2021 ◽  
Vol 65 (2) ◽  
Author(s):  
Hari Babu Bollikolla ◽  
V. S. Narasimha Raju Pericherla ◽  
Jagan Mohana Rao Saketi ◽  
V. Balaji Neduri ◽  
Chandra Mohan Kurmarayuni ◽  
...  

Abstract. A series of 10 new hispolonpyrazole sulfonamides were designed and synthesized using hispolons and 4-sulfonamide phenylhydrazine hydrochloride with better yields. The synthesized pyrazole sulfonamides were screened for anti-TB, anti-bacterial, and anti-fungal activities to compare the role sulfonamide moiety. Among them, 3a and 3b showed selective potent anti-tubercular nature (MIC 6.25µg/mL). Further, the antimicrobial studies of the compounds showed only compound 3b with a good inhibition zone on Staphylococcus aureus among other bacteria and fungi studied.   Resumen.Se prepararon 10 nuevas hispolon-pirazol-suklfonamidas con buenos rendimientos haciendo reaccionar hipolonas y el clorhidrato de 4-sulfonamidil-fenílhidrazina. Los productos obtenidos se probaron contra cepas de hongos y bacterias con especial interés en la tuberculosis, encontrando algunos derivados con actividades del orden de MIC 6.25µg/mL.

Author(s):  
Sudhakar Chekuri ◽  
Arun Jyoti B ◽  
Saraswathi JSompaga ◽  
Shivaprasadi Panjala ◽  
Roja Ran Anupalli

Anti-microbial and anti-fungal activity of different solvent extracts of Acalypha indica (Euphorbeace family) was tested against bacterial pathogens (Pseudomonasaeruginosa, E.Coli, KlebsiellaPneumonia and Staphylococcus aureus) and fungal strains (Candida albicans, Aspergillus niger, Candida tropicalis andCandida kefyr) using the Agar Well diffusion method . It was observed that all the extracts showed positive activity) against bacteria and fungi. Ethanolic extract of Acalypha indica showed more potency against Staphylococcus aureus with an inhibition zone of12.46 (mm) and Methanolic extract exhibited higher activity against E.coli with an inhibition zone of11.26 (mm). Ethanolic extract of Acalypha indica showed prominent antifungal activity against candida albicans with an inhibition diameter of 12.53 (mm) and Aspergillus niger with a diameter of 9.21 (mm) when compared to other solvent extracts. Erythromycin and Ketoconazole were used as positive standards for antimicrobial and anti fungal experiments. In the present study, Ethanol extract showed a varying degree of inhibition to the growth of tested organisms compared to Methanol, Acetone and Chloroform against Bacteria and Fungi. The results confirmed the presence of antibacterial and antifungal compounds in shade dried extracts of Acalypha indica against human pathogenic organisms.


2020 ◽  
Vol 6 (2) ◽  
pp. 246
Author(s):  
Yayuk Bulam Sarifati ◽  
Sjarif Ismail ◽  
Khemasili Kosala

Mekai leaves (Pycnarrhena cauliflora Diels.) (P. cauliflora). Are known to contain flavonoid compounds, tannins and phenolics that act as antibacterial agents and are used in the treatment of eye pain. Staphylococcus aureus (S. aureus) is one of the examples of bacterial diseases of eye pain and also a major cause of many infections in communities and health facilities with cases of resistance to various antimicrobial agents. The purpose of this study was to prove the antibacterial activity of mekai leaves ethanol extract against S. aureus bacteria. This research is an experimental research. The stages of this research began by extracting mekai leaves using maceration method with 96% ethanol solvent. Antibacterial activity was tested by the disc method (Kirby-Bauer) using ethanol extract concentrations of mekai leaves (EPC) 20%, 30%, 40%, 50%, 60%, 70%, and 80%, positive control using 25 μg amoxicillin and negative control using DMSO 10%. The measurement results of inhibition zones of mekai leaf ethanol extract 20%, 30%, 40%, 50%, 60%, 70% and 80% respectively were 8.32 mm, 8.32 mm, 8.32 mm, 8.67 mm, 9.00 mm, 8.67 mm, and 8.33 mm. While the positive control measurement of 25 μg amoxicillin against S. aureus is 28.67 mm and the measurement of 10% negative DMSO control does not produce inhibitory zones, so it can be concluded that the ethanol extract of mekai leaves has antibacterial activity, but the area of ​​inhibition zone produced is smaller than amoxicillin 25 µg. The results of statistical tests using Mann Whitney between negative controls with all EPC concentrations obtained significant differences with p values ​​<0.05, it can be concluded that there is antibacterial activity produced at all EPC concentrations.


2018 ◽  
Vol 2018 ◽  
pp. 1-6 ◽  
Author(s):  
Ahmed M. Amer

The discovery of novel and more efficient antimicrobial agents from natural sources like plants is one of the most important ways through which the growing threat of antibiotic-resistant pathogens can be overcome. Herein, we report the potential antimicrobial activity ofCichorium endiviaL.subsp.pumilum. Different concentrations of various solvent extracts prepared from several parts of chicory were tested for their antimicrobial effect against a panel of microorganisms. The antimicrobial activity was analyzed using the well diffusion method, where zones of inhibition were used as indicators of antimicrobial activity. The results indicated the superiority of seed extracts over both leaf and root extracts. Methanol extracts showed higher activity compared with chloroform and water extracts. Increased solvent extract concentration was accompanied by a parallel increase in the diameter of the inhibition zone. Gram-positive bacteria were found to be more sensitive than Gram-negative bacteria and fungi. On a whole, the highest observed inhibition zones (21.3 ± 0.6 and 20.1 ± 0.4 mm) were recorded with the methanolic extract of chicory seeds againstS. aureusandB. cereus, respectively.These results offer insights into the antimicrobial potency of this Egyptian local plant and provide a basis for further phytochemical and pharmacological research.


2018 ◽  
Vol 101 (4) ◽  
pp. 956-959 ◽  
Author(s):  
Maria Anna Coniglio ◽  
Pasqualina Laganà ◽  
Giuseppina Faro ◽  
Marina Marranzano

Abstract The purpose of this study was to investigate the antibacterial effect of 71 organic Sicilian honeys of different botanical origins against Staphylococcus aureus [American Type Culture Collection (ATCC) 9144™] and Pseudomonas aeruginosa (ATCC 27853™). The antimicrobial activity was determined by means of an agar diffusion assay from the estimation of the diameter of the inhibition zone produced by the honeys. S. aureus was more inhibited than P. aeruginosa (chi-square value 11.2698, P value 0.000788). In particular, a statistically significant inhibition growth against S. aureus was exhibited by the polyfloral (chi-square value 6.1714, P value 0.012983) and the eucalyptus honeys (chi-square value 4, P value 0.0455). Results partially suggest Sicilian organic polyfloral and eucalyptus honeys as possible alternatives to antimicrobial agents when S. aureus resistance causes failure of initial conventional antibiotic treatment.


2021 ◽  
Vol 23 (1) ◽  
pp. 378
Author(s):  
Piotr Roszkowski ◽  
Jolanta Szymańska-Majchrzak ◽  
Michał Koliński ◽  
Sebastian Kmiecik ◽  
Małgorzata Wrzosek ◽  
...  

Eleven novel imide-tetrazoles were synthesized. In the initial stage of research, in silico structure-based pharmacological prediction was conducted. All compounds were screened for antimicrobial activity using standard and clinical strains. Within the studied group, compounds 1–3 were recognized as leading structures with the most promising results in antimicrobial studies. Minimal inhibitory concentration values for compounds 1, 2, 3 were within the range of 0.8–3.2 μg/mL for standard and clinical Gram-positive and Gram-negative bacterial strains, showing in some cases higher activity than the reference Ciprofloxacin. Additionally, all three inhibited the growth of all clinical Staphylococci panels: Staphylococcus aureus (T5592; T5591) and Staphylococcus epidermidis (5253; 4243) with MIC values of 0.8 μg/mL. Selected compounds were examined in topoisomerase IV decatenation assay and DNA gyrase supercoiling assay, followed by suitable molecular docking studies to explore the possible binding modes. In summary, the presented transition from substrate imide-thioureas to imide-tetrazole derivatives resulted in significant increase of antimicrobial properties. The compounds 1–3 proposed here provide a promising basis for further exploration towards novel antimicrobial drug candidates.


2019 ◽  
Vol 7 (7) ◽  
pp. 391-397
Author(s):  
O. Adeyanju ◽  
S. V. Francis ◽  
R. R. Ede ◽  
P.S. Jang ◽  
J.K. Bulus

Elemental analysis, phytochemical screening and antimicrobial activities of aqueous and ethanolic leaf extract of Pilostigma reticulatum (dc) Hochst were studied using paper disc diffusion method against Streptococcus pyogen, Escherichia coli and Salmonella thvpi. Elemental analysis of the plant sample revealed the presence of Ca (1.51 ± 0.01μg/g), Mg (0.43 ± 0.02μg/g). P (0.29 ± 0.01 μg/g), Mn (3.01 ± 0.01 μg/g), Fe (1.04 ± 0.01 μg/g), Zn (1.05 ± 0.02  and Cu was below detectable limit(BDL).The results of the antimicrobial studies indicated that the extracts inhibited the growth of one or more tested pathogens.The ethanolic extract showed a broad spectrum of antimicrobial activity. Phytochemical investigation revealed the presence of tannins, alkaloids, glycosides, flavonoids, carbohydrates and terpenes. Anthraquinone and saponin were not present. Inhibition zone by the extract ranges from 4.0mm to 30mm.The minimum inhibitory concentration (MIC) ranges from 8.0 x102 µg/ml to 1x104 µg/ml. Pilostigma reticulatum leaf may be able to produce antimicrobial agents in drug delivery.


2014 ◽  
Vol 886 ◽  
pp. 337-340 ◽  
Author(s):  
Jun Xie ◽  
Xiao Qin Jiang ◽  
Ya You Ye ◽  
Hao Kai Teng ◽  
Bing Wang ◽  
...  

This work was designed to evaluate the antibacterial activity of one novel leather material treated with bactericides. The growth of bacteria species such as colibacillus and staphylococcus aureus were measured by the diameter of inhibition zone. The results showed that glutaraldehyde exhibits an antibacterial activity against colibacillus and staphylococcus aureus. Besides, it also is testified that 2-Octyl-4-isothiazolin-3-one was an excellent bactericidal agents to staphylococcus aureus, instead of colibacillus. The concentrations of tea saponin and sodium above 0.05mg/L, the growth of bacteria was restrained. In addition, compared with single of bactericidal agents, the mixture of two bactericidal agents showed much better antibacterial activity. Among these antimicrobial agents, the mxture of 2-Octyl-4-isothiazolin-3-one and glutaraldehyde were of great potential in application.


Author(s):  
Mina Usefi ◽  
Hengameh Zandi ◽  
Sara Jambarsang ◽  
Mehdi Mokhtari ◽  
Mahmood Noori Shadkam

Introduction: Today, disinfection of surfaces by using antimicrobial agents is critical for the prevention and control of pathogens and reduction of infection in hospital. The aim of this study was to investigate and compare the effects of two disinfectants against Staphylococcus aureus isolated from the NICU of Shahid Sadoughi Hospital of Yazd in 2017. Materials and Methods: In this descriptive cross sectional study, bacterial culture of samples collected from different surfaces of the NICU and S. aureus isolates were identified using conventional biochemical tests. Peracetic acid and chlorine dioxide various concentrations were used as disinfectants. Their effects against Staphylococcus aureus were determined by Standard disc diffusion method. Data were analyzed by linear mixed models in SPSS version 23. Results: 39.39% of samples were found to be S. aureus infected. The mean diameter of growth inhibition zone for peracetic acid 0.1% was significantly lower than that for peracetic acid 0.2%, and peracetic acid 0.1% was significantly higher than that for chlorine dioxide (P < 0.001). The comparison of growth inhibition zone diameters for peracetic acid 0.1% and chlorine dioxide disinfectants showed that the average diameter of the inhibition zone created by peracetic acid 0.1% was significantly higher than that created by chlorine dioxide. The most effective disinfectant on S. aureus strains isolated was peracetic acid 0.2% and the least effective disinfectant was chlorine dioxide. Conclusion: In health care facilities with S. aureus infection, peracetic acid 0.2% can be used effectively to reduce nosocomial infection rate.


Author(s):  
Mohammed AbdulReda Yassen

Bacterial infections become a great health problems. The new antimicrobial agents are will reduce this problem. In this study, antimicrobial of activity of extract of Nigella sativa seed that used against Staphylococcus aureus isolates was evaluated. Started with an objective to appraisal the antibacterial potentials of ethanol extractofNigella sativaprepared in different concentrations (50,100, 200& 400 mg/ml) against Staphylococcus aureus and associated its activity with antibiotic concentration value Ciprofloxacin (5µg),Amoxicillin (25µg) & Penicillin (6µg) by determining the inhibition zone produced around the holes after growth on Muller-Hinton agar. This results showed activity of antibacterial of the Nigella sativa at differentconcentrationsand standard antibiotics exhibited various degrees of zones of inhibition in the culture media depending mainly upon the type of plant extract,concentration of extract in addition to the type of tested bacterial. Nearly all the Nigella sativa extracts were found to have significant activity (p<0.05) against all tested bacteria related with negative control. In the same time the current study was recorded that inhibition zones diameter against examined bacteria raised significantly difference (p<0.05) at extract concentration raised (400 mg / ml ). The MIC values ofethanolic extracts of Nigella sativaextended from 0.156 to 0.312 mg/ml against tested bacteria. Whereas the MBC values ranged 1.248 mg/ml.


2020 ◽  
Vol 21 (9) ◽  
Author(s):  
BQ. MUTMAINNAH ◽  
AFAF BAKTIR ◽  
NI’MATUZAHROH NI’MATUZAHROH

Abstract. Mutmainnah BQ, Baktir A, Ni’matuzahroh. 2020. Characteristics of Methicillin-Resistant Staphylococcus aureus (MRSA) and Methicillin Sensitive Staphylococcus aureus (MSSA) and their inhibitory response by ethanol extract of Abrus precatorius. Biodiversitas 21: 4076-4085. Three isolates of Staphylococcus bacteria with the code MRSA 22372, MSSA 22187 and MSSA 22366 originated from the urine of the patient at Dr. Regional General Hospital Soetomo, Clinical Microbiology Installation Surabaya, Indonesia. Differences in bacterial strains affect their sensitivity to antimicrobial agents. The active ingredient of the ethanol extract of the leaves of Abrus precatorius L. has the potential to inhibit bacterial growth. This study aims to further characterize the bacteria MRSA 22372, MSSA 22187 and MSSA 22366 based on morphological, biochemical and molecular characters and to compare the growth inhibitory response of these three bacteria due to the treatment of variations in the ethanol extract of A. precatorius of 25 mgL-1- 800 mgL-1 leaves. The results showed there were differences in the diameter of bacterial colonies, the ability to ferment glucose and sucrose, and the production of urease and catalase. The molecular characteristics of the three bacteria have no similarity in the order of nucleotide bases or phylogenetic proximity to each other. Ethanol extract of A. precatorius leaves at a concentration of 800 mgL-1 inhibited the growth of MSSA 22187 with an inhibition zone of 41 mm and decreased the MSSA 22366 growth by 67.6%. MIC value of ethanol extract of A. precatorius leaves in all three bacteria was 25 mgL-1 with growth inhibition up to 29.4%, 35.3%, and 29.4% respectively. Keyword : MRSA, MSSA, ethanol extract, Abrus precatorius L.


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