scholarly journals Design, Synthesis, and Antimicrobial Activity of Certain New Indole-1,2,4 Triazole Conjugates

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2292
Author(s):  
Reem I. Al-Wabli ◽  
Mona A. Alsulami ◽  
Sarah I. Bukhari ◽  
Nadine M. S. Moubayed ◽  
Maha S. Al-Mutairi ◽  
...  
Keyword(s):  
Inhibition Zone ◽  
Moderate Activity ◽  
Antimicrobial Drugs ◽  
Design Synthesis ◽  
Inhibition Concentration ◽  
Microbial Infections ◽  
New Chemical Entities ◽  
Microbial Strains ◽  
Mic Value

The increasing prevalence of microbial infections and the emergence of resistance to the currently available antimicrobial drugs urged the development of potent new chemical entities with eminent pharmacokinetic and/or pharmacodynamic profiles. Thus, a series of new indole-triazole conjugates 6a-u was designed and synthesized to be assessed as new antimicrobial candidates using the diameter of the inhibition zone and minimum inhibitory concentration assays against certain microbial strains. Their in vitro antibacterial evaluation revealed good to moderate activity against most of the tested Gram-negative strains with diameter of the inhibition zone (DIZ) values in the range of 11–15 mm and minimum inhibition concentration (MIC) values around 250 µg/mL. Meanwhile, their in vitro antifungal evaluation demonstrated a potent activity against Candida tropicalis with MIC value as low as 2 µg/mL for most of the tested compounds. Moreover, compound 6f is the most potent congener with an MIC value of 2 µg/mL against Candida albicans.

scholarly journals Design, synthesis and biological evaluation of novel benzodioxole derivatives as COX inhibitors and cytotoxic agents

BMC Chemistry ◽  
2020 ◽  
Vol 14 (1) ◽  
Author(s):  
Mohammed Hawash ◽  
Nidal Jaradat ◽  
Saba Hameedi ◽  
Ahmed Mousa
Keyword(s):  
Cancer Cell Line ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Cervical Cancer Cell Line ◽  
Moderate Activity ◽  
Selectivity Ratio ◽  
Design Synthesis ◽  
Cox Inhibitors ◽  
Cytotoxic Compound

Abstract Non-steroidal anti-inflammatory drugs are among the most used drugs. They are competitive inhibitors of cyclooxygenase (COX). Twelve novel compounds (aryl acetate and aryl acetic acid groups) were synthesized in this work in order to identify which one was the most potent and which group was most selective towards COX1 and COX2 by using an in vitro COX inhibition assay kit. The cytotoxicity was evaluated for these compounds utilizing MTS assay against cervical carcinoma cells line (HeLa). The synthesized compounds were identified using FTIR, HRMS, 1H-NMR, and 13C-NMR techniques. The results showed that the most potent compound against the COX1 enzyme was 4f with IC50 = 0.725 µM. The compound 3b showed potent activity against both COX1 and COX2 with IC50 = 1.12 and 1.3 µM, respectively, and its selectivity ratio (0.862) was found to be better than Ketoprofen (0.196). In contrast, compound 4d was the most selective with a COX1/COX2 ratio value of 1.809 in comparison with the Ketoprofen ratio. All compounds showed cytotoxic activity against the HeLa Cervical cancer cell line at a higher concentration ranges (0.219–1.94 mM), and the most cytotoxic compound was 3e with a CC50 value of 219 µM. This was tenfold more than its IC50 values of 2.36 and 2.73 µM against COX1 and COX2, respectively. In general, the synthesized library has moderate activity against both enzymes (i.e., COX1 and COX2) and ortho halogenated compounds were more potent than the meta ones.

scholarly journals In vitro antimicrobial susceptibility of Mycoplasma mycoides mycoides large colony and Arcanobacterium pyogenes isolated from clinical cases of ulcerative balanitis and vulvitis in Dorper sheep in South Africa

2005 ◽  
Vol 76 (4) ◽  
Author(s):  
A. Kidanemariam ◽  
J. Gouws ◽  
M. Van Vuuren ◽  
B. Gummow
Keyword(s):  
South Africa ◽  
Inhibition Zone ◽  
Antimicrobial Drugs ◽  
Disk Diffusion Test ◽  
Large Colony ◽  
Mycoplasma Mycoides ◽  
Inhibition Zones ◽  
Arcanobacterium Pyogenes

The in vitro activities of enrofloxacin, florfenicol, oxytetracycline and spiramycin were determined against field isolates of Mycoplasma mycoides mycoides large colony (MmmLC) by means of the broth microdilution technique. The minimum inhibitory concentrations (MICs) of these antimicrobial drugs were determined for a representative number of 10 isolates and 1 type strain. The susceptibility of Arcanobacterium pyogenes to enrofloxacin, oxytetracycline and tilmicosin was determined by means of an agar disk diffusion test. The MICs of enrofloxacin, florfenicol, oxytetracycline and spiramycin were within the ranges of 0.125-0.5, 1.0-2.0, 2.0-4.0 and 4.0-8.0 µg / m , respectively. This study has shown that resistance of MmmLC against enrofloxacin, florfenicol, oxytetracycline and spiramycin was negligible. All the field strains of A. pyogenes that were tested were susceptible to enrofloxacin, oxytetracycline and tilmicosin with mean inhibition zones of 30.6, 42.3 and 35.8mm, respectively. Although there is lack of data on in vivo efficacy and in vitro MIC or inhibition zone diameter breakpoints of these antimicrobial drugs for MmmLC, the MIC results indicate that these 4 classes of antimicrobial drugs should be effective in the treatment of ulcerative balanitis and vulvitis in sheep in South Africa.

scholarly journals Phytochemical and proximate content of Carapa procera bark and its antimicrobial potential against selected pathogens

PLoS ONE ◽  
2021 ◽  
Vol 16 (12) ◽  
pp. e0261755
Author(s):  
Derrick Ansah Owusu ◽  
Alfred Elikem Kwami Afedzi ◽  
Lydia Quansah
Keyword(s):  
Candida Albicans ◽  
Crude Protein ◽  
Inhibition Zone ◽  
Antimicrobial Activities ◽  
Proximate Analysis ◽  
Inhibition Concentration ◽  
Microbial Infections ◽  
Phytochemical Constituents ◽  
Carapa Procera ◽  
Management And Conservation

Medicinal plants represent a great source of antimicrobial and phytochemical constituents which are increasingly used to treat microbial infections and other ailments such as tuberculosis, anemia, and trachoma. Despite the use of antibiotics, antimicrobial resistance continues to be a world issue, in as much as nutrition. This study investigated the presence of phytochemicals, proximate compositions, and antimicrobial activity of methanolic extract of Carapa procera bark. The bark of Carapa procera was collected, cleaned and air dried for 72 h. The powder obtained was treated with diethyl ether and soaked in methanol (99%) for 72 h to obtain crude extract. The extract was used to test for the presence of phytochemicals and antimicrobial activities. The raw bark was used for proximate analysis. The result showed presence of steroids, tannins and saponins, but no alkaloids present. The 100 mg/mL extract had the highest inhibition zone on all tested organisms from 24.00 ± 0.94 to 26.67 ± 1.18, and 50 mg/mL showed the least (16.67 ± 1.24) on Candida albicans. Staphylococcus aureus showed the lowest minimum inhibition concentration (MIC) of 3.12 mg/mL, whereas the Gram-negative bacteria exhibited variations in their sensitivity with E. coli having the highest MIC of 25 mg/mL. The extract had high MIC (6.25 mg/mL) on Candida albicans than clotrimazole (50 mg/mL). The proximate compositions of Carapa procera were moisture (6.07 ± 0.07%), ash (12.46 ± 0.46%), crude protein (9.54 ± 0.12%), crude fat (1.42 ± 0.06%) and carbohydrate (70.50 ± 0.35%). The energy value was 1413.17 kj. Thus, Carapa procera possesses both antimicrobial and nutritional potentials worth exploring and domesticating for sustainable management and conservation.

Novel 2-(5-Aryl)thiophen-2-yl)benzimidazoles; Design, Synthesis and In vitro Evaluation Against Cercarial Phase of Schistosoma mansoni

2020 ◽  
Vol 17 (11) ◽  
pp. 1432-1438
Author(s):  
Serry Atta El Bialy ◽  
Basem Mansour ◽  
Waleed Abdelhakeem Bayoumi ◽  
Amira Taman ◽  
Hassan Mohammed Eissa
Keyword(s):  
Structural Modification ◽  
Anthelmintic Activity ◽  
Ring System ◽  
Literature Survey ◽  
Moderate Activity ◽  
Significant Activity ◽  
Design Synthesis ◽  
Interesting Class ◽  
Low Activity

Background: Literature survey has pointed out that Benzimidazoles represent an interesting class of anthelmintics, of which several potent members were developed. Objective: Benzimidazoles hybridized with pharmacophoric moieties possessing anthelmintic activity were designed, synthesized to be evaluated against cercaria. Methods: Structural modification was achieved through 2- and 5-positions. Moreover, an in vitro cercarial assay was adopted to evaluate target compounds. Results and Discussion: Biological screening revealed that compound 3h showed significant activity with a survival index of 35% at a 100 μg/mL concentration. Whereas, compounds 3a and 3c showed moderate activity, the rest of the tested compounds exhibited low activity. Conclusion: The current study evidenced that the new hybrids "benzimidazole-thiophen-aryl" are successful as cercacidal agents. Further studies of this novel tri-ring system are suggested on adult worms of S. mansoni.

Design, Synthesis and Antibacterial, Antifungal Activity of Some Coumarin Acetohydrazide Derivatives

2021 ◽  
pp. 3931-3937
Author(s):  
A. R. Chabukswar ◽  
P.V. Adsule ◽  
P.B. Randhave ◽  
Manini Mantri
Keyword(s):  
Antifungal Activity ◽  
Moderate Activity ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Design Synthesis ◽  
E Coli ◽  
Gram Positive Bacteria ◽  
Antibacterial And Antifungal ◽  
Gyrase Inhibitors

We have designed and synthesized (Z)-2-(5-methyl-2-oxo-2H-chromen-7-yl) oxy)-N’-(2-oxoindolin-3-ylidin) acetohydrazide derivatives by reacting 7-hydroxy-4-methyl-coumarin and substituted isatin to afford 12 substituted coumarin acetohydrazide derivatives. The synthesized compounds of coumarin acetohydrazide derivatives were designed and evaluated to study for their possible interactions as DNA gyrase inhibitors. All the synthesized coumarin acetohydrazide compounds have been characterized by spectral analysis IR, 1H NMR and mass spectroscopy. The compounds have been evaluated for In vitro antibacterial and antifungal activity against S. aureus, B. subtilus, E. coli, P. aeruginosa and fungi C. albicans and A. niger. In case of Gram positive bacteria and Gram negative bacteria Compound P5C, M5C, C5C exhibited significant activity. Compounds P5N, M5N, C5N shown moderate activity. Compound P5C, M5C, C5C shown significant Antifungal activity against C. albicans and A. niger. Compounds P5C, M5C, C5C are found to exert significant antibacterial as well as antifungal activity and can serve as potential compound against infectious diseases in future.

Oxazolone–1,2,3-Triazole Hybrids: Design, Synthesis and Antimicrobial Evaluation

2018 ◽  
Vol 18 (17) ◽  
pp. 1506-1513 ◽  
Author(s):  
Kashmiri Lal ◽  
Lokesh Kumar ◽  
Ashwani Kumar ◽  
Anil Kumar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Properties ◽  
Dilution Method ◽  
Antimicrobial Drugs ◽  
Activity Data ◽  
Design Synthesis ◽  
Docking Simulations ◽  
Comparable Activity ◽  
Antimicrobial Evaluation

Background: Oxazolones and 1,2,3-triazoles are among the extensively studied heterocycles in medicinal chemistry. Both of these moieties are reported to possess a broad spectrum of biological activity including antimicrobial. Objective: The objective of the current work is to design, synthesize and antimicrobial evaluation of some new oxazolone-1,2,3-triazole hybrids. Methods: The designed oxazolone-1,2,3-triazole hybrids were synthesized using copper(I)-catalyzed azide-alkyne cycloaddition. The antimicrobial evaluation was carried out using serial dilution method. Results: Most of the synthesized hybrids showed significant antimicrobial properties. Some of the compounds were found to be possessing better or comparable activity to that of the standards used. The docking simulations results are also in agreement with the antimicrobial activity data. Conclusion: Sixteen new hybrids were synthesized and tested in vitro for their antimicrobial activity. Some of the tested compounds exhibited promising antimicrobial activity and could be utilized for the development of the lead compounds for new and more potent antimicrobial drugs.

scholarly journals Susceptibility Assessment of Methicillin-Resistant Staphylococcus aureus Strains to Lepidium sativum Extract

Dose-Response ◽  
2019 ◽  
Vol 17 (2) ◽  
pp. 155932581985042
Author(s):  
Amna A. Saddiq ◽  
Azza M. Mohamed
Keyword(s):  
Staphylococcus Aureus ◽  
Methicillin Resistant Staphylococcus Aureus ◽  
Exposure Period ◽  
Inhibition Zone ◽  
Lepidium Sativum ◽  
Susceptibility Assessment ◽  
Methicillin Resistant ◽  
Bacteria Growth ◽  
Microbial Infections

Many plant-derived compounds have been used to treat microbial infections. Staphylococcus aureus a common cause of many organ infections, has generated increasing concern due to its resistance to antibacterial drugs. This work was carried out to explore the susceptibility of 6 strains (LN872136, LN872137, LN871238, LN871239, LN872140, and LN871241) of methicillin-resistant Staphylococcus aureus to aqueous extract of Lepidium sativum seeds in vitro. Various concentrations (5-20 mg/mL) were used to evaluate the effect of the extract on bacteria growth via the assessment of the microbial biomass and the inhibition zone (IZ). The results showed that the plant extract at 15 or 20 mg/mL, significantly decreased the the biomass of S aureus strains after 24 or 48 hours exposure period. Staphylococcus aureus (LN871241) showed the largest IZ at 20 mg/mL and documented by scanning electron microscope. The current work may suggest that L sativum seed extract can be candidate as a promising antimicrobial agent to treat infection with methicillin-resistant S aureus.

scholarly journals The effectiveness of a nonalcoholic disinfectant containing metal ions, with broad antimicrobial activity

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Tokuhiro Matsubara ◽  
Shuichi Maki ◽  
Yukiko Toshimori
Keyword(s):  
Metal Ions ◽  
Patch Test ◽  
Efficacy And Safety ◽  
Safety Test ◽  
Microbial Infections ◽  
Acute Cytotoxicity ◽  
Multiple Cell ◽  
Microbial Strains ◽  
Virucidal Efficacy

AbstractDisinfectants have different efficacies depending on their use and the target microorganism. This study aimed to evaluate the efficacy and safety of our new nonalcoholic disinfectant, which consists mainly of metal ions. According to the 17th revised Japanese Pharmacopoeia and ASTM international E1052 method, the bactericidal and virucidal efficacy of this new disinfectant against 13 microorganisms was evaluated by the in vitro quantitative suspension test. Additionally, the disinfectant cytotoxicity against multiple cell lines was examined. Then, a safety test using a human open patch test was performed with 26 healthy volunteers. This disinfectant showed strong bactericidal and virucidal activities: all microorganisms except enterovirus were inactivated very quickly. The infectivity of 12 microbial strains was eliminated within 5 min of disinfectant exposure. Additionally, this disinfectant showed little acute cytotoxicity in vitro. All volunteers were negative in the human open patch test. Our new disinfectant has a broad spectrum of microbial targets, is safe for human skin, and demonstrates no cytotoxicity. This disinfectant could prevent common microbial infections.

scholarly journals The Effect of Giving Croton Leaf Crude Extract (Codiaeum variegatum) as an Alternative to The Antibacterial of Edwardsiella tarda in Vitro

2021 ◽  
Vol 10 (3) ◽  
pp. 282
Author(s):  
Annisa Isti Fauziyyah ◽  
Arief Prajitno ◽  
Mohammad Fadjar ◽  
Arif Syaifurrisal ◽  
Farid Muchtar Riyadi
Keyword(s):  
Leaf Extract ◽  
Inhibition Zone ◽  
Positive Control ◽  
Edwardsiella Tarda ◽  
Dilution Method ◽  
Bacterial Disease ◽  
Inhibition Concentration ◽  
Codiaeum Variegatum ◽  
Production Problems

Production problems related to aquaculture cannot be separated from diseases that can cause death in fish. Efforts to overcome the bacterial disease Edwardsiella tarda can be done by using natural materials such as the leaves of croton (Codiaeum variegatum). This study aimed to analyze the content of active compounds contained in croton leaf extract which is antibacterial against E. tarda bacteria. Inhibition test was performed by dilution method Minimum Inhibition Concentration (MIC test) and agar diffusion (disc test). The MIC test used five concentrations: 1 mg/L, 10 mg/L, 100 mg/L, 500 mg/L, and 1000 mg/L on Tryptone Soy Broth (TSB) media, while the disc test used five doses of croton leaf extract, namely: A (100 mg/L), B ( 200 mg/L), C (300 mg/L), D (400 mg/L) and E (500 mg/L), 2 controls (positive and negative), and three replications on Tryptone Soy Agar (TSA) media and incubated for 2x24 h. The positive control used chloramphenicol (5 mg/L) antibiotic. Croton leaf extract contains several compounds, namely saponins, flavonoids, tannins, steroids, and polyphenols, which are antibacterial and could kill the test bacteria with the highest average inhibition zone results obtained at a dose of E (500 mg/L) of 6.34 mm, while the lowest results were obtained at dose A (100 mg/L) of 3.12 mm.

scholarly journals Significance and Biological Importance of Pyrimidine in the Microbial World

2014 ◽  
Vol 2014 ◽  
pp. 1-31 ◽  
Author(s):  
Vinita Sharma ◽  
Nitin Chitranshi ◽  
Ajay Kumar Agarwal
Keyword(s):  
Genetic Architecture ◽  
Antimicrobial Agents ◽  
Antimicrobial Activities ◽  
Present Review ◽  
Microbial World ◽  
Adverse Conditions ◽  
Biological Importance ◽  
Microbial Infections ◽  
New Chemical Entities

Microbes are unique creatures that adapt to varying lifestyles and environment resistance in extreme or adverse conditions. The genetic architecture of microbe may bear a significant signature not only in the sequences position, but also in the lifestyle to which it is adapted. It becomes a challenge for the society to find new chemical entities which can treat microbial infections. The present review aims to focus on account of important chemical moiety, that is, pyrimidine and its various derivatives as antimicrobial agents. In the current studies we represent more than 200 pyrimidines as antimicrobial agents with different mono-, di-, tri-, and tetrasubstituted classes along with in vitro antimicrobial activities of pyrimidines derivatives which can facilitate the development of more potent and effective antimicrobial agents.

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