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 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 and Antimicrobial Screening of Some Novel 2, 5-Disubstituted 1, 3, 4-oxadiazole Derivatives

2011 ◽  
Vol 8 (s1) ◽  
pp. S149-S154 ◽  
Author(s):  
P. Panneerselvam ◽  
G. Geete Ganesh
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Antibacterial And Antifungal Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
E Coli ◽  
H Nmr ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
New Compounds

The syntheses of series of 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives are described. A total of twelve new compounds were synthesized and characterized by IR,1H-NMR and Mass spectral data. All newly synthesized compounds were screened for their antimicrobial activityi.e. antibacterial activity againstS. aureusandE. coliand antifungal activity against fungusA. nigar. CompoundsG5andG7exhibited significant both antibacterial and antifungal activity whileG2,G10andG3,G9showed antibacterial and antifungal activity respectively. These compounds were 2, 5-disubstituted 1, 3, 4-oxadiazole moiety at position two and five showed reasonable antibacterial and antifungal activity.

scholarly journals Synthesis, Characterization and Antimicrobial Activity of Methylquinolino[3,2-b][1,5]benzodiazepine and Methylquinolino[3,2-b][1,5]benzoxazepine and its Various Metal Complexes

2007 ◽  
Vol 4 (1) ◽  
pp. 32-38 ◽  
Author(s):  
B. Basavaraju ◽  
H. S. Bhojya Naik ◽  
M. C. Prabhakara
Keyword(s):  
Antimicrobial Activity ◽  
Metal Complexes ◽  
Antimicrobial Agents ◽  
Spectral Studies ◽  
Antibacterial And Antifungal Activity ◽  
H Nmr ◽  
Uv Visible ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
Metal Ligand

2-Chloro-6-methylquinoline-3-carbaldehyde was condensed witho-Phenylenediammine and 2-aminophenol in presence of potassium iodide. The resulting Methylquinolino[3,2-b][1,5]benzodiazepine (MQBD) and Methylquinolino[3,2-b][1,5]benzoxazepine(MQBO) were characterized by elemental analysis and spectral studies. The metal chelatesvizPd(II), Rh(III) and Ru(III) of ligands were prepared and characterized by metal-ligand (M:L) ratio, UV-Visible, IR,1H NMR spectroscopes and magnetic properties. The antibacterial and antifungal activity of MQBD, MQBO and its metal complexes were screened against various bacteria and fungi. The results show that all these samples are good antimicrobial agents.

scholarly journals Antimicrobial activity of Hypericum annulatum moris and Hypericum elegans stephan ex willd. essential oils from Serbia

2013 ◽  
Vol 19 (1) ◽  
pp. 7-11
Author(s):  
Aleksandra Djordjevic ◽  
Jelena Lazarevic ◽  
Violeta Mitic ◽  
Radosav Palic ◽  
Gordana Stojanovic
Keyword(s):  
Antimicrobial Activity ◽  
Antifungal Activity ◽  
Essential Oil ◽  
Essential Oils ◽  
Antibacterial And Antifungal Activity ◽  
Significant Difference ◽  
Bacteria And Fungi ◽  
Antibacterial And Antifungal ◽  
Hypericum Species

The in vitro antimicrobial activity of Hypericum annulatum and Hypericum elegans essential oils was evaluated against a panel of standardized bacteria and fungi using broth microdilution assay. Both essential oils showed antimicrobial activity against all the tested microorganisms. Hypericum annulatum essential oil showed better antibacterial than antifungal activity, being more effective against Pseudomonas aeruginosa and Escherichia coli while H. elegans essential oil showed no significant difference between antibacterial and antifungal activity. Antimicrobial testing of ?-pinene, ?-pinene and ?-myrcene compounds was also performed. All the compounds were active against all the tested microorganisms, however, based on the MIC, MBC and MFC values, none of these compounds could be thought of as the main bearer of the oils? antimicrobial activity. This is the first report regarding the antimicrobial activity of the essential oils of the two Hypericum species.

scholarly journals Synthesis and biological activity of 4-thiazolidinone derivatives of phenothiazine

2012 ◽  
Vol 77 (1) ◽  
pp. 17-26 ◽  
Author(s):  
Ritu Sharma ◽  
Pushkal Samadhiya ◽  
Savitri Srivastava ◽  
Santosh Srivastava
Keyword(s):  
Antimicrobial Activity ◽  
Heterocyclic Compounds ◽  
Thioglycolic Acid ◽  
Cycloaddition Reaction ◽  
Aromatic Aldehydes ◽  
Knoevenagel Reaction ◽  
Antituberculosis Activity ◽  
Bacteria And Fungi ◽  
Derivatives Of ◽  
Anhydrous Zncl2

A new series of N-[3-(10H-phenothiazinyl)-propyl]-2-(substituted phenyl)-4-oxo-5-( substituted benzylidene)-1,3-thiazolidine-carboxamide, 5(as) have been synthesized. The cycloaddition reaction of thioglycolic acid with N-[3-(10H-phenothiazinyl)-propyl]-N?-[(substituted phenyl)-methylidene]- urea, 3(a-s) in the presence of anhydrous ZnCl2 afforded new heterocyclic compounds N-[3-(10H-phenothiazinyl)-propyl]-2-(substituted phenyl)-4-oxo- 1,3-thiazolidine-carboxamide, 4(a-s). The later product on treatment with several selected substituted aromatic aldehydes in the presence of C2H5ONa undergoes Knoevenagel reaction to yield 5(a-s). The structure of compounds 1, 2, 3(a-s), 4(a-s) and 5(a-s) were confirmed by IR, 1H NMR, 13C NMR, Fmass and chemical analysis. All above compounds were screened for their antimicrobial activity against some selected bacteria and fungi and for antituberculosis activity compounds have been screened against the bacterium M. tuberculosis.

scholarly journals Synthesis of New Furothiazolo Pyrimido Quinazolinones from Visnagenone or Khellinone and Antimicrobial Activity

Molecules ◽  
2018 ◽  
Vol 23 (11) ◽  
pp. 2793 ◽  
Author(s):  
Ameen Abu-Hashem
Keyword(s):  
Antimicrobial Activity ◽  
Growth Inhibition ◽  
Spectral Data ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Heterocyclic Compounds ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Bacteria And Fungi ◽  
New Compounds

Substituted-6-methyl-1-thioxo-1,2-dihydro-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-ones (5a,b) were synthesized from condensation of visnagenone (2a) or khellinone (2b) with 6-amino-thiouracil (3) in dimethylformamide or refluxing of (4a) or (4b) in dimethylformamide. Hence, compounds (5a,b) were used as the starting materials for preparing many new heterocyclic compounds such as; furo[3,2-g]pyrimido[1,6-a]quinazoline (6a,b), furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazolinone (7a,b), substituted-benzylidene-furo[3,2-g]thiazolo[2′,3′:2,3]pyrimido[1,6-a]quinazoline-3,5-dione (8a–f), 3-oxo-furo[3,2-g]pyrimido[1,6-a]quinazoline-pentane-2,4-dione (9a,b), 1-(pyrazole)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (10a,b), 2-(oxo or thioxo)-pyrimidine-furo[3,2-g]pyrimido[1,6-a]quinazolinone (11a–d), 1-(methylthio)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (12a,b), 1-(methyl-sulfonyl)-furo[3,2-g]pyrimido[1,6-a]quinazolinone (13a,b) and 6-methyl-1-((piperazine) or morpholino)-3H-furo[3,2-g]pyrimido[1,6-a]quinazolin-3-one (14a–d). The structures of the prepared compounds were elucidated on the basis of spectral data (IR, 1H-NMR, 13C-NMR, MS) and elemental analysis. Antimicrobial activity was evaluated for the synthesized compounds against Gram-positive, Gram-negative bacteria and fungi. The new compounds, furothiazolo pyrimido quinazolines 8a–f and 11a–d displayed results excellent for growth inhibition of bacteria and fungi.

scholarly journals Synthesis and Antimicrobial Activity of Some Chalcone Derivatives

2008 ◽  
Vol 5 (3) ◽  
pp. 461-466 ◽  
Author(s):  
Y. Rajendra Prasad ◽  
A. Lakshmana Rao ◽  
R. Rambabu
Keyword(s):  
Aqueous Solution ◽  
Antimicrobial Activity ◽  
Potassium Hydroxide ◽  
Room Temperature ◽  
Antimicrobial Agents ◽  
Aromatic Aldehydes ◽  
Plate Method ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

In an effort to develop antimicrobial agents, a series of chalcones were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehydes in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized compounds were characterized by means of their IR,1H-NMR spectral data and elemental analysis. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.

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.

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