Antimicrobial Evaluation and Efficient Green Synthesis of 8-Substituted-2,5-dihydro-1,5-benzothiazepine Derivatives

2019 ◽  
Vol 4 (1) ◽  
pp. 32-35
Author(s):  
Priyanka Sharma

8-Substituted-2,5-dihydro-1,5-benzothiazepine derivatives have been synthesized by the reaction of 1-(2-furyl)-3-(3,4-dimethoxyphenyl)-2-propenone with six 5-substiuted-2-minobenzenethiols in dry ethanol saturated with dry HCl gas and also in the presence of aluminium nitrate as catalyst in dry ethanol. All the newly synthesized compounds were characterized by analytical and spectral data comprising IR, 1H NMR, 13C NMR, 19F NMR and mass studies. All these compounds have also been evaluated for their antimicrobial assay against the Gram-positive bacteria, Staphylococcus aureus and the Gram-negative bacteria, Pseudomonas aeruginosa and the fungus, Candida albicans. The antifungal activity was found to be more significant than antibacterial activity.

2018 ◽  
Vol 6 (2) ◽  
pp. 212
Author(s):  
Elok Dea Orens Ubung Wisnu ◽  
Indah Purnama Sary ◽  
Dwi Koko Pratoko

N-phenylbenzamide is benzamide derivatives, which is potential as an antibacterial agent. N-phenyl-4-chlorobenzamide is N-phenylbenzamide derivative that substitued by chloro to the para position and it was expected to enhance the antibacterial activity. N-phenyl-4-chlorobenzamide was synthesized by reacting 1,3-diphenyilthiourea and 4-chlorobenzoil chloride. This compound has been purified and provided 53% of product with crystal shape, white color, and melting point of 195-197 oC. The purification of this compound was confirmed by TLC and the structure was identified by 1H-NMR, 13C-NMR, and FTIR spectroscopy. This compound was tested for its activity against gram positive bacteria Staphylococcus aureus and gram negative bacteria Pseudomonas aeruginosa, evaluated by well diffusion method and the result showed no activity against both Staphylococcus aureus and Pseudomonas aeruginosa.   Keywords: N-phenyl-4-chlorobenzamide, synthesis, antibacterial activity


2015 ◽  
Vol 70 (3-4) ◽  
pp. 97-102 ◽  
Author(s):  
Pedro Aqueveque ◽  
Carlos Leonardo Céspedes ◽  
José Becerra ◽  
Marcelo Dávila ◽  
Olov Sterner

Abstract Liquid fermentations of the fungus Stereum rameale (N° 2511) yielded extracts with antibacterial activity. The antibacterial activity reached its peak after 216 h of stirring. Bioassay-guided fractionation methods were employed for the isolation of the bioactive metabolites. Three known compounds were identified: MS-3 (1), vibralactone (2) and vibralactone B (3). The three compounds showed antibacterial activity as a function of their concentration. Minimal bactericidal concentrations (MBC) of compound 1 against Gram-positive bacteria were as follows: Bacillus cereus (50 μg/mL), Bacillus subtilis (10 μg/mL) and Staphylococcus aureus (100 μg/mL). Compounds 2 and 3 were active only against Gram-negative bacteria. The MBC of compound 2 against Escherichia coli was 200 μg/mL. Compound 3 inhibited significantly the growth of E. coli and Pseudomonas aeruginosa, with MBC values of 50 and 100 μg/mL, respectively.


2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Alexis Peña ◽  
Luis Rojas ◽  
Rosa Aparicio ◽  
Libia Alarcón ◽  
José Gregorio Baptista ◽  
...  

The essential oil of the leaves of Espeletia nana Cuatrec, obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were α-pinene (38.1%), β-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), α-zingiberene (4.0%), and γhimachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923(200 μg/mL) and Enterococcus faecalis ATCC 29212 (600 μg/mL).


2017 ◽  
Vol 2017 ◽  
pp. 1-5 ◽  
Author(s):  
Salu Rai ◽  
Uday Narayan Yadav ◽  
Narayan Dutt Pant ◽  
Jaya Krishna Yakha ◽  
Prem Prasad Tripathi ◽  
...  

In Nepal, little is known about the microbiological profile of wound infections in children and their antimicrobial susceptibility patterns. Total of 450 pus/wound swab samples collected were cultured using standard microbiological techniques and the colonies grown were identified with the help of biochemical tests. The antimicrobial susceptibility testing was performed by Kirby-Bauer disc diffusion technique. Methicillin-resistantStaphylococcus aureusisolates were detected by using cefoxitin disc and confirmed by determining minimum inhibitory concentrations (MIC) of oxacillin. 264 (59%) samples were culture positive. The highest incidence of bacterial infections was noted in the age group of less than 1 year (76%). Out of 264 growth positive samples, Gram-positive bacteria were isolated from 162 (61%) samples and Gram-negative bacteria were found in 102 (39%) samples.Staphylococcus aureus(99%) was the predominant Gram-positive bacteria isolated andPseudomonas aeruginosa(44%) was predominant Gram-negative bacteria. About 19% ofS. aureusisolates were found to be methicillin-resistant MIC of oxacillin ranging from 4 μg/mL to 128 μg/mL. Among the children of Nepal, those of age less than 1 year were at higher risk of wound infections by bacteria.Staphylococcus aureusfollowed byPseudomonas aeruginosawere the most common bacteria causing wound infections in children.


2016 ◽  
Vol 2016 ◽  
pp. 1-8 ◽  
Author(s):  
Amit Gupta ◽  
Rajendra Singh ◽  
Pankaj K. Sonar ◽  
Shailendra K. Saraf

A series of new 4-thiazolidinone derivatives was synthesized, characterized by spectral techniques, and screened for antimicrobial activity. All the compounds were evaluated against five Gram-positive bacteria, two Gram-negative bacteria, and two fungi, at concentrations of 50, 100, 200, 400, 800, and 1600 µg/mL, respectively. Minimum inhibitory concentrations of all the compounds were also determined and were found to be in the range of 100–400 µg/mL. All the compounds showed moderate-to-good antimicrobial activity. Compounds4a[2-(4-fluoro-phenyl)-3-(4-methyl-5,6,7,8-tetrahydro-quinazolin-2-yl)-thiazolidin-4-one] and4e[3-(4,6-dimethyl-pyrimidin-2-yl)-2-(2-methoxy-phenyl)-thiazolidin-4-one] were the most potent compounds of the series, exhibiting marked antimicrobial activity againstPseudomonas fluorescens,Staphylococcus aureus,and the fungal strains. Thus, on the basis of results obtained, it may be concluded that synthesized compounds exhibit a broad spectrum of antimicrobial activity.


2019 ◽  
Vol 35 (4) ◽  
pp. 1248-1253
Author(s):  
Lubna Swellmeen ◽  
Amal Uzrail ◽  
Rand Shahin ◽  
Yusuf AL-Hiari

Fluoroquinolones are well known to have an anti-infective action. In the present study we described the synthesis of novel florouquinolones derivative as antimicrobial agent. The biological test highlighted a good inhibitory activity for the 7-Chloro-1-Alkyl-6-fluoro-8-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid derived synthons especially against pathogenic Gram-negative bacteria (Pseudomonas aeruginosa) and Gram-positive bacteria (Staphylococcus aureus and Streptococcus agalactiae). The binding interactions were monitored and could explain the good inhibitory activity of the synthesized derivatives of florouquinolones.


2021 ◽  
Vol 9 (2) ◽  
pp. 64-70
Author(s):  
Ahmed A. Al-Naqshbandi ◽  
Hedy A. Hassan ◽  
Mahmoud A. Chawsheen ◽  
Haval H. Abdul Qader

Wound infection with antibiotic-resistant bacteria can extend a patients’ debility and increase the expense of treatment in the long term; therefore, careful management of patients with wound infections is necessary to avoid complications. The usage of antimicrobial agent is a major factor in resistance development. This study aims to understand the causes of wound infections, as well as the criteria for diagnosing them for more sensible antibiotic prescribing. Samples from 269 wound patients were collected, and cultured for bacterial growth. Gram stain technique, bacterial identification via VITEK 2 compact system were investigated in this study. Gram negative bacteria accounted for 59.15% of the total isolates, while pathogenic gram positive bacteria accounted for 40.85% of total isolates. Escherichia coli and Pseudomonas aeruginosa are the dominant pathogenic gram negative bacteria in wounds, while Staphylococcus aureus, and Staphylococcus epidermidis are the dominant pathogenic gram positive bacteria. Pseudomonas aeruginosa showed 100% resistance to the majority of antibiotic tested, including Ampicillin, Amoxicillin/Clavulanic Acid, Aztreona, Ceftriaxone, and others. Staphylococcus aureus and Staphylococcus epidermidis are 100% resistant to Ampicillin, Ceftriaxone, and Cefotaxime. For more efficient antibiotic prescriptions, the causative microorganisms, and their current susceptibility patterns need to be mandated for testing before prescribing any antibiotics to patients. Prescriptions are frequently based solely on general information about the antibiotic's function, rather than on individual response variation to the pathogen and the antibiotic. Particularly when the common pathogens in this study show multidrug resistance in wounds.


Author(s):  
Satish M. Chavan

Synthesis of novel ethyl 3-amino-5-(methylthio)-4-(5-substituted phenyloxazol-2-yl) thiophene-2-carboxylate derivatives from 3-amino-4-carbamoyl-5-(methylthio)thiophene-2-carboxylate was carried out by traditional as well as microwave irradiation green protocol. Ethyl 3-amino-5-(methylthio)-4-(5-substituted phenyloxazol-2-yl) thiophene-2-carboxylate derivatives were screened for antimicrobial screening against gram positive bacteria Staphylococcus aureus (ATCC 29737), gram negative bacteria Escherichia coli (ATCC 25922), Pseudomonas aeruginosa (ATCC 27853) and Candida albicans (MTCC 277), Aspergillus niger (MCIM 545) fungi.


2013 ◽  
Vol 78 (9) ◽  
pp. 1323-1333 ◽  
Author(s):  
Garima Matela ◽  
Robina Aman ◽  
Chetan Sharma ◽  
Smita Chaudhary

A new series of diisopropyloxytin- and triorganotin(IV) complexes of H2hbgl (1) of the general formula Sn(OPri)2(hbgl) (2), Sn(OPri)2(Hhbgl)2 (3), Ph3Sn(Hhbgl) (4), Bu3Sn(Hhbgl) (5) and Me3Sn(Hhbgl) (6), [where H2hbgl= a ligand of thymol derivative namely, N-(2-hydroxy-3-isopropyl-6-methyl benzyl)Glycine] were synthesized by reacting tin- and triorganotin(IV) chloride with the ligand, with the aid of sodium iso-propoxide in appropriate stiochiometric ratios (1:1 and 1:2). These complexes were characterized by elemental analysis, IR, 1H nuclear magnetic resonance. The spectral data suggest that the carboxylate group, in complexes 2-5, was bonded in a bidentate manner, while a unidentate bonding was observed in complex 6. All five complexes were tested in vitro for their antibacterial activity against Gram-positive bacteria namely, Staphylococcus aureus MTCC 96, Bacillus subtilis MTCC 121 and two Gram-negative bacteria namely, Escherichia coli MTCC 1652 and Pseudomonas aeruginosa MTCC 741. All the five complexes were also tested against three pathogenic fungal strains namely, Aspergillus niger, A. flavus and Penicillium sp.


2017 ◽  
Vol 5 (33) ◽  
pp. 6953-6962 ◽  
Author(s):  
Florent Le Guern ◽  
Tan-Sothea Ouk ◽  
Karine Grenier ◽  
Nicolas Joly ◽  
Vincent Lequart ◽  
...  

Following light irradiation, a new nanomaterial, elaborated from CNCs, chlorin-e6 and polymyxin B, demonstrated efficiency against Gram-negative bacteria (Escherichia coli,Pseudomonas aeruginosa) and Gram-positive bacteria (Staphylococcus aureus,Staphylococcus epidermidis).


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