scholarly journals SYNTHESIS AND SCREENING OF BENZOFURAN FUSED C-2,4,6-SUBSTITUTED PYRIMIDINE DERIVATIVES AS A NEW ANTIBACTERIAL AND ANTIFUNGAL AGENT

2017 ◽  
Vol 9 (9) ◽  
pp. 27
Author(s):  
Javarappa Rangaswamy ◽  
Nagaraja Naik
Keyword(s):  
Antimicrobial Activity ◽  
Development Program ◽  
Pyrimidine Ring ◽  
Antibacterial And Antifungal Activity ◽  
Pyrimidine Derivatives ◽  
Pharmacological Activities ◽  
Spectral Techniques ◽  
Wide Range ◽  
Antibacterial And Antifungal ◽  
Drug Development Program

Objective: Benzofuran and their heterocyclic analogs represent an important class of molecules which have a wide range of pharmacological activities. Therefore, in this study synthesis and antimicrobial activity of benzofuran fused C-2,4,6-substituted pyrimidine derivatives was extensively discussed.Methods: Benzofuran fused C-2,4,6-substituted pyrimidine derivatives (4a-k) were built by cyclo condensation, Claisen-Schmidt condensation followed by cyclization via coupling of benzoyl fragments, which include benzofuran, a pyrimidine ring and C-6 substituted phenyl residue with various substituents, connected by linker-S-band. The structures of the synthesized compounds were confirmed by analytical and spectral techniques and evaluated their antimicrobial activity.Results: The results of antibacterial and antifungal activity against various microbes, most of the compounds have shown considerable antimicrobial activity, but compounds 4g and 4e exhibits superior activity compared to standards, this may be due to presence bromo and fluro electron withdrawing substituent on the benzoyl moiety and more lipophilic nature of pyrimidine ring.Conclusion: According to the activity studies, it is observed that the synthesis and antimicrobial activity of benzofuran fused C-2,4,6-substituted pyrimidine derivatives have been shown better antimicrobial activity. The obtained results suggest that these classes of compounds can be considered as new hits for further structural optimization to obtain better antimicrobial drug development program.

scholarly journals SYNTHESIS, CHARACTERIZATION AND ANTIMICROBIAL ACTIVITY OF NOVEL PYRAZOLO[3,4-b]PYRIDINES AND THEIR SPIRO-HETEROCYCLIC DERIVATIVES

2014 ◽  
Vol 10 (7) ◽  
pp. 2901-2915 ◽  
Author(s):  
Shawkat A. Abdelmohsen ◽  
Talaat I El Emary
Keyword(s):  
Antimicrobial Activity ◽  
Aromatic Aldehydes ◽  
Antibacterial And Antifungal Activity ◽  
Pyrimidine Derivatives ◽  
Spiro Derivatives ◽  
Heterocyclic Derivatives ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
New Compounds ◽  
Hydrazone Derivative

The present work describes the synthesis of a novel series of heterocyclic moieties derived from 5-acetylpyrazolo[3,4-b]pyridine (1). The formation of chalcones (2a-d) was utilized to synthesize pyrazoline, isoxazoline and pyrimidine derivatives (3-10). Thiosemicarbazone and semicarbazone (11, 17) were utilized to synthesize other new triazolethiones, thiadiazole and selenadiazole derivatives (11-19). Some new spiro derivatives (22-25) were synthesized by the reaction of chalcone (21) of 1 and isatine with hydrazines, hydroxyl amines and thiourea. Also, The reaction of 1 with cyanoacetyl hydrazine gave the hydrazide-hydrazone derivative 26, which was allowed to react with aromatic aldehydes and α-cyanocinnamonitrile to afford coumarine and substituted pyridine derivatives (28, 29). The structures of all the new compounds have been established on the basis of their analytical and spectral data. Twenty two of the synthesized compounds were also evaluated for their antibacterial and antifungal activity against various strains of bacteria and fungi and most are found to possess promising antimicrobial activity when compared with Chloramphenicol and Clotrimazole

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 Antimicrobial Activity of Skin Secretion of Rana hosii Frog (Anura: Ranidae) against several pathogenic microbes

2020 ◽  
Vol 8 (2) ◽  
pp. 48
Author(s):  
Feskaharny Alamsjah ◽  
Djong Hon Tjong ◽  
Zil Fadhillah Rahma
Keyword(s):  
Antimicrobial Activity ◽  
Inhibition Zone ◽  
Experimental Methods ◽  
Microbiology Laboratory ◽  
Antibacterial And Antifungal Activity ◽  
Skin Secretion ◽  
E Coli ◽  
Skin Secretions ◽  
Pathogenic Microbes ◽  
Antibacterial And Antifungal

The research on antimicrobial activity of skin secretion derived from Rana hosii (Anura: Ranidae) against several pathogenic microbes had been conducted at Microbiology Laboratory and at Genetics and Biomolecular Laboratory, both in the Biology Department, Universitas Andalas. The research used to survey and experimental methods. The study aimed to determine the effectivity of Rana hosii skin secretion to inhibit microbial activity, hence it tested onto some pathogenic microbes such as Escherichia coli, Staphylococcus aureus and Candida albicans. The results showed that the biggest inhibition zone formed against E. coli was 10.96 + 0.63 mm, on S. aureus was 11.74 + 1.00 mm, while on C. albicans was 7.42 + 0.80 mm. The results indicated that the skin secretions from Rana hosii frog could be a potential broad-spectrum antibacterial, and antifungal activity against C. albicans.

scholarly journals Synthesis , spectroscopic characterization and biological study of some new Schiff bases based on 2-hydroxybenzadehyde

2017 ◽  
Vol 13 (2) ◽  
pp. 5995-6005
Author(s):  
S. Abdelnabi ◽  
Chasib K. Bkhakh ◽  
Mouayed Y. Kadhum
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Schiff Bases ◽  
Aromatic Amines ◽  
Spectroscopic Characterization ◽  
Biological Study ◽  
Antibacterial And Antifungal Activity ◽  
Element Analysis ◽  
Antibacterial And Antifungal

Four new Schiff bases were synthesized from condensation of aldehyde ( 2-hydroxy benzaldehyde ) with aromatic amines (4-introaniline ; 4,4-oxydianiline ; 4,4-diaminodipleny sulfone and sulfanilamide) . These Schiff bases were characterized by IR, NMR , GC. mass and element analysis. Moreover, the Schiff bases were screened for their antibacterial and antifungal activity against various microorganisms and compared with standard compounds. In general , the results were indicated that some Schiff bases had good antimicrobial activity.

scholarly journals Lichen Xanthones as Models for New Antifungal Agents

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2617 ◽  
Author(s):  
Diana Resende ◽  
Patrícia Pereira-Terra ◽  
Ângela Inácio ◽  
Paulo Costa ◽  
Eugénia Pinto ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antibacterial Activity ◽  
Fungicidal Activity ◽  
Antifungal Agents ◽  
Multidrug Resistant ◽  
Antimicrobial Compounds ◽  
Pathogenic Microorganisms ◽  
Antibacterial And Antifungal Activity ◽  
Chemistry Research ◽  
Antibacterial And Antifungal

Due to the emergence of multidrug-resistant pathogenic microorganisms, the search for new antimicrobial compounds plays an important role in current medicinal chemistry research. Inspired by lichen antimicrobial xanthones, a series of novel chlorinated xanthones was prepared using five chlorination methods (Methods A–E) to obtain different patterns of substitution in the xanthone scaffold. All the synthesized compounds were evaluated for their antimicrobial activity. Among them, 3-chloro-4,6-dimethoxy-1-methyl-9H-xanthen-9-one 15 showed promising antibacterial activity against E. faecalis (ATCC 29212 and 29213) and S. aureus ATCC 29213. 2,7-Dichloro-3,4,6-trimethoxy-1-methyl-9H-xanthen-9-one 18 revealed a potent fungistatic and fungicidal activity against dermatophytes clinical strains (T. rubrum, M. canis, and E. floccosum (MIC = 4–8 µg/mL)). Moreover, when evaluated for its synergistic effect for T. rubrum, compound 18 exhibited synergy with fluconazole (ΣFIC = 0.289). These results disclosed new hit xanthones for both antibacterial and antifungal activity.

Synthesis, Characterization, Antimicrobial Activity and Theoretical Studies of New Polymeric Schiff-base

2019 ◽  
Vol 41 (4) ◽  
pp. 591-591
Author(s):  
Maha Abid Al Hussain Hameed Maha Abid Al Hussain Hameed ◽  
Maida Abdulaa Adnan Maida Abdulaa Adnan
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Diffusion Method ◽  
Theoretical Studies ◽  
Spectral Techniques ◽  
Ft Ir ◽  
Schiff Base Compound ◽  
Polymeric Schiff Base ◽  
Antibacterial And Antifungal ◽  
Base Compound

A novel Schiff-base compound was synthesized by condensation of 4-hydroxybenzaldehyde and 4-aminoazobenzene. The prepared Schiff-base was converted to a polymer by reaction with formaldehyde and resorcinol. The two types of the prepared compounds were characterized with spectral techniques (FT-IR and 1H-NMR). The biological activity as antibacterial and antifungal was tested using the cork well diffusion method against some standard microorganisms, which indicate that these compounds showed good antimicrobial activity. HyperChem-8 program has been used to determine total energy, LUMO-HOMO, bond length and angles.

IBS Therapeutic has Broad Spectrum Antimicrobial Activity

2021 ◽  
Author(s):  
Ashley L. Cunningham ◽  
Orhi Esarte Palomero ◽  
Bradley J. Voss ◽  
M. Stephen Trent ◽  
Bryan W. Davies
Keyword(s):  
Antimicrobial Activity ◽  
Irritable Bowel Syndrome ◽  
Broad Spectrum ◽  
Enteric Pathogens ◽  
Drug Resistant ◽  
Antibacterial And Antifungal Activity ◽  
Resistant Strains ◽  
Irritable Bowel ◽  
Antibacterial And Antifungal ◽  
Drug Resistant Strains

Otilonium bromide is a poorly absorbed oral medication used to control irritable bowel syndrome. It is thought to act as a muscle relaxant in the intestine. Here we show that otilonium bromide has broad-spectrum antibacterial and antifungal activity, including against multi-drug resistant strains. Our results suggest otilonium bromide could act on enteric pathogens and may offer a new scaffold for poorly absorbed intestinal antimicrobial therapy.

scholarly journals Synthesis and Antimicrobial Activity of Novel Benzoxazoles

2012 ◽  
Vol 67 (9-10) ◽  
pp. 466-472 ◽  
Author(s):  
Mustafa Arisoy ◽  
Ozlem Temiz-Arpaci ◽  
Fatma Kaynak-Onurdag ◽  
Selda Ozgen
Keyword(s):  
Antimicrobial Activity ◽  
Inhibitory Concentration ◽  
Antimicrobial Activities ◽  
Microbial Pathogens ◽  
Drug Resistant ◽  
Dilution Technique ◽  
Spectral Techniques ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
New Compounds

A series of 2-(p-substituted-benzyl)-5-[[4-(p-chloro/fluoro-phenyl)piperazin-1-yl]ace tamido] -benzoxazoles were synthesized in need of new compounds for the fight against microbial pathogens. Their structures were elucidated by spectral techniques. These new derivatives, along with previously synthesized 2-(p-substituted-benzyl)-5-substituted-benzoxazoles, were evaluated for their antibacterial and antifungal activities against standard strains and drugresistant isolates in comparison with ampicillin, gentamicin sulfate, ofloxacin, vancomycin, fluconazole, and amphotericin B trihydrate. The minimum inhibitory concentration (MIC) of each compound was determined by a two-fold serial dilution technique. The compounds were found to possess a broad spectrum of antimicrobial activities with MIC values of 32 - 256 μg/ml. Although standard drugs were more active against the pathogenes employed in this study, the activities of the new benzoxazoles and reference drugs against drug-resistant isolates of the microorganisms were largely similar

Bioactive Chemical Constituents and Comparative Antimicrobial Activity of Callus Culture and Adult Plant Extracts from Alternanthera tenella

2009 ◽  
Vol 64 (5-6) ◽  
pp. 373-381 ◽  
Author(s):  
Marcos J. Salvador ◽  
Paulo S. Pereira ◽  
Suzelei C. França ◽  
Regina C. Candido ◽  
Izabel Y. Ito ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Callus Culture ◽  
Culture Media ◽  
Chemical Constituents ◽  
Adult Plant ◽  
Antibacterial And Antifungal Activity ◽  
Crude Extracts ◽  
Antibacterial And Antifungal ◽  
Adult Plants

Crude extracts of a callus culture (two culture media) and adult plants (two collections) from Alternanthera tenella Colla (Amaranthaceae) were evaluated for their antibacterial and antifungal activity, in order to investigate the maintenance of antimicrobial activity of the extracts obtained from plants in vivo and in vitro. The antibacterial and antifungal activity was determined against thirty strains of microorganisms including Gram-positive and Gram-negative bacteria, yeasts and dermatophytes. Ethanolic and hexanic extracts of adult plants collected during the same period of the years 1997 and 2002 [Ribeirão Preto (SP), collections 1 and 2] and obtained from plant cell callus culture in two different hormonal media (AtT43 and AtT11) inhibited the growth of bacteria, yeasts and dermatophytes with inhibition halos between 6 and 20 mm. For the crude extracts of adult plants bioassay-guided fractionation, purification, and isolation were performed by chromatographic methods, and the structures of the isolated compounds were established by analysis of chemical and spectral evidences (UV, IR, NMR and ES-MS). Steroids, saponins and flavonoids (aglycones and C-glycosides) were isolated. The minimum inhibitory concentration (MIC) of the isolated compounds varied from 50 to 500 μg/mL

scholarly journals Antimicrobial Activity of Oleanolic and Ursolic Acids: An Update

2015 ◽  
Vol 2015 ◽  
pp. 1-14 ◽  
Author(s):  
Jéssica A. Jesus ◽  
João Henrique G. Lago ◽  
Márcia D. Laurenti ◽  
Eduardo S. Yamamoto ◽  
Luiz Felipe D. Passero
Keyword(s):  
Antimicrobial Activity ◽  
Animal Health ◽  
Mechanisms Of Action ◽  
Human Pathogens ◽  
Future Perspectives ◽  
Pharmacological Activities ◽  
Long Period ◽  
Wide Range ◽  
Potential Use

Triterpenoids are the most representative group of phytochemicals, as they comprise more than 20,000 recognized molecules. These compounds are biosynthesized in plants via squalene cyclization, a C30hydrocarbon that is considered to be the precursor of all steroids. Due to their low hydrophilicity, triterpenes were considered to be inactive for a long period of time; however, evidence regarding their wide range of pharmacological activities is emerging, and elegant studies have highlighted these activities. Several triterpenic skeletons have been described, including some that have presented with pentacyclic features, such as oleanolic and ursolic acids. These compounds have displayed incontestable biological activity, such as antibacterial, antiviral, and antiprotozoal effects, which were not included in a single review until now. Thus, the present review investigates the potential use of these triterpenes against human pathogens, including their mechanisms of action, viain vivostudies, and the future perspectives about the use of compounds for human or even animal health are also discussed.

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