Synthesis and preliminary biological evaluation of antibacterial and antifungal 5‐arylidene tetramic acid‐cadmium(II) complexes

2021 ◽  
Author(s):  
Dimitris Matiadis ◽  
Valentina Stefanou ◽  
Dimitrios Tsironis ◽  
Angeliki Panagiotopoulou ◽  
Olga Igglessi‐Markopoulou ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Tetramic Acid ◽  
Antibacterial And Antifungal

Novel Thiazole-Based Thiazolidinones as Potent Anti-infective Agents: In silico PASS and Toxicity Prediction, Synthesis, Biological Evaluation and Molecular Modelling

2020 ◽  
Vol 23 (2) ◽  
pp. 126-140 ◽  
Author(s):  
Christophe Tratrat
Keyword(s):  
In Silico ◽  
Antimicrobial Agents ◽  
Target Identification ◽  
Biological Evaluation ◽  
Microbial Infection ◽  
Toxicity Prediction ◽  
Discovery Studio ◽  
Bacteria And Fungi ◽  
Multiple Drugs ◽  
Antibacterial And Antifungal

Aims and Objective: The infectious disease treatment remains a challenging concern owing to the increasing number of pathogenic microorganisms associated with resistance to multiple drugs. A promising approach for combating microbial infection is to combine two or more known bioactive heterocyclic pharmacophores in one molecular platform. Herein, the synthesis and biological evaluation of novel thiazole-thiazolidinone hybrids as potential antimicrobial agents were dissimilated. Materials and Methods: The preparation of the substituted 5-benzylidene-2-thiazolyimino-4- thiazolidinones was achieved in three steps from 2-amino-5-methylthiazoline. All the compounds have been screened in PASS antibacterial activity prediction and in a panel of bacteria and fungi strains. Minimum inhibitory concentration and minimum bacterial concentration were both determined by microdilution assays. Molecular modeling was conducted using Accelrys Discovery Studio 4.0 client. ToxPredict (OPEN TOX) and ProTox were used to estimate the toxicity of the title compounds. Results: PASS prediction revealed the potentiality antibacterial property of the designed thiazolethiazolidinone hybrids. All tested compounds were found to kill and to inhibit the growth of a vast variety of bacteria and fungi, and were more potent than the commercial drugs, streptomycin, ampicillin, bifomazole and ketoconazole. Further, in silico study was carried out for prospective molecular target identification and revealed favorable interaction with the target enzymes E. coli MurB and CYP51B of Aspergillus fumigatus. Toxicity prediction revealed that none of the active compounds was found toxic. Conclusion: Substituted 5-benzylidene-2-thiazolyimino-4-thiazolidinones, endowing remarkable antibacterial and antifungal properties, were identified as a novel class of antimicrobial agents and may find a potential therapeutic use to eradicate infectious diseases.

scholarly journals Synthesis, spectral studies and biological activity of 2, 3-disubstituted imidazo [2, 1-b] benzothiazole derivatives

2018 ◽  
Vol 6 (01) ◽  
pp. 01-08
Author(s):  
Yashveer Singh ◽  
Baljeet Kaur ◽  
Amandeep Kaur ◽  
Vivek Kumar Gupta ◽  
Monika Gupta
Keyword(s):  
Antimicrobial Activity ◽  
Catalytic Domain ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Thiazole Ring ◽  
Standard Drug ◽  
Atp Binding Site ◽  
Benzothiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

Benzothiazole is a heterocyclic compound formed by the fusion of benzene and thiazole ring. The moiety had been reported to act via competing with ATP binding site at the catalytic domain of tyrosine kinase. The present work involves the synthesis and biological evaluation of 4, 5 disubstituted imidazo [2, 1-b] benzothiazole derivatives. The antimicrobial activity of the synthesized derivatives was carried out against Gram + ve bacteria Staphylococcus aureus (MTCC 3160) and Gram –ve bacteria Bordetella bronchiseptica (MTCC 6838), Pseudomonas aeruginosa (T11) and fungal strains Candida albicans (MTCC 1637). Ciprofloxacin and Fluconazole were used as standard drug for antibacterial and antifungal activity respectively. The compounds 6a1, 6a2, 6a3, 6b1 and 8a1 exhibited good antimicrobial activity against all the strains. The derivative 8a1 was further screened for anticancer activity against MCF-7 cell line using Doxorubicin as standard. The structures of the synthesized compounds were established by IR and NMR spectral studies.

scholarly journals Chemistry and Biological Evaluation of Some New Triazolopyrimidine Derivatives Containing Isopropyl Group

2019 ◽  
pp. 390-396
Author(s):  
Janaki H. Chauhan ◽  
Haresh K. Ram
Keyword(s):  
Antifungal Activity ◽  
1H Nmr ◽  
Biological Evaluation ◽  
Spectroscopic Techniques ◽  
Efficient Synthesis ◽  
Antibacterial And Antifungal Activity ◽  
Isopropyl Group ◽  
Elemental Analyses ◽  
Antibacterial And Antifungal

An efficient Synthesis of a novel series of N,7-bis(substitutedphenyl)-4,7-dihydro-5-isopropyl-[1,2,4]triazolo-[1,5-a]pyrimidine-6-carboxamide (4a-j) was accomplished from N-(substituedphenyl)-4-methyl-3-oxopentanamide, 3-amino-1,2,4-triazole and different aldehyde reflex 20 min with DMF and then after the cooling product was obtained. All the recently synthesized compounds were characterized by the Mass, IR, 1H-NMR and mass spectroscopic techniques and by elemental analyses. The newly synthesized compounds were assessed for their antibacterial and antifungal activity.

Synthesis and Biological evaluation of some newer Pyrazole Derivatives

2021 ◽  
pp. 6304-6308
Author(s):  
Ajay Sharma ◽  
Gyanendra Kumar Sharma ◽  
Himansu Chopra
Keyword(s):  
Biological Evaluation ◽  
Pyrazole Derivatives ◽  
Wide Scope ◽  
Phenyl Hydrazine ◽  
Carbon Particles ◽  
Ongoing Work ◽  
Definition Of ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation ◽  
Heterocyclic Moiety

Pyrazoline is a 5-membered heterocyclic moiety has two adjoining nitrogen iotas and three carbon particles inside the ring. Pyrazoline subordinate are related wide scope of pharmacological and restorative exercises, for example, antibacterial, antifungal, pain relieving, calming, hostile to parasitic, against malarial, against oxidant. The ongoing work of exploration is fundamentally engaged at the revelation and improvement of a progression of 1,3,5-trisubstituted pyrazoline. A progression of new 1-phenyl-3-(4-nitrophenyl)- 5-(subbed phenyl) pyrazoline subordinates (2a-2j) were blended by the response of subbed acetophenone and subbed benzaldehyde within the sight of fluid sodium hydroxide arrangement by Claisen Schmidt buildup system. The subbed chalcone were integrated which is additionally dense with phenyl hydrazine in ethanol and results in the definition of conclusive subordinates of pyrazoline (2a-2j). The response blend was observed by TLC and the last mixes were refined by recrystallization from wanted dissolvable. All the structures of blended mixes were affirmed by FTIR, 1H NMR, mass unearthly information and essential investigation. All the recently combined mixes (2a-2j) were assessed for antibacterial and antifungal movement. Mixes 2f, 2i and 2h showed powerful inhibitory impact against on strains of both bacterial and parasitic species.

scholarly journals Biological evaluation of some octanoyl derivatives of methyl 4,6-O-cyclohexylidene-α-D-glucopyranoside

2013 ◽  
pp. 53-64 ◽  
Author(s):  
Abul KMS Kabir ◽  
Sarkar MA Kawsar ◽  
Mohammad MR Bhuiyan ◽  
Md Safiqur Rahman ◽  
Bilkiss Banu
Keyword(s):  
Pathogenic Bacteria ◽  
Biological Evaluation ◽  
Phytopathogenic Fungi ◽  
Bacterial Strains ◽  
Antibacterial And Antifungal Activities ◽  
Inhibition Concentration ◽  
Fungal Phytopathogens ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Some acylated derivatives of methyl 4,6-O-cyclohexylidene-?-D-glucopyranoside, including the precursor, were employed as test compounds for in vitro antimicrobial functionality test against ten human pathogenic bacteria and six phytopathogenic fungi. For comparative studies, biological activity of standard antibiotics, Ampicillin and Nystatin were also carried out against these microorganisms. The study revealed that the tested samples exhibited moderate to good antibacterial and antifungal activities. It was also observed that the test substances were more effective against fungal phytopathogens than those of the bacterial strains. Encouragingly, a good number of test compounds exhibited better antimicrobial activity than the standard antibiotics employed. Minimum Inhibition Concentration (MIC) test of methyl 4,6-O-cyclohexylidene-3-Odecanoyl- 2-O-octanoyl-?-D-glucopyranoside was conducted against INABA ET (Vibrio) and MIC was found to be 12.5 ?g/disc. DOI: http://dx.doi.org/10.3329/cujbs.v3i1.13406 The Chittagong Univ. J. B. Sci.,Vol. 3(1&2):53-64, 2008

scholarly journals Synthesis and Antimicrobial Activity of New Derivatives of Angular Polycyclic Phenoxazine Ring System

2019 ◽  
Vol 35 (4) ◽  
pp. 1320-1326
Author(s):  
Mercy Amarachukwu Ezeokonkwo ◽  
Kingsley Chizoba Iloka ◽  
Uchechukwu Chris Okoro ◽  
Efeturi Abreham Onoabedje ◽  
Benjamin Ebere Ezema ◽  
...  
Keyword(s):  
Mass Spectra ◽  
Antifungal Agents ◽  
Salmonella Typhi ◽  
Biological Evaluation ◽  
Ring System ◽  
Klebsiella Pneumonia ◽  
Streptococcus Pneumonia ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Synthesis of angular polycyclic phenoxazine derivatives incorporating different phenols is reported in 30-99% yields. O-arylation of 6-chlorodibenzo[a,j] phenoxazin-5-one with a variety of electron-deficient, electron-neutral and electron-rich phenols under the catalytic palladium (II) acetate/t-BuXphos system furnished the compounds of interest. The highest yields were obtained when the intermediate was coupled with electron-rich phenols. IR, 1H-NMR, 13C-NMR and Mass spectra data, confirmed the structures of all the synthesized compounds. Study on the in vitro biological evaluation of the compounds against microorganisms revealed that they are potent antibacterial and antifungal agents, as they showed significant biological activity against Staphylococcus aureus, Streptococcus pneumonia, Escherichia coli, Salmonella typhi, klebsiella pneumonia, Pseudomonas aeruginasa, Basillus substilis, Candida albicans and Aspergillus niger.

scholarly journals Synthesis and Biological Evaluation of 2-(3-Methyl-2-oxoquinoxalin-1(2H)-yl)-N'-(substituted phenyl-methyledene/ethylidene)acetohydrazides

2010 ◽  
Vol 7 (4) ◽  
pp. 1435-1439 ◽  
Author(s):  
Gopal Krishna Rao ◽  
R. B. Kotnal ◽  
P. N. Sanjay Pai
Keyword(s):  
Antimicrobial Activity ◽  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Antibacterial And Antifungal Activities ◽  
Quinoxaline Derivatives ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

A series of quinoxaline derivatives was prepared and evaluated for antitubercular, antibacterial and antifungal activities. The title compounds were prepared by condensation of substituted aromatic aldehydes and substituted acetophenones with 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl) acetohydrazide. Structures of all these compounds were confirmed by their spectral studies. Among synthesized compounds (4r, 4t, 4u, 4wand4x) have shown good anti tubercular activity (25 µg mL-1) when compared to reference drugs pyrazinamide (10 µg mL-1) and streptomycin (7.5 µg mL-1). In this study, few derivatives showed broad spectrum of antimicrobial activity at low concentration. The MICs (Minimum inhibitory concentration) of some compounds are 2-4 µg mL-1.

scholarly journals Total Synthesis and Biological Evaluation of the Tetramic Acid Based Natural Product Harzianic Acid and Its Stereoisomers

2015 ◽  
Vol 17 (3) ◽  
pp. 692-695 ◽  
Author(s):  
Alan R. Healy ◽  
Francesco Vinale ◽  
Matteo Lorito ◽  
Nicholas J. Westwood
Keyword(s):  
Total Synthesis ◽  
Natural Product ◽  
Biological Evaluation ◽  
Tetramic Acid ◽  
Synthesis And Biological Evaluation
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