scholarly journals Novel Structural Hybrids of Pyrrole and Thiazole Moieties: Synthesis and Evaluation of Antibacterial and Antifungal Activities

2021 ◽  
Vol 68 (4) ◽  
pp. 990-996
Author(s):  
Mohamed A. Salem ◽  
Samir Y. Abbas ◽  
Marwa A. M. Sh. El-Sharief ◽  
Mohamed H. Helal ◽  
Moustafa A. Gouda ◽  
...  

One of the best ways to design new biocidal agents is synthesizing hybrid molecules by combining two or more bioactive moieties in a single molecular scaffold. So, new series of pyrroles bearing a thiazole moiety were synthesized using 1-methyl-1H-pyrrole-2-carbaldehyde thiosemicarbazones 1a–c. Cyclization of thiosemicarbazone derivatives 1a–c with ethyl chloroacetate, ethyl 2-chloropropanoate, chloroacetone and phenacyl bromide afforded the corresponding thiazolidin-4-ones 2a–c, 5-methylthiazolidin-4-ones 3a–c, 4-methyl-2,3-dihydrothiazoles 4a–c, and 4-phenyl-2,3-dihydrothiazoles 5a–c, respectively. The antimicrobial activity of the new thiazole derivatives was evaluated.

2016 ◽  
Vol 11 (7) ◽  
pp. 1934578X1601100
Author(s):  
Simona Casiglia ◽  
Maurizio Bruno ◽  
Sergio Rosselli ◽  
Felice Senatore

The chemical composition of the essential oil from flowers of Eringium triquetrum Vahl. collected in Sicily was evaluated by GC and GC-MS. The main components were pulegone (50.6%), piperitenone (30.5%) and menthone (7.0%). Comparison of this oil with other studied oils of Eringium species is discussed. The oil showed good antibacterial and antifungal activities against some microorganisms that infest historical art works.


Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2092 ◽  
Author(s):  
Ibrahim Radini

A novel series of pyrazolyl 1,3,4-thiadiazines 5a–c, 8a–c, 12, 15a–c, 17a–c, and 20 was prepared from the reaction of pyrazole-1-carbothiohydrazide 1a,b with 2-oxo-N′-arylpropanehydrazonoyl chloride, 2-chloro-2-(2-arylhydrazono)acetate, and 3-bromoacetylcoumarin. Moreover, the regioselective reaction of 5-pyrazolone-1-carbothiohydrazide 1a with 4-substituted diazonium salts and 4-(dimethylamino)benzaldehyde gave the corresponding hydrazones 21a–c and 22. The newly prepared compounds were characterized by spectroscopy and elemental analysis. Many new synthesized compounds showed considerable antimicrobial activity against tested microorganisms. Hydrazones 21a–c and 22 showed remarkable antibacterial and antifungal activities. 4-(2-(p-tolyl)hydrazineylidene)-pyrazole-1-carbothiohydrazide 21a displayed the highest antibacterial and antifungal activities with minimum inhibitory concentration (MIC) values lower than standard drugs chloramphenicol and clotrimazole, in the range of 62.5–125 and 2.9–7.8 µg/mL, respectively.


Author(s):  
Dhanapal Venkatachalam ◽  
Samuel Thavamani ◽  
Aneesh C. Sebastian ◽  
V. B. Anju ◽  
Christy Mathew ◽  
...  

Objective: The objective of the study was to evaluate in-vitro efficacy of antibacterial, and antifungal activities of chloroform extract of leaf of Sida cordifolia L. against some human pathogenic bacterial and fungal strains. S. cordifolia (Malvaceae) is used as anti-rheumatic, analgesic, antipyretic, anti-asthmatic, nasal decongestant, antiviral, laxative, diuretic, aphrodisiac, hypoglycemic, hepatoprotective and in the treatment of Parkinson disease. Methodology: Chloroform extract of S.cordifolia was used for antimicrobial screening. Antibacterial activity was tested against pathogenic bacterial strains Eschericha coli and Staphylococcus aureus. Also antifungal activity was tested against one human pathogenic fungal strain i.e. Candida albicans. Antibacterial and antifungal activities of S. cordifolia extract was carried out by using disc diffusion method. Results: Chloroform extract of S. cordifolia showed the largest zone of inhibition (10mm) against S. aureus at 50µgm/mL and no zone of inhibition against E.coli at 50µgm/ml. Chloroform extract has shown more potent antibacterial activity against S.aureus. Chloroform extract was found to be more effective against human pathogenic fungus C. albicuns. The zone of inhibition of chloroform extract was 10mm.The phytochemical screening demonstrated the presence of different types of compounds like alkaloids, tannins and phenolic compounds which may contribute for the anti-microbial action of this plant.  Conclusions: The results concludes that chloroform extract of S. cordifolia leaf possess antimicrobial activity.


2011 ◽  
Vol 6 (9) ◽  
pp. 1934578X1100600
Author(s):  
Soni A. Singh ◽  
Yogesh A. Potdar ◽  
Rasika S. Pawar ◽  
Sujata V. Bhat

Nine conjugated acid derivatives from monoterpene citral have been synthesized using ester, amide condensations, Wittig, Knoevenagel, Baylis-Hillman reactions and their antimicrobial activities were evaluated through disc diffusion and serial dilution methods. Several derivatives displayed interesting antimicrobial activity. Particularly, the Baylis-Hillman adducts 8-10 were found to have more potent antibacterial and antifungal activities than standard drugs namely chloramphenicol and nystatin respectively.


2017 ◽  
Vol 9 (3) ◽  
pp. 297-306 ◽  
Author(s):  
R. Ali ◽  
A. Rahim ◽  
A. Islam

7-Hydroxy-3',4'-methylenedioxy- and 7-benzyloxy-3',4'-methylenedioxy flavanones have been synthesized starting from 2,4-dihydroxyacetophenone. Subsequently biocidal activities of the flavanones have been investigated along with their corresponding chalcones against some bacterial and fungal strains. 2'-Hydroxy-4'-benzyloxy-3,4-methylenedioxy chalcone (5) and its corresponding flavanone (7) showed good antibacterial and antifungal activities against some selected bacterial and fungal strains. On the other hand, 2',4'-dihydroxy-3,4-methylenedioxy chalcone (4) showed no antibacterial and antifungal activities while its corresponding flavanone (6) showed a little antibacterial activity only at higher concentration but did not show antifungal activity. The synthesized chalcones and flavanones have been characterized using UV-Vis, IR and 1H NMRspectral data together with elemental analysis.


2011 ◽  
Vol 61 (2) ◽  
pp. 171-185 ◽  
Author(s):  
Mosaad Mohamed ◽  
Samir Awad ◽  
Naglaa Ahmed

Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivativesA series of 6-aryl-5-cyano-2-thiouracil derivatives (1a-d) was synthesized by the reaction of ethyl cyanoacetate with thiourea and aldehydes. These products were used as intermediate compounds for the synthesis of a number of thiouracil derivatives (2a-dto10a-d). All compounds were screened for antibacterial and antifungal activities. Some of the prepared compounds, 6-(4-fluorophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2a), 4-oxo-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2d), 6-(4-fluorophenyl)-4-hydrazino-2-thioxo-1,2-dihydropyrimidine-5-cabonitrile (7a) and 4-hydrazino-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrimidine-5-carbonitrile (7d) revealed promising antimicrobial activity.


2015 ◽  
Vol 21 (4) ◽  
pp. 191-194 ◽  
Author(s):  
Oussama Cherif ◽  
Fatma Masmoudi ◽  
Fatma Allouche ◽  
Fakher Chabchoub ◽  
Mohamed Trigui

AbstractAn efficient synthesis of new pyrrolopyrimidinones 3a-d and isoxazolopyrimidinones 4a-c from the respective aminocyanopyrroles 1a-d and aminocyanoisoxazoles 2a-c is presented. The synthesized compounds were screened for antimicrobial activity against a panel of bacteria and fungi. Compound 4c exhibits remarkable activity against a broad spectrum of Gram-positive and Gram-negative bacteria and pathogenic fungi.


2012 ◽  
Vol 9 (1) ◽  
pp. 318-322 ◽  
Author(s):  
Bhikan J Khairnar ◽  
Rahul S. Salunke ◽  
Premchand B. Patil ◽  
Sanjay A . Patil ◽  
Rajeshwar J . Kapade ◽  
...  

A series of novel 3- methyl-7-substituted-4H,4-benzothiazine-2-carbohydrazide (3a-e) and corresponding thiosemicarbazides (4-a-q); 2-[3-methyl-7-substituted- 4H-1, 4-benzothiazine-2-yl]-N-(aryl) hydrazine carbothiamide have been synthesized. The thiosemicarbazide when cyclized with iodine via intramolecular cyclisation gave benzothiazonyl oxadiazoles (5-a-q); 5-(3-methyl -7-substitued-4H- 1,4-benzothiazin-2-yl)-N—aryl- 1,3,4- oxadiazol -2-amine and the compounds were tested for antibacterial and antifungal activities against different microorganisms.


2017 ◽  
Vol 16 (2) ◽  
pp. 11-15 ◽  
Author(s):  
Asma Saqib

In recent years, there has been a growing interest in researching and developing new antimicrobial agents from various sources to combat microbial resistance. Apple cider vinegar, otherwise known as cider vinegar or ACV, is a type of vinegar made from cider or apple must and has a pale to medium amber color. Unpasteurized or organic ACV contains mother of vinegar. It has been used for medicinal purpose for thousands of years for its various medicinal properties. The antimicrobial activity of cider vinegar has been recognized but not investigated. It can be used as alternative to commercial antimicrobial agents. The present study aims at finding the antibacterial and antifungal activities of various dilutions of ACV against diverse range of bacteria and fungi to generate data for which little investigation exist.


2008 ◽  
Vol 5 (1) ◽  
pp. 23-33 ◽  
Author(s):  
N. M. Raghavendra ◽  
P. P. Thampi ◽  
P. M. Gurubasavarajaswamy

Several substituted-quinazolin-3(4H)-ones were synthesized by condensation of 2-chloro-N-(4-oxo-substituted-quinazolin-3(4H)-yl)-acetamides with various substituted piperazines through single step reaction. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolin-4-one derivatives were investigated for their antibacterial and antifungal activities.


Sign in / Sign up

Export Citation Format

Share Document