scholarly journals Synthesis and Antimicrobial Activities of 1-((5-Chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide

2021 ◽  
Vol 47 (3) ◽  
pp. 1296-1302
Author(s):  
Oluwaseyi B. Ovonramwen ◽  
Bodunde J. Owolabi ◽  
Abiodun Falodun

A new 1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide was synthesized from methyl-1-[(5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl]pyrrolidine-2-carboxylate and ethylamine. The compound methyl-1-[(5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl]pyrrolidine-2-carboxylate was synthesized from methyl pyrrolidine-2-carboxylate and 5-chloro-4-chlorosulfonyl-1-ethyl-2-methyl-imidazole. The compounds were characterized based on FTIR, 1H, 13C NMR, and DEPT 135 analysis. Antimicrobial activities of the 1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide against Gram-positive (methicillin-susceptible Staphylococcus aureus, methicillin-resistant Staphylococcus aureus, and Bacillus subtilis), Gram-negative (Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae), and Candida albicans were carried out using the standard microbiological method. The newly synthesized 1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide had no activities against the tested organisms. Keywords:    1-((5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl)-N-ethylpyrrolidine-2-carboxamide; methyl-1-[(5-chloro-1-ethyl-2-methyl-1H-imidazol-4-yl)sulfonyl]pyrrolidine-2-carboxylate; L-proline; ethylamine.

Medicina ◽  
2008 ◽  
Vol 44 (12) ◽  
pp. 977 ◽  
Author(s):  
Alvydas Pavilonis ◽  
Algirdas Baranauskas ◽  
Ligita Puidokaitė ◽  
Žaneta Maželienė ◽  
Arūnas Savickas ◽  
...  

Objective. To evaluate the antimicrobial activity of soft and purified propolis extracts. Study object and methods. Antimicrobial activity of soft and purified propolis extracts was determined with reference cultures of Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 33499, Pseudomonas aeruginosa ATCC 27853, Proteus mirabilis ATCC 12459, Bacillus subtilis ATCC 6633, Bacillus cereus ATCC 8035, and fungus Candida albicans ATCC 60193. Microbiological tests were performed under aseptic conditions. Minimum inhibitory concentration (MIC) – the highest dilution of preparation (the lowest concentration of preparation) that suppresses growth of reference microorganisms – was determined. Results. Concentration of phenolic compounds in soft propolis extract that possesses antimicrobial activity against gram-positive (Staphylococcus aureus, Enterococcus faecalis) and gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis) is 0.587±0.054 mg and 0.587±0.054–0.394±0.022 mg (P>0.05) and in purified propolis extract – 0.427±0.044 mg and 0.256±0.02 mg (P>0.05). Klebsiella pneumoniae is most resistant to soft propolis extract when the concentration of phenolic compounds is 1.119± 0.152 mg and to purified propolis extract when the concentration of phenolic compounds is 1.013±0.189 mg (P>0.05). Spore-forming Bacillus subtilis bacteria are more sensitive to soft and purified propolis extracts when the concentration of phenolic compounds is 0.134±0.002 mg and 0.075±0.025 mg, respectively, and Bacillus cereus – when the concentration is 0.394±0.022 mg and 0.256±0.02 mg (P>0.05). Sensitivity of fungus Candida albicans to soft and purified propolis extracts is the same as Bacillus subtilis. Encapsulated bacterium Klebsiella pneumoniae is most resistant to antimicrobial action of soft and purified propolis extracts as compared with gram-positive Staphylococcus aureus and Enterococcus faecalis bacteria (P<0.05), gram-negative Escherichia coli, Pseudomonas aeruginosa, and Proteus mirabilis (P<0.05), sporeforming Bacillus subtilis and Bacillus cereus bacteria (P<0.05), and fungus Candida albicans (P<0.05). There is no statistically significant difference between antimicrobial effect of soft propolis extract and purified propolis extract on gram-positive bacteria, gram-negative bacteria, spore-forming bacteria, encapsulated bacteria, and Candida fungus. Conclusions. Soft and purified propolis extracts possess antimicrobial activity. They could be recommended as natural preservatives in the manufacture of pharmaceutical products.


2012 ◽  
Vol 61 (3) ◽  
pp. 223-225
Author(s):  
MUHAMMAD JAWWAD SAIF ◽  
MOHAMMED ZUBER ◽  
JAMIL ANWAR ◽  
MUNAWAR ALI MUNAWAR

The antimicrobial activity of two new series of bis-piperidinium compounds with alkyl chains of different lengths against bacterial (Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus and Bacillus subtilis) and fungal strains (Aspergillus flavus, Aspergillus niger, Rhodolorula rubera, Lipomyces lopofera and Candida albicans), are described. Antimicrobial activities of the synthesized compounds were compared to that of dodecyltrimethylammonium chloride. Bis-piperidinium salts possessing 12-16 carbon side chains showed better antimicrobial properties as compared to the standard dodecyltrimethylammonium chloride.


Author(s):  
LUCIANA HELENA MAIA PORTE ◽  
MARIA HELENA MIGUEZ ROCHA LEÃO ◽  
ALEXANDRE PORTE

Lactoferrina bovina (bLF), proveniente do soro de leite, foimicroencapsulada pela técnica de spray drying. Microcápsulascontendo 20 % de bLF foram produzidas, utilizando-se comomaterial de parede dextrina: amido octenilsuccinato (OSA) emdiferentes proporções: 100:00, 75:25, 50:50, 25:75 e 0:100 %.Foram avaliadas a cor e a estabilidade de cor das microcápsulassob armazenamento em ambientes com diferentes umidadesrelativas e a atividade antimicrobiana da lactoferrina liberadadas microcápsulas. As microcápsulas apresentaram cor clara etenderam a escurecer sob armazenamento em ambiente com altaumidade relativa. Verifi cou-se atividade inibitória das microcápsulasde bLF produzidas para diferentes bactérias Gram positivas(Bacillus subtilis CCT 2576, Staphylococcus aureus CCT 2740,Micrococcus luteus CCT 2692, Enterococcus faecium CCT 5079,Streptococcus faecium ATCC 10541, Rhodococcus equi CCT0541), Gram negativas (Pseudomonas aeruginosa ATCC 13388,Salmonella choleraesius CCT 4296, Escherichia coli CCT 0547) elevedura (Candida albicans ATCC 10231). A concentração inibitóriamínima (MIC) das microcápsulas variou de acordo com o microorganismotestado (MIC entre 2,5-100 mg.mL-1). Com exceção deB. subtilis (MIC entre 50-100 mg.mL-1 para as microcápsulas), aconcentração de bLF contida nas microcápsulas necessária parainibir o crescimento dos micro-organismos foi menor do que a bLFnativa. Esses resultados sugerem efeito de potencialização daatividade antimicrobiana da bLF após o processamento por spraydrying.


2018 ◽  
Vol 13 (4) ◽  
pp. 1934578X1801300
Author(s):  
Daniyar Sadyrbekov ◽  
Timur Saliev ◽  
Yuri Gatilov ◽  
Ivan Kulakov ◽  
Roza Seidakhmetova ◽  
...  

A cyclopropane derivative of limonene, (1 S, 4 S, 6 R)-7,7-dichloro-4-[(1 S)-2,2-dichloro-1-methylcyclopropyl]-1-methylbicyclo [4.1.0] heptane (compound 2), was synthesized and its structure was determined by NMR and X-ray crystallographic methods. In addition, an antimicrobial activity of the compound against Gram-positive ( Staphylococcus aureus, Bacillus subtilis) and Gram-negative ( Escherichia coli, Pseudomonas aeruginosa) bacterial strains was also scrutinized.


2015 ◽  
Vol 10 (6) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Corina Danciu ◽  
Florin Borcan ◽  
Codruta Soica ◽  
Istvan Zupko ◽  
Erzsébet Csányi ◽  
...  

In recent years polyurethane microstructures (PM) have gained increasing attention in the pharmaceutical field due to the importance of their practical application. Since finding that such a formulation with genistein could improve its applications, we have conducted a preliminary study regarding the in vitro antiproliferative (MCF7, MDA-MB-231 and T47D) and antimicrobial ( Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Salmonella enteritidis (D), Bacillus subtilis, B. cereus, and Candida albicans) activity in order to test whether polyurethane micro structuresre present a good option for further modulation of genistein's bioavailability. It was concluded that the polyurethane micro structures are a bad in vitro partner for the isoflavone genistein.


1994 ◽  
Vol 302 (2) ◽  
pp. 535-538 ◽  
Author(s):  
J Alvarez-Bravo ◽  
S Kurata ◽  
S Natori

Previously, we identified a core undecapeptide of sapecin B having antimicrobial activity. Based on the structure of this peptide, we systematically synthesized peptides consisting of terminal basic motifs and internal oligo-leucine sequences and examined their antimicrobial activities. Of these peptides, RLKLLLLLRLK-NH2 and KLKLLLLLKLK-NH2 were found to have potent microbicidal activity against Staphylococcus aureus, Escherichia coli, methicillin-resistant S. aureus and Candida albicans in liquid medium. We also synthesized the D-enantiomer of KLKLLLLLKLK-NH2. This enantiomer was resistant to tryptic digestion and persisted longer in the culture medium, showing greater antimicrobial activity than the original peptide.


Author(s):  
E. A. Parashchuk ◽  
N. I. Tkachuk ◽  
S. M. Marchyshyn ◽  
H. R. Kozyr

Мета роботи. Визначення антимікробної активності бедринцю ломикаменевого підземних органів екстракту густого. Матеріали і методи.  Oб’єктoм для дoслідження обрано бедринцю ломикаменевого підземних органів екстракт густий (БЕГ-1, одержаний екстрагуванням 75 % етанолом і БЕГ-2, екстрагент 85 % етанол). В якості тест-культур використовували 5 музейних штамів: грампозитивні мікроорганізми Staphylococcus aureus АТСС 6538, спорову культуру Bacillus subtilis АТСС 6633, грамнегативну культуру Escherichia coli АТСС 25922 та Pseudomonas aeruginosa АТСС 9027. Антифунгальну дію з’ясовували відносно Candida albicans АТСС 885-653. Бактеріостатичні властивoсті дoсліджуваних oб’єктів встанoвлювали за результатами росту еталонних штамів мікроорганізмів у нативному водному розчині бедринцю та в розведені 1:2 та 1:4 в м'ясо-пептонному бульйоні; бактерицидні – за відсутністю росту вмісту пробірок із розведенням екстракту на щільних пoживних середoвищах (м’ясо-пептонний агар – МПА) для грампозитивних мікроорганізмів S. aureus, B. subtilis, для грамнегативної культури E. coli, P. аeruginosa. Агар Сабуро використовували для дріжджеподібних грибів роду Candida (C. аlbicans). Результати й обговорення. Бедринцю ломикаменевого підземних органів екстракт густий має широкий спектр антибактеріальної активності. Нативний екстракт БЕГ-1 по відношенню до тест-штамів S. aureus, B. subtilis, C. аlbicans проявляв бактерицидну дію. Бактеріостатичну дію він проявляв до P. aeruginosa, а по відношенню до E. coli антимікробного ефекту не виявлено. Екстракти в розведені 1:2 та 1:4 проявили бактерицидну дію відносно B. subtilis, бактеріостатичну – до S. aureus, C. albicans і не виявлено протимікробної дії до E. coli та P. aeruginosa. Нативний зразок БЕГ-2 по відношенню до усіх досліджуваних 5 тест–штамів проявив бактерицидну активність; у розведені 1:2 та 1:4 проявляв бактерицидну та бактеріостатичну дію відносно S. aureus, B. subtilis, C. albicans. Антимікробна дія по відношенню до E. coli та P. aeruginosa не виявлена. Антимікрoбну активність нативного бедринцю ломикаменевого екстракту густого також вивчали у дoслідах in vitro методом дифузії в агар –  метод “колодязів”. Штами S. aureus, C. albicans, B. subtilis, P. aeruginosa, E. coli проявили чутливість до нативного бедринцю ломикаменевого підземних органів екстракту густого. Грампозитивні бактеріальні штами S. aureus,а також гриби C. albicans, B. subtilis є найбільш чутливими до  БЕГ-2, а БЕГ-1 проявляв порівняно меншу чутливість. Грамнегативні культури P. aeruginosa та E. coli також проявили помірну чутливість до  БЕГ-1, але значно більшу чутливість до БЕГ-2. Висновки. 1. Експериментально встановлено, що обидва досліджувані зразки бедринцю ломикаменевого підземних органів екстракту густого проявляють антибактеріальну активність. 2. Бедринцю ломикаменевого підземних органів екстракт густий проявляв більш виражену антимікробну активність по відношенню до грампозитивної мікрофлори, тому є перспективним для створення лікарського засобу з антимікробними властивостями.


2016 ◽  
Vol 33 (3) ◽  
pp. 140-145
Author(s):  
Mst Laila Akter Banu ◽  
AKM Bashar ◽  
Md Mujibur Rahman Howlader ◽  
Md Shamsul Alam ◽  
Md Ashraf Hussain

Microorganisms, usually from the dental caries, are the main sources of diseases in dental pulp (root canals) and periapical region. Facultative bacteria and fungi have been identified in therapy resistant persistent endodontic infection. The objectives of this study was to evaluate the antimicrobial efficacy of Mineral Tri Oxide Aggregate (MTA) against therapy resistant endodontic microorganisms. The efficacy of MTA was also compared with that of calcium hydroxide. Six standard bacterial stains were used: Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli, bacillus subtilis, Candida albicans and Enterococcus faecalis. The agar diffusion method on Muller- Hilton media was employed. The plates containing media were inoculated with the specified bacterial suspensions. Two standard holes were prepared on each microorganism inoculated plate with a copper puncher and one hole was completely filled with MTA & the other with Ca (OH)2 . The plates were then kept at environmental temperature for one hour to ensure prediffusion and then incubated at 370C for 24 hours. After 24 hours, the diameters of inhibition zones were measured. Tests were replicated for thirty times for each sample and mean values were taken. Zone of inhibition as measured for MTA and Ca (OH)2 were statistically analyzed with Student’s t-Test and Post Hoc Games Howell Test and were presented as mean ± SD to compare of efficacy of MTA and calcium hydroxide on different microorganisms. Both MTA and Ca(OH)2 were found to produce zone of inhibition against Staphylococcus aureus (ATCC 25923), Pseudomonas aeruginosa (ATCC 27853), , Bacillus subtilis (BTCC 17 ), and Candida albicans (BTCC 493). MTA showed highest activity against S. aureus and lowest activity against P. aeruginosa which was similar to the activity range of Ca (OH)2 against the mentioned organisms. But both of them failed to produce any activity against E. coli and. E. faecalis. MTA was found to produce a lower efficacy than Ca (OH)2 while comparing the zone of inhibition between them and statistically it was significant. Mineral Tri Oxide Aggregate (MTA) showed antimicrobial efficacy against some therapy resistant microorganisms but it did not show antimicrobial efficacy against Escherichia coli and Enterococcus faecalis. MTA was found to produce a lower antimicrobial efficacy than Ca (OH)2.J Bangladesh Coll Phys Surg 2015; 33(3): 140-145


2021 ◽  
Vol 10 (9) ◽  
pp. e22610918051
Author(s):  
Soraya Castro Trindade ◽  
Jurandi Nery Pereira-Filho ◽  
Laerte Oliveira Barreto Neto ◽  
Thais Brito de Oliveira Moura ◽  
Antonio Pedro Fróes de Farias ◽  
...  

As espécies do gênero Lippia (Verbenaceae) possuem diversas moléculas bioativas, oriundas do seu metabolismo secundário, que apresentam atividade antimicrobiana, analgésica, antifúngica e imunomoduladora. Este estudo teve como objetivo avaliar a atividade antimicrobiana in vitro do extrato metanólico das folhas de L. alnifolia, L. origanoides, L. insignis e L. thymoides frente a microrganismos de importância clínica.  Foi realizada uma triagem fitoquímica dos extratos das plantas e a avaliação da atividade antimicrobiana pelo método de difusão em disco, além da determinação da concentração inibitória mínima (MIC) frente às bactérias Bacillus subtilis, Escherichia coli, Micrococcus luteus, Pseudomonas aeruginosa, Staphylococcus aureus e Salmonella choleraesuis, e os fungos Candida albicans e Candida glabrata. A presença de saponinas, terpenos, esteroides, cumarinas, ácidos fenólicos e flavonoides foi observada na análise fitoquímica. Os extratos metanólicos das folhas de L. alnifolia, L. origanoides e L. insignis apresentaram atividade antimicrobiana contra todas os microrganismos testados. O extrato metanólico da L. thymoides apresentou atividade antimicrobiana frente aos microrganismos M. luteus, P. aeruginosa, S. aureus, C. albicans e C. glabrata. A maioria dos extratos apresentou atividade bacteriostática e todos os extratos apresentaram atividade fungistática para C. albicans e fungicida para C. glabrata. A utilização dos extratos de Lippia pode ser uma alternativa viável no tratamento de doenças infecciosas de origem bacteriana e fúngica.


Medicina ◽  
2011 ◽  
Vol 47 (3) ◽  
pp. 24 ◽  
Author(s):  
Vilma Jurkštienė ◽  
Alvydas Pavilonis ◽  
Daiva Garšvienė ◽  
Algirdas Juozulynas ◽  
Laimutė Samsonienė ◽  
...  

The aim of the study was to determine antimicrobial activity of rhaponticum and shrubby cinquefoil extracts. Material and Methods. Ethanol extract from the leaves of rhaponticum (Rhaponticum carthamoides D.C. Iljin) and shrubby cinquefoil (Potentilla fruticosa L.) was produced at the Department of Food Technology, Kaunas University of Technology. The antimicrobial activity of the viscous extract or rhaponticum and shrubby cinquefoil was evaluated using standard microorganism cultures (bacteria Staphylococcus aureus ATCC 25923, Enterococcus faecalis ATCC 29212, Escherichia coli ATCC 25922, Klebsiella pneumoniae ATCC 33499, Pseudomonas aeruginosa ATCC 27853, Proteus mirabilis ATCC 12459, Bacillus subtilis ATCC 6633, Bacillus cereus ATCC 8035 and fungi Candida albicans ATCC 60193). The minimum inhibitory concentration (MIC) of the examined preparations was determined. Results. Both studied preparations – rhaponticum (Rhaponticum carthamoides D.C. Iljin) and shrubby cinquefoil (Potentilla fruticosa L.) – demonstrated similar antimicrobial activity. The highest sensitivity to the studied preparations was observed in microbes with eukaryotic cell structure: Candida albicans, which is a fungus, and a spore-forming prokaryotic bacterium, Bacillus cereus. The highest resistance was observed in Escherichia coli and Klebsiella pneumoniae. Conclusions. The studied preparations – viscous extracts of rhaponticum and shrubby cinquefoil – are substances with antimicrobial activity against gram-positive (Staphylococcus aureus and Enterococcus faecalis) and gram-negative (Escherichia coli, Klebsiella pneumoniae, Pseudomonas aeruginosa, and Proteus mirabilis) bacteria, spore-forming bacteria (Bacillus subtilis and Bacillus cereus), and fungi (Candida albicans).


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