SYNTHESIS AND EVALUATION OF SOME SUBSTITUTED 2-AMINOTHIAZOLE DERIVATIVES FOR THEIR ANTITUBERCULAR, ANTIMICROBIAL & ANTIFUNGAL ACTIVITY

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (01) ◽  
pp. 24-32
Author(s):  
S. R. Pattan ◽  
◽  
S. H Kale ◽  
R. A. Mali ◽  
S. S. Dengale ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Antitubercular Activity ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Standard Drug ◽  
E Coli ◽  
H Nmr ◽  
Antimicrobial And Antifungal Activity ◽  
Micro Organisms

Millions of people are affected by infectious diseases caused by micro-organisms. Further the widespread microbial resistance had renewed the interest in quest for new antitubercular, antimicrobial & antifungal agents. The present study deals with synthesis & evaluation of some substituted 2-aminothiazole derivatives for their antitubercular, antimicrobial and antifungal activity. 2-aminothiazole derivatives were synthesized by treating substituted acetophenones with thiourea in presence of bromine to give 2-amino 4-substituted phenylthizole and then further treated with chloracetyl chloride to give 2-chloro-N-(4-substituted phenylthizole-2-yl)-acetamide which on refluxing with primary amine gives 15 derivatives. All the synthesized compounds were characterized by IR, H-NMR and elemental analysis.All the synthesized compounds were screened for their antibacterial activity against S. aureus and E. coli by using cup plate agar diffusion method. The activity was measured in terms of zone of inhibition and compared with standard drug ciprofloxacin, sulfonamide. The aminothiazole derivatives were evaluated for antitubercular activity and their result were compared with standard streptomycin.

scholarly journals Screening of Antimicrobial Activity of Various Extracts of the Stem Justicia gendarussa

2019 ◽  
pp. 1-7
Author(s):  
Dhanapal Venkatachalam ◽  
Akhib Rahman ◽  
Basil Sunny ◽  
Jensy Jacob ◽  
Nikhil Kuriyan ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Aqueous Extract ◽  
Antimicrobial Agents ◽  
Pathogenic Fungus ◽  
Hexane Extract ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Standard Drug ◽  
Antibacterial And Antifungal

Objective: The present study was designed to check in-vitro efficacy of Antibacterial and antifungal activity of aqueous and hexane extracts of stem of Justicia gendarussa against selected bacterial and fungal strains. Justicia gendarussa, belonging to the family Acanthaceae, commonly known as ‘‘vatham kolli’ was used in treatment of bronchitis, inflammation, eye diseases, ear ache, vaginal discharges, rheumatism, dysentery, eczema and jaundice. Methodology: Hexane and aqueous extracts of Justicia gendarussa was used for antimicrobial screening. Antibacterial activity was tested against pathogenic bacterial strains Eschericha coli and Staphylococcus aureus. Also antifungal activity was tested against one human pathogenic fungal strain i.e. Candida albicans. Antibacterial and antifungal activities of Justicia gendarussa extract was carried out by using disc diffusion method. Results: Aqueous extract of Justicia gendarussa showed the largest zone of inhibition (5mm) against Eschericha coli, at 50µgm/ml and 3mmzone of inhibition against S. aures, at 50µgm/ml. Hexane extract does not   showing activity against to human pathogenic E. coli and S. aures, at 50µgm/ml. Aqueous extract has shown more potent antibacterial activity against Eschericha coli. Aqueous extract was found to be more effective against human pathogenic fungus Candida albicuns than hexane extract and standard drug. The zone of inhibition of Aqueous extract was 11mm and the zone of inhibition of hexane extract was7mm and standard only 2mm.The phytochemical screening demonstrated the presence of different types of compounds like terpenoids, tannins, and flavonoids which may contribute for the anti-microbial action of this plant. Conclusions: These findings provide scientific evidence of traditional use of Justicia gendarussa and also indicate the potential of this plant for the development of antimicrobial agents.

scholarly journals Production and Screening of Streptomyces-Extracellular Chitinase

2021 ◽  
Vol 2 (4) ◽  
pp. 1-16
Author(s):  
Ibrahim Sani ◽  
Aminu Argungu Umar ◽  
Evelyn Uzoamaka Udeze
Keyword(s):  
Enzyme Activity ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Ammonium Sulphate ◽  
Nitrogen Sources ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Standard Drug ◽  
Significant Difference ◽  
Chitinase Production

The aim of this research was to produce Streptomyces-extracellular chitinase and screen its antifungal activity on a clinically isolated Candida albicans. The Streptomyces were isolated from an agricultural farmland; they were identified and screened for the chitinase production. Effects of time, temperature, pH and nitrogen sources on the chitinase production were determined using standard methods. Ammonium sulphate precipitation was used to partially purify the chitinase. Protein concentrations were determined spectrophotometrically using bovine serum albumin as standard. Agar-well diffusion method was used to evaluate the antifungal activity of the chitinase on C. albicans. The isolated Streptomyces were of three (3) strains, and all the strains are Gram positive, catalase positive, oxidase positive while, Strain A and C are indole positive and only Strain B is citrate positive. The maximum chitinase production was at 72 h, 40°C and when yeast extract was used as the nitrogen source. Ammonium sulphate (80%) precipitation yielded the highest enzyme activity of 39.0U/ml. The maximum enzyme activity was observed at temperature of 40oC, pH 5.5 and 1.0% colloidal chitin (substrate). The partially purified chitinase showed a zone of inhibition of 20.11 ± 1.26 mm against the Candida albicans. This result has no significant difference (P>0.05) when compared with that of the standard drug (Fluconazole) with 21.42 ± 0.08 mm zone of inhibition. These findings suggest that Streptomyces at favourable conditions produce chitinase, and this enzyme can be used as an antifungal agent on Candida albicans and other chitin containing fungi.

scholarly journals SYNTHESIS, ANTIMICROBIAL, ANTITUBERCULAR AND CHEMINFORMATIC STUDIES OF 2-(1-BENZOFURAN-2-YL)-N'-[(3Z)-2-OXO-1, 2-DIHYDRO-3H-INDOL-3-YLIDENE] QUINOLINE-4-CARBOHYDRAZIDE AND ITS DERIVATIVES

2017 ◽  
Vol 9 (5) ◽  
pp. 260 ◽  
Author(s):  
S. Santoshkumar ◽  
N. D. Satyanarayana ◽  
R. Anantacharya ◽  
P. Sameer
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
In Silico ◽  
Antitubercular Activity ◽  
Mean Value ◽  
Diffusion Method ◽  
Pharmacokinetic Parameters ◽  
Moderate Activity ◽  
Significant Activity ◽  
Standard Drug

Objective: Synthesis of novel 2-(1-benzofuran-2-yl)-N'-[(3Z)-2-oxo-1, 2-dihydro-3H-indol-3-ylidene] quinoline-4-carbohydrazide and its derivatives for antimicrobial and antitubercular activity.Methods: Synthesis was carried out using the general method and the structures were confirmed by IR, 1H-NMR, [13]C-NMR and mass spectral analysis. The antibacterial activity was carried by agar well diffusion method, antifungal activity was performed by poison food technique and antitubercular activity was carried out by Microplate Alamar Blue Assay (MABA) method with the help of H37Rv. In silico absorption, distribution, metabolism, excretion, toxicity (ADMET) study of the drug, likeliness was carried out in ACD/lab-2.Results: The results revealed that at 25 mg/ml concentration, compounds 3a and 5a showed good antibacterial activity at 3.5±0.1, 3.8±0.3, 3.6±0.2 respectively against E. coli, K. pneumonia and S. typhimurium, when compared with drug streptomycin with similar concentration. The percentage of inhibition found at 50 µg/ml concentration, compounds 2b and 6a exhibited good antifungal activity at 53±1.15, 57±1.52 against A. flavus and C. neoformans, compared with standard drug fluconazole. The increase in activity was found to be dose dependent. The analogue 2a showed good antitubercular activity at 12.5±0.5 µg/ml, compounds 2b, 3a, 4a-b, 5a-b and 6a-b exhibited significant activity at 25±0.57 µg/ml and compound 3b showed moderate activity at 50±0.57 µg/ml. The mean value of P<0.05 were considered to be statistically significant. The absorption, distribution, metabolism, excretion and toxicity studies of the entitled molecules were analyzed and found to be in acceptable range.Conclusion: The study reveals that compounds containing benzofuran coupled nitrogen heterocycles are essential for activity as they possess excellent drug-like characteristics, suggesting to be potentially best inhibitor of H37Rv strain. The in silico ADME analysis also revealed that all the compounds were in acceptable range to obey the pharmacokinetic parameters.

scholarly journals IN VITRO ANTIMICROBIAL ACTIVITY OF ROOT EXTRACT OF CLITORIA TERNATEA

2017 ◽  
Vol 10 (11) ◽  
pp. 52
Author(s):  
Amita Shobha Rao ◽  
Shobha Kl ◽  
Prathibha Md’almeida ◽  
Kiranmai S Rai
Keyword(s):  
Antimicrobial Activity ◽  
Resistant Strain ◽  
Multidrug Resistant ◽  
Diffusion Method ◽  
Root Extract ◽  
Alcoholic Extract ◽  
Zone Of Inhibition ◽  
Gram Negative ◽  
E Coli ◽  
Multidrug Resistant Strain

  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.

scholarly journals Evaluation of the anti-mycotic activity of Rosemary Oil Against Candida al-bicans

2019 ◽  
Vol 10 (2) ◽  
pp. 1228-1232
Author(s):  
Shebi S ◽  
Geetha RV ◽  
Lakshmi Thangavelu Lakshmi Thangavelu
Keyword(s):  
Antifungal Activity ◽  
Fungal Growth ◽  
Fungal Species ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Disc Diffusion Method ◽  
Rosemary Oil ◽  
Athlete’S Foot ◽  
Systemic Infections ◽  
Sterile Filter

An antifungal medication, also known as an antimycotic medication, is a pharmaceutical fungicide or fungistatic used to treat and prevent mycoses such as athlete's foot, ringworm, candidiasis, serious systemic infections such as Cryptococcal meningitis, and others. In traditional medicine, extracts and essential oil from flowers and leaves are used in the belief they may be useful to treat a variety of fungal disorders. The aim of this study was to analyse the antimycotic properties of rosemary oil and its principal components. The Rosemary oil was screened for antifungal activity by the disc diffusion method. Activated cultures of Candida albicans in Sabouraud’s broth was adjusted to 0.5 McFarland standards [108cfu/ml]. 100 µl of the inoculum was introduced to molten Sabourauds dextrose agar and poured in the sterile Petri plates and allowed to set. Sterile filter paper discs (6.0 mm diameter) impregnated with 25µl, 50µl and 100µl /disc were placed on fungal seeded plates and incubated at 28oC for 48 hrs. Clear zones within which fungal growth was absent were measured and recorded as the diameter (mm) of complete growth inhibition. All the concentrations of the test solution inhibited the fungal species with varying degree of sensitivity. The extract showed good antifungal activity at different concentrations with a maximum zone of inhibition of 38 mm at concentration 100µl. This study provides a sample large enough to determine the antifungal properties of Rosemary oil and suggests further studies for possible therapeutic use.

scholarly journals Antibacterial and Antifungal Activity of Clove Extract (Syzygium Aromaticum): Review

2021 ◽  
Vol 2 (2) ◽  
pp. 93-103
Author(s):  
Nathaniel Hiwandika ◽  
Susana Elya Sudrajat ◽  
Ika Rahayu
Keyword(s):  
Antifungal Activity ◽  
Antifungal Agents ◽  
Ethanolic Extract ◽  
Therapeutic Effects ◽  
Syzygium Aromaticum ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Clove Essential Oil ◽  
Clove Extract ◽  
Antibacterial And Antifungal

Cloves is one of the native Indonesian plants and is used in many aspects of life. Cloves are used in multiple industries and as detergents, soaps, perfumes, food seasonings, aromatherapy, etc. Cloves are mainly used for ingredients in kretek cigarettes in Indonesia. Various studies of cloves reported they have good pharmacological and therapeutic effects. The main compounds of clove extract are eugenol and β-caryophyllene, which are powerful antibacterial and antifungal agents. The clove ethanolic extract showed the activity to inhibit Gram positive and negative bacteria such as B. cereus, S. aureus, E. coli, P. aeruginosa, S. pneumoniae, S. aureus, S. epidermidis, A. hydrophila, K. pneumoniae, P. gingivalis, and P. mirabilis. Clove essential oil has shown the ability to inhibit the growth of V. inaequalis, C. albicans, C. glabrata, and C. tropicalis. Cloves extract can be used as an essential ingredient of various medicines. However, it requires further research and trials.

IN VITRO ANTIMICROBIAL ACTIVITY OF CYNODON DACTYLON (L.) PERS. LEAF EXTRACTS. ANTIMICROBIAL ACTIVITY BY ZONE OF INHIBITION ESTIMATION

INDIAN DRUGS ◽  
2015 ◽  
Vol 52 (04) ◽  
pp. 37-41
Author(s):  
S. M Pawaskar ◽  
◽  
K. C. Sasangan
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Ethyl Acetate ◽  
Petroleum Ether ◽  
Cynodon Dactylon ◽  
Diffusion Method ◽  
Zone Of Inhibition ◽  
Leaf Extracts ◽  
In Vitro Antimicrobial Activity

The present study was undertaken to evaluate in vitro antimicrobial activity of the successive leaf extracts of Cynodon dactylon in petroleum ether, ethyl acetate, acetone, ethanol, methanol and water, against various gram positive & gram negative bacterial strains using zone of inhibition. Both Agar well diffusion method & Agar disc diffusion method were used to evaluate the antibacterial efficacy. The microorganisms used in the test were – Escherichia coli, Proteus vulgaris, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Shigella flexneri, Salmonella typhi, Salmonella paratyphi A, Salmonella paratyphi B, Bacillus subtilis, Streptococcus pyogenes, Vibrio cholerac and Enterobacter aerogenes. Two fungal strains - Candida albicans and Saccharomyces cerevisiae were also tested to evaluate the antifungal potential of the said plant extract. The reference antibiotics chloramphenicol & ampicillin (antibacterial); nystatin & clotrimazole and (antifungal) were also tested against these standard microorganisms used in the assay and the results were compared with that of the plant extracts.The results of the study revealed that all the seven successive extracts of the leaf powder of Cynodon dactylon ( L.) Pers. exhibited prominent antimicrobial and antifungal activity against all microorganisms used in the study. The nonpolar extracts i.e. petroleum ether, ethyl acetate and acetone showed the most significant antibacterial and antifungal activity against all tested organisms. The petroleum ether and ethyl acetate extracts showing maximum inhibition in the range of 8 mm - 15 mm. This was closely followed by, acetone extract, which showed the inhibition in the range of 9 mm - 13 mm.

scholarly journals Synthesis and Antimicrobial Activity of Piperine Analogues Containing 1,2,4-Triazole Ring

2019 ◽  
Vol 31 (5) ◽  
pp. 1077-1080
Author(s):  
Kottakki Naveen Kumar ◽  
Karteek Rao Amperayani ◽  
V. Ravi Sankar Ummdi ◽  
Uma Devi Parimi
Keyword(s):  
Antimicrobial Activity ◽  
Triazole Ring ◽  
Diffusion Method ◽  
Moderate Activity ◽  
Disc Diffusion ◽  
Disc Diffusion Method ◽  
Antibacterial Study ◽  
Gram Negative ◽  
E Coli ◽  
Micro Organisms

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.

scholarly journals Novel 4,6-Disubstituted s-Triazin-2-yl Amino Acid Derivatives as Promising Antifungal Agents

2020 ◽  
Vol 6 (4) ◽  
pp. 237
Author(s):  
Rakia Abd Alhameed ◽  
Zainab Almarhoon ◽  
Essam N. Sholkamy ◽  
Salman Ali Khan ◽  
Zaheer Ul-Haq ◽  
...  
Keyword(s):  
Amino Acid ◽  
Antifungal Activity ◽  
Active Site ◽  
Antifungal Agents ◽  
Docking Studies ◽  
Amino Acid Derivatives ◽  
Active Site Residues ◽  
Standard Drug ◽  
Drug Compounds ◽  
Inhibition Zones

A novel series of 4,6-disubstituted s-triazin-2-yl amino acid derivatives was prepared and characterized. Most of them showed antifungal activity against Candida albicans compared to clotrimazole (standard drug). Compounds bearing aniline derivatives, piperidine and glycine on the triazine core showed the highest inhibition zones at concentrations of 50, 100, 200, and 300 μg per disc. In addition, docking studies revealed that all the compounds accommodated well in the active site residues of N-myristoltransferase (NMT) and exhibited complementarity, which explains the observed antifungal activity. Interestingly, none of these compounds showed antibacterial activity.

scholarly journals Antifungal Activity of the Essential Oil of Echinops kebericho Mesfin: An In Vitro Study

2020 ◽  
Vol 2020 ◽  
pp. 1-7
Author(s):  
Tamirat Bekele Beressa ◽  
Serawit Deyno ◽  
Paul E. Alele
Keyword(s):  
Candida Albicans ◽  
Antifungal Activity ◽  
Essential Oil ◽  
Cryptococcus Neoformans ◽  
Antioxidant Properties ◽  
Pathogenic Fungi ◽  
Diffusion Method ◽  
Potential Candidate ◽  
Standard Drug

Background. Echinops kebericho is an endemic medicinal plant in Ethiopia widely used in the treatment of infectious and noninfectious diseases. Essential oils are known for their antibacterial, antifungal, antiviral, insecticidal, and antioxidant properties. This study evaluated the antifungal activity of essential oil from E. kebericho against four common pathogenic fungi and two standard strains. Methods. The essential oil was obtained by hydrodistillation. The antifungal screening was done by agar well diffusion method. Minimal inhibitory concentrations (MICs) were determined by broth microdilution. Minimal fungicidal concentrations (MFCs) were determined by subculturing fungal strains with no visible growth onto a Sabouraud dextrose agar (SDA) plate. Results. Candida albicans and Cryptococcus neoformans were highly sensitive while Aspergillus flavus did not show sensitivity up to 1 mg/ml of essential oil; MICs ranged from 0.083 mg/ml to 0.208 mg/ml. Concentration and fungal species showed significant dose-dependent associations ( p < 0.0001 ) with antifungal activity. The MICs of essential oil were comparable to those of the standard drug (fluconazole) against C. glabrata and C. krusei. The lowest MFC of the essential oil was observed against Candida parapsilosis (0.145 mg/ml) while the highest MFC was against Candida krusei (0.667 mg/ml). Conclusion. Echinops kebericho essential oil showed noteworthy antifungal activity against Cryptococcus neoformans, Candida albicans, and Candida glabrata and could be a potential candidate for further antifungal drug development.

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