scholarly journals Review of antibacterial and antifungal activity of 1,2,4-triazole derivatives

2018 ◽  
pp. 63-68
Author(s):  
Т. О. Samura
Keyword(s):  
Antifungal Activity ◽  
Heterocyclic Compounds ◽  
Practical Importance ◽  
Complex Compounds ◽  
Biologically Active ◽  
Alkyl Aryl ◽  
Triazole Derivatives ◽  
Antimicrobial And Antifungal Activity ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Derivatives of 1,2,4-triazole is a very  perspective class of heterocyclic compounds which have high therapeutic effectiveness. The main direction of research on these derivatives are antifungal, antiviral, antibacterial, soothing, hypnotic, anticonvulsant, anti-inflammatory and other activities. The aim was to analyze literature data and generalize recent advances in the study of antimicrobial and antifungal action of 1,2,4-triazole derivatives which can help to create new biologically active substances of this type of activity. Bibliosemantical method, systems thinking and the results of our own research were used in the work. The results of the literature review of antimicrobial and antifungal activity among new alkyl, aryl and heteryl derivatives of 1,2,4-triazole and among complex compounds, which contain 1,2,4-triazole are as ligands were analyzed and systematized. Some dependence of this type of activity on specialty of chemical structure of heterocyclic system derivatives was specified. Perspective of purposeful synthesis of new derivatives of 1,2,4-triazole and products of their transformation as available object for studying biological activity and expanding knowledge about antimicrobial and antifungal activity of this class of heterocyclic compounds were shown with informational analysis. Topicality and practical importance of finding biologically active compounds and receiving biologically active substance by synthesis of new derivatives of 1,2,4-triazole with high antimicrobial activity in relation to gram-negative and gram-positive bacteria were demonstrated.

Copper-catalyzed Convenient Synthesis and SAR Studies of Substituted-1,2,3-triazole as Antimicrobial Agents

2018 ◽  
Vol 16 (1) ◽  
pp. 3-10
Author(s):  
Aniket P. Sarkate ◽  
Kshipra S. Karnik ◽  
Pravin S. Wakte ◽  
Ajinkya P. Sarkate ◽  
Ashwini V. Izankar ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antimicrobial Agents ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
One Pot ◽  
Triazole Derivatives ◽  
Sar Studies ◽  
Convenient Synthesis ◽  
Antibacterial And Antifungal

Background:A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.Objective:We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.Methods:A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.Results and Conclusion:From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.

Chemical modification and Physicochemical properties of new derivatives 5-(thiophen-3-ilmethyl)-4-R1-1,2,4-triazole-3-thiol

2021 ◽  
pp. 4621-4629
Author(s):  
O.A. Bihdan ◽  
V.V. Parchenko
Keyword(s):  
Physicochemical Properties ◽  
High Reactivity ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Triazole Derivatives ◽  
Pharmaceutical Ingredients ◽  
Current Trends ◽  
Wide Range ◽  
Derivatives Of

Current trends in the search for new biologically active compounds among synthetic molecules have arguably proved a priority in studies of the heterocyclic 1,2,4-triazole system. For many years, 1,2,4-triazole derivatives remain the object of close attention of scientists of various scientific fields. The unique properties of 1,2,4-triazole derivatives include high reactivity, which allows different modification of this system, practical absence of toxicity of these derivatives and the presence of a wide range of biological, pharmacological properties, which in the complex provides the prerequisites for the creation of new biologically active compounds, and in the future, active pharmaceutical ingredients (AFI). The aim of our work is to investigate some transformations in a number of derivatives of 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiol, to study the physicochemical properties of the new synthesized compounds. A well-known fact remains the successful attempt of many scientists involved in the study of the heterocyclic 1,2,4-triazole system to synthesize potential biologically active compounds. The process of creating new molecules is very painstaking and requires considerable effort. The chemical approaches for the synthesis of the starting compounds required for further transformations are well known and described. Therefore, we used the corresponding N-R1-2 as intermediates for the synthesis of new 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiols appropriate ones were used N-R1-2-(2-(thiophen-3-yl) acetyl) hydrazinocarbothioamide.

2-Hydroxypropyl derivatives of 1,2,3-thiadiazole and 1,2,3-triazole: Synthesis and antifungal activity

2011 ◽  
Vol 83 (3) ◽  
pp. 715-722 ◽  
Author(s):  
Yury Morzherin ◽  
Polina E. Prokhorova ◽  
Dmitry A. Musikhin ◽  
Tatiana V. Glukhareva ◽  
Zhijin Fan
Keyword(s):  
Mass Spectrometry ◽  
Antifungal Activity ◽  
Ir Spectroscopy ◽  
Elemental Analysis ◽  
Antifungal Activities ◽  
Triazole Derivatives ◽  
New Compounds ◽  
Derivatives Of

A series of novel 5-(2-hydroxypropyl)amino-1,2,3-thiadiazole and 5-(2-hydroxy-propyl)sulfanyl-1,2,3-triazole derivatives were designed and synthesized as candidate fungicides. The new compounds were identified by NMR and IR spectroscopy, mass spectrometry, and elemental analysis. Their antifungal activities were evaluated.

scholarly journals Antimicrobial and antifungal activity of new fluorophenyl-containing 1,2,4-triazoles

2021 ◽  
pp. 87-93
Author(s):  
О. А. Бігдан
Keyword(s):  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Antifungal Activity ◽  
Practical Significance ◽  
Scientific Publications ◽  
Reference Drug ◽  
Minimum Concentration ◽  
Antimicrobial And Antifungal Activity ◽  
Derivatives Of ◽  
Serial Dilutions

The achievements of the world organic chemistry are most clearly represented by scientific publications that prove the promising nature of heterocyclic substances. The possibility of combining various pharmacophore fragments and 1,2,4-triazole in one molecule is quite popular. In 2018, the drug Trifuzol-NEO appeared on the veterinary market of Ukraine, which took its rightful place among synthetic immunomodulators for various groups of unproductive animals. So, further studies of new promising compounds among substituted 1,2,4-triazole, which can be used as objects for the creation of new original domestic antimicrobial and antifungal agents, remains relevant and has theoretical and practical significance. The aim of our work was to investigate the antimicrobial and antifungal activity of a number of new fluorophenyl-containing derivatives of 1,2,4-triazole and, in some cases, to trace the presence of certain patterns between structure and action. The sensitivity of new fluorophenyl-containing derivatives of 1,2.4-triazole was studied by the method of serial dilutions in accordance with the methodological recommendations. From the initial concentration of the new synthesized compounds of 1 mg/ml, a series of two-fold serial dilutions were prepared in Mueller–Hinton broth in a volume of 1 ml. Then, 0.1 ml of microbial curtain (106 m. c./ml) was added to each tube. MIC (MIC) was determined in the absence of visible growth in a test tube with the minimum concentration of the drug, the minimum bactericidal concentration (MBcK) – in the absence of growth on agar after inoculation from transparent tubes. Dimethyl sulfoxide was used as a solvent for the compounds in the studies. The research was carried out at the Department of Microbiology, Virology and Immunology of Zaporizhzhia State Medical University. Analyzing the results of studying the sensitivity of substances to Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, it should be noted that almost all compounds were active against the bacteria. It should be noted that a number of compounds were found to be the most active against Staphylococcus aureus, and 5-(2-fluorophenyl)-4-(((5-nitrofuran-2-yl)methylene)amino-4H-1,2,4-triazole-3-thiols generally exceeded several times the activity indices of the reference drug (MIC 1.95 μg/ml, MBcK 3.9 μg/ml) to Staphylococcus aureus. Most of the compounds were found to be quite active against Candida albicans. Among the corresponding 5-(2-fluorophenyl)-4-((aryl)ylidene)amino-1,2,4-triazole-3-thiols, the highest activity for Candida albicans exhibit 5-(2-fluorophenyl) -4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol and 5-(2-fluorophenyl)-4-((2,3-dimethoxyphenyl)ylidene)amino-1,2,4-triazole-3-thiol. It was found that most of the compounds exhibit a moderate antimicrobial and a fairly high antifungal effect. The most sensitive strain was S. aureus in relation to 5-(2-fluorophenyl)-4-(((5-nitrofurans-2-yl)methylene)amino-4H-1,2,4-triazole-3-thiol, Candida albicans proved to be very sensitive to 5-(2-fluorophenyl)-4-((4-bromophenyl)ylidene)amino-1,2,4-triazole-3-thiol and 5-(2-fluorophenyl)-4((2,3-dimethoxyphenyl)ylidene)amino-1,2,4-triazole-3-thiol.

Dual Acting Isatin-heterocyclic Hybrids: Recent Highlights as Promising Pharmacological Agents

2018 ◽  
Vol 16 (2) ◽  
pp. 220-236 ◽  
Author(s):  
Srinubabu Maddela ◽  
Githa Elizabeth Mathew ◽  
Della Grace Thomas Parambi ◽  
Fakhria Aljoufi ◽  
Bijo Mathew
Keyword(s):  
Single Molecule ◽  
Heterocyclic Compounds ◽  
Structural Modification ◽  
Drug Efficacy ◽  
Biologically Active ◽  
Synergistic Activity ◽  
Pharmacological Activities ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Derivatives Of

Background: For the development of suitable lead molecules to different diseases is a highly challenging task for medicinal chemists. Nowadays, hybrid pharmacophore concept has developed as a useful structural modification tool in the drug design of new drug candidates for different diseases. Hybrid pharmacophore approach consists of combination of two or more pharmacophoric moieties from different biologically active compounds with complementary functions or different mechanisms of action into a single molecule. This often results in synergistic activity or enhanced drug efficacy. Objective: To develop the suitable leads for different diseases there will be a lot of scope to study the substitution of heterocyclic moieties on the different positions of isatin ring. The broad and potent activities of the isatin and their derivatives have been established them as pharmacologically significant scaffolds. In this review, an attempt has been made with specifically emphasizing the hybridization of Isatin with different derivatives of heterocyclic compounds on the different positions of the isatin ring (aryl ring, isatin nitrogen and C2/C3 carbonyl moieties). Conclusion: This review highlighted the recent advances of dual acting isatin-heterocyclic hybrids presenting various pharmacological activities viz., anticancer, antitubercular, anti-inflammatory and antimicrobial.

scholarly journals Design, Synthesis, Antibacterial and Antifungal Activity of Novel 2-[(E)-2-aryl-1-ethenyl]-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4- dihydro-4-quinolinones

2012 ◽  
Vol 9 (3) ◽  
pp. 1481-1489
Author(s):  
Anisetti Ravinder Nath ◽  
Malladi Srinivas Reddy
Keyword(s):  
Antifungal Activity ◽  
Knoevenagel Condensation ◽  
Catalytic Amount ◽  
The Novel ◽  
Plate Method ◽  
Design Synthesis ◽  
H Nmr ◽  
Elemental Analyses ◽  
Antimicrobial And Antifungal Activity ◽  
Antibacterial And Antifungal

The novel 2-[(E)-2-aryl-1-ethenyl]-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4- dihydro-4-quinolinones (4a-j) analogs were synthesized by Knoevenagel condensation of a solution of 2-methyl-3-(2-sulfanyl-1H-benzo[d]imidazole-5-yl)-3,4-dihydro-4-quinazolinone (3) with aromatic aldehyde in presence of catalytic amount of piperidine. Compounds (4a-j) showed significant biological activity against all the standard strains. All the synthesized compounds were characterized on the basis of their IR,1H NMR, MASS spectroscopic data and elemental analyses. All the compounds have been tested for antimicrobial and antifungal activity by the cup-plate method.

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