scholarly journals Synthesis, Characterization and Antimicrobial Activity of N-2-(4-Chlorophenyl)acetyl Derivatives of (S)-Amino Acids

2019 ◽  
Vol 32 (2) ◽  
pp. 381-384
Author(s):  
G. Venkateshappa ◽  
P. Raghavendra Kumar ◽  
Krishna2

This paper reports the synthesis, characterization and antibacterial activity of N-2-(4-chlorophenyl)acetyl derivatives of various (S)-amino acids such as (S)-alanine, (S)-phenylalanine, (S)-leucine, (S)-methionine, (S)-proline and (S)-tryptophane. These compounds have been successfully synthesized and their structures were confirmed by 1H NMR and 13C NMR and FT-IR spectroscopy. The antimicrobial activity of these six (S)-amino acids derivatives have been evaluated by the agar well diffusion method against pathogens both Gram-positive (S. aureus) and Gram-negative (K. aerogenes, E. coli and P. desmolyticumas) bacteria and fungi (A. flavus and C. albicans). All these compounds have shown mild to moderate antimicrobial activity.

2019 ◽  
Vol 2019 ◽  
pp. 1-8 ◽  
Author(s):  
Anwar Ali Chandio ◽  
Ayaz Ali Memon ◽  
Shahabuddin Memon ◽  
Fakhar N. Memon ◽  
Qadeer Khan Panhwar ◽  
...  

Present study deals with the synthesis of the p-tert-butylcalix[4]arene diamide derivative as ligand (L) and its Fe3+ complex, followed by its characterization using TLC and FT-IR, while UV-Vis and Job’s plot study were performed for complex formation. Antimicrobial activity of the derivative (L) and its metal complex was carried out by the disc diffusion method against bacteria (Escherichia coli and Staphylococcus albus) and fungi (R. stolonifer). Different concentrations of the derivative (L) (6, 3, 1.5, 0.75, and 0.37 μg/mL) and its Fe3+ complex were prepared, and Mueller–Hinton agar was used as the medium for the growth of microorganisms. Six successive dilutions of the derivative (L) and Fe3+ complex were used against microorganisms. Two successive dilutions (6 and 3 μg/mL) of the derivative (L) showed antibacterial action against both Gram-positive and Gram-negative bacteria. In addition, three successive dilutions (6, 3, and 1.5 μg/mL) of the derivative (L) showed antifungal activity. However, all of six dilutions of the Fe3+ complex showed antimicrobial activity. Derivative (L) showed 3 and 1.5 μg/mL minimum inhibitory concentrations (MIC) against bacteria and fungi, respectively. On the contrary, its Fe3+ complex showed 0.37 μg/mL value of MIC against bacteria and fungi. Hence, Fe3+ complex of the derivative (L) was found to be a more effective antimicrobial agent against selected bacteria and fungi than the diamide derivative (L).


Author(s):  
Chinyere Benardette Chinaka Ikpa ◽  
Uchechukwu C. Okoro ◽  
Collins I. Ubochi ◽  
Kieran O. Nwanorh

The 2-phenylsulphonamide derivatives of amino acids were synthesis by simple substitution of benzenesulphonylchloride (6) with amino acids (1-5) containing pharmacological active functionalities. Structures of the synthesised compounds (7a-7e) were characterised using FT-IR, NMR(1H,13C) and elemental analysis. The anti bacterial activities of the synthesised compounds were evaluated against gram positive bacteria: Staph and Streptococcus, gram negative bacteria: E-coli, Klebsiella, Proteus, and pseudomonas using 200 µl of 10 mg/ml and minimum inhibitory concentration (MIC) were also determined. The compounds exhibited effective anti bacterial properties though some are not more active than the standard drug ciprofloxacin.


2017 ◽  
Vol 8 (1) ◽  
Author(s):  
Vashisht Kiran ◽  
Thakur Vivek ◽  
Kumar Deepak ◽  
Sharma Khemchand

There are many single drug and compound formulations prescribed for Jwara (~ fever) in Ayurvedic classics. Tribhuvanakirti Rasa (TKR), Godanti Bhasma (GB) and Sudarshana Ghana Vati (SGV) are widely used compound formulations that are separately indicated for the treatment of Jwara (~fever) in different dosage schedules. In Ayurvedic Formulary of India Tribhuvana-Mishrana (TM) has been chiefly indicated in treatment of Sarva Jwara (~ fever). Therefore, in this study comparative antimicrobial activity of TM and its individual ingredients viz. TKR, GB and SGV were evaluated against four fever-causing microbes such as gram-positive bacteria Staphylococcus aureus and the gram-negative bacteria Salmonella typhii, Escherichia coli and Pseudomonas aeruginosa. The aqueous extract of all the four samples (formulation as whole and the three individual ingredients separately) in a dose 125mcg/ml were tested for their antimicrobial activity against four different microbes by agar well diffusion method. The study shows that TM and its ingredients independently show significant antimicrobial activity. S. aureus was found to be most sensitive to SGV and moderately sensitive to TKR and TM while S. typhii was found to be most sensitive to TM as compared to others. TKR was found to be most effective against E.coli while SGV and TM both showed significant antimicrobial effect against E. coli. TM could provide an alternative to synthetic antibiotics against human microbial infections.


Author(s):  
Amita Shobha Rao ◽  
Shobha Kl ◽  
Prathibha Md’almeida ◽  
Kiranmai S Rai

  Objective: Infections caused by Gram-negative bacteria are important causes of morbidity and mortality. Extracts of plants and herbs such as Clitorea ternatea are used as diuretic. This work attempts to find out antimicrobial activity of aqueous and alcoholic extract of C. ternatea roots against Pseudomonas aeruginosa (ATCC 27853), Escherichia coli (ATCC 25922), clinical strains of Klebsiella pneumoniae, and Candida albicans.Methods: The agar well-diffusion method was done using Mueller Hinton agar and Sabouraud’s dextrose agar. The microorganism grown in peptone water was inoculated into culture medium. 4 mm diameter well punched into the agar was filled with 20 μl of aqueous and alcoholic root extracts C. ternatea extracts in various concentrations (100-25 μg/ml). The plates were incubated and antimicrobial activity was evaluated.Results: Aqueous root extract of C. ternatea with the concentration of 100 μg/ml showed zone of inhibition against E. coli (ATCC 25922) 18 mm, P. aeruginosa (ATCC 27853) 14 mm, multidrug resistant strain of K. pneumoniae 15 mm. Alcoholic extract of C. ternatea with the concentration of 100 μg/ml showed zone of inhibition of 35 mm against E. coli (ATCC 25922), P. aeruginosa (ATCC 27853) 22 mm, and multidrug resistant strain of K. pneumoniae 28 mm. C. albicanswas resistant to both extract of C. ternatea root. Conclusions: Alcoholic extract of C. ternatea is a better antibacterial agent against multidrug resistant Klebsiella species and other Gram-negative pathogens. Further, studies are required to identify active substances from the alcoholic extracts of C. ternatea for treating infections.


2019 ◽  
Vol 31 (5) ◽  
pp. 1077-1080
Author(s):  
Kottakki Naveen Kumar ◽  
Karteek Rao Amperayani ◽  
V. Ravi Sankar Ummdi ◽  
Uma Devi Parimi

A series 1,2,4-triazole piperine analogues (TP1-TP6) were designed and synthesized. The structures were confirmed using 1H NMR and 13C NMR. Antibacterial study was done using Gram-positive (Staphylococcus aureus and Bacillus cereus) and Gram-negative micro-organisms (E. coli and Pseudomonas aeruginosa) by disc diffusion method. Compound containing chloro substitution (TP6) showed the highest effect, while compound TP1, TP3, TP4, TP5 showed the moderate activity.


2021 ◽  
Vol 14 (4) ◽  
pp. 1730-1736
Author(s):  
Kalpana. P. R

Chitosan, a cationic biopolymer is a major derivative of chitin. It is biocompatible, non-toxic and environ-friendly material and has broad spectrum antimicrobial activity. However, it is less effective in neutral or basic conditions due to its solubility only in acidic medium. Therefore, chemical modification with suitable groups is necessary to enhance the potency of chitosan. The present study was mainly conducted to explore the effect of structural modifications on antimicrobial potential of chitosan. N-Methyl, N-Ethyl and N-Propyl pyrrole were reacted with N-chloroacyl-6-O-triphenylmethylchitosan prepared by stepwise modification of chitosan to form N-Methyl, N-Ethyl and N-Propyl pyrrole derivatives of chitosan. Structural characterization of these pyrrole derivatives was done by IR, NMR, XRD, DSC and Elemental Analysis. The gram-negative bacterium Escherichia coli, gram-positive bacterium Staphylococcus aureus were selected for antibacterial activity and the fungus C. albicans was selected for antifungal activity by agar diffusion method and MIC method. Antimicrobial activity of the N-Methyl, N-Ethyl and N-Propyl pyrrole derivatives on E. coli, S. aureus and C. albicans showed an inhibitory effect on all the organisms. The potency of inhibition was found to be varied with the substitutions. The maximum activity was shown by N-pyrrolylpropylchitosan against E. coli (zone of inhibition 1.2±0.05cm, MIC 0.15±0.03mg/ml), S. aureus (zone of inhibition 1.4±0.03cm, MIC 0.15±0.01mg/ml), C. albicans (zone of inhibition 0.8±0.03cm, MIC 0.2±0.03mg/ml). The study also confirmed that all the three derivatives exhibited higher inhibition than that of chitosan against E. coli (zone of inhibition 0.7±0.03cm, MIC 0.09±0.02mg/ml), S. aureus (zone of inhibition 0.8±0.03cm, MIC 0.09±0.02mg/ml), C. albicans (zone of inhibition 0.6±0.03cm, MIC 0.09±0.03mg/ml). Results demonstrated that these three N-alkylpyrrole chitosan derivatives exhibited improved potency and hence can have the more applicability as antimicrobials.


Author(s):  
G. Venkateshappa ◽  
G. Shivaraju ◽  
P. Raghavendra Kumar

Amino acids play important roles in organisms to sustain in living state and perform as body constituents, enzymes and antibodies. At insalubrious situations, use of amino acids derivatives as drugs in the maintenance of normal health is better choice than common unnatural synthetic drugs. This is due to the fact that the amino acids derivatives may be more bio-compatible, biodegradable and eliminate easily than others.  In this sense we have made an effort and report herein the synthesis of N-{2-(4-chlorophenyl) acetyl} amino alcohols synthesised by reduction of N-{2-(4-chlorophenyl)acetyl} derivatives of (S)-amino acids such as (S)-phenylalanine, (S)-alanine, (S)-methionine, (S)-leucine, (S)-tryptophan and (S)-proline. These newly synthesized amino acids derivatives were analysed by proton, carbon-13 NMR and FT-IR spectroscopy. The composition of solid derivatives was determined by elemental analysis. Further, antimicrobial activities of these derivatives were assessed on usual bacteria K. aerogenes, E. coli, S. aureus and P. desmolyticum and fungi A. flavus and C. albicans. The compounds were witnessed moderate activity than authorised antibacterial and fungal agents Ciprofloxacin and Fluconazole respectively. The antimicrobial studies also revealed that, these derivatives could be better antifungal agents than antibacterial agents. Finally we compared the experimental results of antimicrobial activities with docking studies.  


Author(s):  
Oluwaseun Raphael Aderele ◽  
Adekunle Kareem Rasaq ◽  
Johnson Oshiobugie Momoh

Aim: The study evaluates the in-vitro antimicrobial activity of Hunteria umbellata against Escherichia coli, Staphylococcus aureus and Streptococcus sp. Place and Duration of Study: The study was carried out for three months in 2019 in Biochemistry Laboratory, Department of Chemical Sciences (Biochemistry unit), School of Pure and Applied Sciences, Lagos State Polytechnic, Ikorodu, Lagos- Nigeria. Methodology: The qualitative and GC-MS analysis of Hunteria umbellata methanolic seed extract were determined using standard procedure. The antimicrobial activity was evaluated by the disc diffusion method and agar well diffusion method. The experimental data was resampled 1000 times to allow for higher degrees of freedom in carrying out t-test to test for the difference of the effect of in-vitro antimicrobial activity of H. umbellata against E. coli, S. aureus and Streptococcus sp using mathematical software R language (3.6.1 version). Line plots, histogram and t-test are used to explain the effect of antimicrobial activity of H. umbellate on the selected bacteria. MIC and MBC were determined using standard methods. Results: The Phytochemical analysis of methanolic seed extract of Hunteria umbellata showed the presence of secondary metabolites like saponins, tannins, flavonoids, steroids, phenol among others. GC-MS assay of the H. umbellata seed extract revealed the presence of eight different compounds. Agar well diffusion method was characterized by inhibition zones of 18.36±0.87, 19.13±1.03 and 21.62±2.53 mm for E.coli, S. aureus and Streptococcus sp respectively at 300 mg/ml-1 and 21.70± 1.60, 23.83± 2.64 and 28.57± 1.52 for E.coli, S. aureus and Streptococcus sp respectively at 500 mg/ml. The results of the analysis show that there is a significant difference between the effects of in-vitro antimicrobial activity of H. umbellate on 3001 and 500 mg/ml on each bacteria tested at 5% level of significance. E.coli, S. aureus and Streptococcus sp were tested against 12 standard antimicrobial agents, of which six was sensitive and another six was resistance to E .coli, seven was sensitive, and five was resistance to S. aureus while four was resistance and eight sensitive to Streptococcus sp. The minimum inhibitory concentration (MIC) for E.coli, S. aureus, and  Streptococcus sp were 250, 125 and 31.25 mgml-1 while their minimum bactericidal concentration (MBC) were 500, 250 and 125 respectively. MIC and MBC tests showed that H. umbellata methanolic seed extract had noticeable bactericidal effects with MBC/MIC values ranging between 2 to 4. The extract has strong potency against these microorganisms with Streptococcus sp being the most susceptible. Conclusions: Hunteria umbellata has potential as natural therapeutic agents against E. coli, S. aureus and Streptococcus sp and they may prevent pathogenic diseases.


2021 ◽  
Vol 2021 ◽  
pp. 1-6
Author(s):  
Waseem Akhtar Qureshi ◽  
B. Vivekanandan ◽  
J. Altrin Jayaprasath ◽  
Daoud Ali ◽  
Saud Alarifi ◽  
...  

This investigation reports the use of agrowaste pomegranate peels as an economical source for the production of fluorescent carbon dots (C-dots) and their potential application as an antimicrobial agent. The carbon dots were prepared through low-temperature carbonization at 200°C for 120 min. The obtained C-dots were found to be small in size and exhibited blue luminescence at 350 nm. Further, the synthesized C-dots were characterized with the help of analytical instruments such as DLS, UV-visible, FT-IR, TEM, and fluorescence spectrophotometer. Antimicrobial activity of the C-dot PP was estimated by the agar diffusion method and MIC. S. aureus and K. pneumoniae are showing susceptibility towards C-dot PP when compared to the standard and showing a moderate activity against P. aeruginosa and resistance towards E. coli. The obtained C dot PPs were found to be around 5-9 nm in size confirmed from DLS analysis and supported by TEM. The synthesized C-dots were investigated to understand their microbial efficiency against pathogens and found to have antimicrobial efficiency. These results suggest that pomegranate peels are a potential source of carbon dots with antimicrobial efficiency.


Author(s):  
Shipra Baluja ◽  
Nilesh Godvani ◽  
Sumitra Chanda

In this work, some novel derivatives of Cyanopyridines and Isoxazoles were synthesized using Vilsmeier-Haack reagent and their structures were confirmed by FTIR, 1H NMR and mass spectroscopic methods. The antibacterial activities of these synthesized compounds were studied in DMSO and DMF by agar well diffusion method against some Gram positive and Gram negative bacteria. It is observed that activity depends upon three S: solvent, strain and structure.


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