scholarly journals Synthesis, characterization and antimicrobial activity of novel tetrazoles clubbed with pyrimidine

2021 ◽  
Vol 9 (2) ◽  
pp. 116-122
Author(s):  
N.D. Bhoge ◽  
B.K. Magare ◽  
P. B. Mohite
Keyword(s):  
Aromatic Aldehydes ◽  
Oxidative Cyclization ◽  
Good Activity ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Tetrazole Derivatives ◽  
Yield And Purity

An attempt was made to synthesize pyrimidine tetrazole derivatives of pharmaceutical interest by oxidative cyclization of chalcones with adequate yield and purity, prompted by the diversity of their wider usage and the fact that they are an integral part of genetic content. The present work involves the reaction of 5-(2,6-dimethylphenyl)-1H-tetrazole with acetic anhydride to yield 1-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl] ethanone (1) and which then treated with different aromatic aldehydes in presence of alkaline medium to chalcones (2a-f). Reaction of chalcones (2a-f) with urea and thiourea to produce 5-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl]-4-(substituted aryl ) pyrimidin-2-ol (3a-f) and 5-[5-(2,6-dimethylphenyl)-1H-tetrazol-1-yl]-4-(substituted aryl) pyrimidin-2-thiol (4a-f) respectively. All compounds were characterized by infrared spectroscopy (IR), H nuclear magnetic resonance (NMR), and mass spectrometry (MS) to prove the structure and assessed in vitro for their efficacy as antibacterial and antifungal activity against four bacteria. The compounds 3c, 3d and 3f and compounds 4c, 4d and 4f possess very good activity against and E. coli and the compounds 3e, 3c and 3a and compounds 4e,4b and 4c possess very good activity against fungi and .

Substituted 4-Formyl-2H-chromen-2-ones: Their Reaction with N-(2,3,4,6-Tetra-Oacetyl- β-D-galactopyranosyl)thiosemicarbazide, Antibacterial and Antifungal Activity of Their Thiosemicarbazone Products

2020 ◽  
Vol 24 (19) ◽  
pp. 2272-2282
Author(s):  
Vu Ngoc Toan ◽  
Nguyen Minh Tri ◽  
Nguyen Dinh Thanh
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Selenium Dioxide ◽  
Antibacterial And Antifungal Activity ◽  
E Coli ◽  
Antibacterial And Antifungal Activities ◽  
Alkyl Ethers ◽  
Antibacterial And Antifungal

Several 6- and 7-alkoxy-2-oxo-2H-chromene-4-carbaldehydes were prepared from corresponding alkyl ethers of 6- and 7-hydroxy-4-methyl-2-oxo-2H-chromen-2-ones by oxidation using selenium dioxide. 6- and 7-Alkoxy-4-methyl-2H-chromenes were obtained with yields of 57-85%. Corresponding 4-carbaldehyde derivatives were prepared with yields of 41-67%. Thiosemicarbazones of these aldehydes with D-galactose moiety were synthesized by reaction of these aldehydes with N-(2,3,4,6-tetra-O-acetyl-β-Dgalactopyranosyl) thiosemicarbazide with yields of 62-74%. These thiosemicarbazones were screened for their antibacterial and antifungal activities in vitro against bacteria, such as Staphylococcus aureus, Escherichia coli, and fungi, such as Aspergillus niger, Candida albicans. Several compounds exhibited strong inhibitory activity with MIC values of 0.78- 1.56 μM, including 8a (against S. aureus, E. coli, and C. albicans), 8d (against E. coli and A. niger), 9a (against S. aureus), and 9c (against S. aureus and C. albicans).

Synthesis and Evaluation of Novel Fluorobenzimidazole Derivatives as Antibacterial and Antifungal Agents

2019 ◽  
Vol 4 (4) ◽  
pp. 209-215
Author(s):  
D. Joshi ◽  
R. Narigara ◽  
G. Jani ◽  
K. Parikh
Keyword(s):  
Bacterial Strains ◽  
Compound I ◽  
Substituted Anilines ◽  
Gram Negative ◽  
E Coli ◽  
New Class ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Multiple Step

A new class of fluorobenzimidazole derivatives (IIIa-j)was synthesized to investigate their antimicrobial potential. All the compounds were prepared by multiple step synthesis, initiating from the synthesis of 5-(difluoromethoxy)-1H-benzimidazole-2-thiol (I). The compound I was further reacted with different derivatives of 2-chloro-N-phenylacetamide (IIa-j) prepared by reacting differently substituted anilines with chloroacetylchloride and triethylamine in DMF (solvent); resulting in formation of fluorobenzimidazoles IIIa-j. The compounds IIIa-j were characterized by spectral analysis viz. 1H NMR, 13C NMR, mass spectra, elemental analysis and IR. All these compounds were screened in vitro for their antimicrobial activity against Gram-positive (S. aureus and E. faecalis) and Gram-negative bacterial (E. coli and P.aeruginosa) strains as well as fungi (A. niger and C. albicans). Some of the compounds exhibited promising results (in MIC) against Gram-negative bacterial strains.

scholarly journals Design and Synthesis of Some New Derivatives of Chlorobenzyl-Oxy-Phenyl-Ethyl-Thio-1H-Tetrazole and Study Their Antibacterial and Antifungal Activity

2021 ◽  
Author(s):  
Ajay N Ambhore
Keyword(s):  
Antifungal Activity ◽  
Carboxylic Acid ◽  
Spectral Characterization ◽  
Antibacterial And Antifungal Activity ◽  
Design And Synthesis ◽  
Structural Resemblance ◽  
Chemistry Research ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Tetrazole Derivatives

Abstract In recent years tetrazole scaffolds have been attracted interest in the field of synthetic and medicinal chemistry research. The unique structure of the tetrazole derivatives exhibits widespread applications in biology and technology. The close structural resemblance with carboxylic acid acts as a booster of the latter. Due to this diversified potential utilization, several methods are reported for the synthesis of tetrazole scaffolds. Here in this chapter, we describe the synthesis of chlorobenzyl-oxy-phenyl-ethyl-thio-1H-tetrazole derivatives ( 6a-p ). The newly synthesized derivatives are characterized by spectral characterization and screened for their antifungal activity. Among these, some of the newly synthesized compounds show potent antifungal activity.

scholarly journals SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF PYRIMIDINE DERIVATIVES

2019 ◽  
pp. 156-163
Author(s):  
BHAGCHAND JAT ◽  
SWAPNA SANTRA ◽  
PRASANTA KUMAR SANTRA
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
High Performance ◽  
Functional Group ◽  
Analytical Data ◽  
Aromatic Aldehydes ◽  
Antibacterial And Antifungal Activity ◽  
Pyrimidine Derivatives ◽  
Antibacterial And Antifungal

Objectives: Synthesis, characterization, and evaluation of antimicrobial activity of novel pyrimidine derivatives containing O, N, and S in the ring. Methods: Pyrimidine derivatives were prepared in three steps. In the first step, chalcones containing -NO2 functional group were synthesized using Claisen-Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the second step, -NO2 group was reduced to -NH2 group. Resulting compounds containing NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,N-diisopropylethylamine to obtain pyrimidine derivatives.Antibacterial and antifungal activity of pyrimidine derivatives were studied in vitro. Results: Pyrimidine derivatives were synthesized and purified using flash column chromatography. Purity of synthesized pyrimidines was determined by high-performance liquid chromatography. Pyrimidines were characterized by elemental analysis, infrared, nuclear magnetic resonance, and mass spectral analysis. Analytical data of synthesized pyrimidines supported the proposed structures. Significant antibacterial and antifungal activity were observed in the synthesized pyrimidine derivatives. Conclusion: Antibacterial and antifungal activity of the newly synthesized pyrimidine derivatives will definitely inspire future researchers for the preparation of new analogs.

scholarly journals Chemical constituents, in vitro antibacterial and antifungal activity of Mentha×Piperita L. (peppermint) essential oils

2019 ◽  
Vol 31 (4) ◽  
pp. 528-533 ◽  
Author(s):  
Nagarjuna Reddy Desam ◽  
Abdul Jabbar Al-Rajab ◽  
Mukul Sharma ◽  
Mary Moses Mylabathula ◽  
Ramachandra Reddy Gowkanapalli ◽  
...  
Keyword(s):  
Antifungal Activity ◽  
Essential Oils ◽  
Chemical Constituents ◽  
Mentha Piperita ◽  
Antibacterial And Antifungal Activity ◽  
Antibacterial And Antifungal

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.

scholarly journals SYNTHESIS, IN VITRO ANTIOXIDANT AND ANTIMICROBIAL EVALUATION OF 3-HYDROXY CHROMONE DERIVATIVES

2018 ◽  
Vol 11 (3) ◽  
pp. 259
Author(s):  
Pallavi Kamble ◽  
Sailesh Wadher
Keyword(s):  
Antioxidant Activity ◽  
Double Bond ◽  
Antifungal Activity ◽  
Phenolic Hydroxyl ◽  
Hydroxyl Group ◽  
Antibacterial And Antifungal Activity ◽  
Activity Data ◽  
Group 4 ◽  
Antibacterial And Antifungal

 Objective: The objective of the present study was to synthesize a series of 3-hydroxychromone derivatives and to evaluate its in vitro antioxidant and antimicrobial activities.Methods: 3-hydroxy chromones were synthesized using an algar flynn oyamada method which includes oxidative cyclization of 2-hydroxy chalcones in basic solution by hydrogen peroxide. 2-hydroxy chalcones were synthesized by Claisen-Schmidt condensation of substituted 2-hydroxy acetophenones with substituted aromatic aldehydes using polyethylene glycol-400 as a recyclable solvent. The synthesized compounds were evaluated for in vitro antioxidant activity by 1,1-diphenyl-2-picrylhydrazyl radical scavenging assay. In addition, these compounds were also screened for in vitro antibacterial and antifungal activity by agar cup method and Poison plate method, respectively.Results: The structures of the synthesized compounds were characterized by infrared, 1H nuclear magnetic resonance and mass spectroscopy. The antioxidant activity data revealed that all the synthesized derivatives exhibited good activity due to the presence of phenolic hydroxyl group, 4-oxo group and 2,3-double bond. Further, the activity increased with the introduction of a more phenolic hydroxyl group and adjacent methoxy group in the structure. The antimicrobial activity data showed that the compounds possess better antibacterial and antifungal activity which is attributed to the presence of phenolic hydroxyl group and 4-oxo group in the structure.Conclusions: The use of inexpensive, eco-friendly and readily available reagents, easy work-up and high purity of products makes the procedure a convenient and robust method for the synthesis of title compounds. The presence of phenolic hydroxyl group, 4-oxo group, and 2,3-double bond in the structure is responsible for their good antioxidant and antimicrobial activities.

Sign in / Sign up

Export Citation Format

Share Document