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1.
Synthesis and Antimicrobial Activity of Some New N‐substituted‐5‐arylidene‐thiazolidine‐2,4‐diones
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Anca Stana Brînduşa Tiperciuc Mihaela Duma Laurian Vlase Ovidiu Crişan Adrian Pîrnău Ovidiu Oniga 《Journal of heterocyclic chemistry》2014,51(2):411-417
A total of 17 new N‐substituted derivatives ( 2b , 2c , 2d , 2e , 2f , 2g , 2h , 2i , 2j , 2k and 3b , 3c , 3d , 3e , 3f , 3g , 3h ) of 5‐((2‐phenylthiazol‐4‐yl)methylene) thiazolidine‐2,4‐dione ( 2a ) and 5‐(2,6‐dichloro‐ benzylidene)thiazolidine‐2,4‐dione ( 3a ) were synthesized. The structural elucidation of the newly synthesized compounds was based on elemental analysis and spectroscopic data (MS, 1H NMR, 13C NMR), and their antimicrobial activities were assessed in vitro against several strains of Gram‐positive and Gram‐negative bacteria and one fungal strain (Candida albicans) as growth inhibition diameter. Some of them showed modest to good antibacterial activity against Gram‐negative Escherichia coli and Salmonella typhimurium and Gram‐positive Staphylococcus aureus, Bacillus cereus, and Enterococcus fecalis bacterial strains, whereas almost all the compounds were inactive against Listeria monocytogenes. All of the synthesized compounds showed moderate to very good activity against C. albicans. 相似文献
2.
《Journal of heterocyclic chemistry》2017,54(2):1619-1624
A series of 1,2‐dihydroquinoxaline‐3‐yl‐3‐substitutedphenyl‐1H‐pyrazole‐4‐carbaldehyde were synthesized and evaluated for their antimicrobial activity against two Gram‐positive and two Gram‐negative organisms and two fungal organisms. The study has shown that pyrazole‐4‐carbaldehyde‐incorporated quinoxaline was essential for activity. Among the compounds, 5a , 5c , 5d had shown significant activity against all selected strains when compared with control. These compounds may prove useful as antimicrobial agents. 相似文献
3.
Ali Aminkhani Mina Talati Roholah Sharifi Firouzeh Chalabian Fatemeh Katouzian 《Journal of heterocyclic chemistry》2019,56(6):1812-1819
A remarkably efficient three‐component reaction to synthesize 2‐amino‐4H‐chromenes derivatives from malononitrile, various aromatic aldehydes, and orcinol was described at room temperature in CH2Cl2 in the presence of catalytic amount of triethylamine. In a facile one‐pot procedure, excellent yields of products were achieved in less than 1 h. Some of the synthesized 2‐amino‐4H‐chromenes derivatives demonstrated potent antibacterial activities against Gram‐positive bacteria including Staphylococcus aureus and Bacillus anthracis, indicated by disk method, minimum inhibitory concentration, and minimum bactericidal concentration approaches. However, none of the tested compounds expressed any antibacterial activities against Enterococcus faecalis and Gram‐negative bacteria. 相似文献
4.
《Journal of heterocyclic chemistry》2017,54(6):3208-3219
Imidazo[4,5‐c ]pyrazole derivatives ( 3a–f , 4a–f , and 5a–f ) were efficiently synthesized by one‐pot three‐component reactions using CeO2–MgO as the catalyst. The synthesized compounds were characterized by IR, 1H NMR, 13C NMR, and mass spectroscopic analyses. The in vitro antimicrobial activity of the synthesized compounds against various bacterial and fungal strains was screened. Compound 3b was highly active [minimum inhibitory concentration (MIC): 0.5 μg/mL] against Gram‐positive Staphylococcus aureus , and compounds 3b , 3f , 4d , and 4e were highly active (MIC: 0.5, 2, 2, and 0.5 μg/mL, respectively) against Gram‐negative Pseudomonas aeruginosa and Klebsiella pneumoniae , relative to standard ciprofloxacin in the antibacterial activity screening. Compounds 3b and 4f were highly active (MIC: 4 and 0.5 μg/mL, respectively) against Aspergillus fumigatus and Microsporum audouinii in the antifungal activity screening compared with the clotrimazole standard. 相似文献
5.
Vikas Shinde Pravin C. Mhaske Aakriti Singh Dhiman Sarkar Pramod Mahulikar 《Journal of heterocyclic chemistry》2019,56(11):3093-3101
A novel series of 4‐(4‐(1‐benzyl‐1H‐1,2,3‐triazol‐4‐yl)phenyl)‐2‐substitutedthiazole derivatives ( 8a‐l) have been synthesized by [3 + 2] cycloaddition reaction of 4‐(4‐ethynylphenyl)‐2‐substitutedthiazole with substituted benzyl azide in aqueous DMF. Starting compounds 4‐(4‐ethynylphenyl)‐2‐substitutedthiazole ( 6a‐d ) were synthesized by reaction of 4‐(2‐substitutedthiazol‐4‐yl)benzaldehyde with Ohira‐Bestmann reagent in methanol. The structures of these novel triazole‐thiazole clubbed derivatives were confirmed by the spectral analysis. The title compounds ( 8a‐l ) were tested for antimycobacterial activity against Mycobacterium tuberculosis H37Ra active and dormant (MTB, ATCC 25177) and antimicrobial activity against standard Gram‐positive bacteria, Staphylococcus aureus (NCIM 2602) and Bacillus subtilis (NCIM 2162), and Gram‐negative bacteria, Escherichia coli (NCIM 2576) and Pseudomonas flurescence (NCIM 2059). Compounds 8a , 8b , 8c , and 8h reported good activity against B subtilis, compounds 8a , 8b , and 8c showed good activity against S aureus, and compound 8b showed good activity against dormant M tuberculosis H37Rv strain. Compounds 8b and 8c found more potent against Gram positive and dormant M tuberculosis H37Rv strains. These novel triazole‐thiazole clubbed analogues found to be a capable leads for further optimization and development. 相似文献
6.
Mallikarjun Reddy Sura Vasu Govardhana Reddy Peddiahgari Rajendra Prasad Reddy Bhoomireddy Rama Krishna Vadde 《Journal of heterocyclic chemistry》2013,50(6):1395-1399
A new series of 2,4‐diaryl‐6‐methyl‐5‐nitropyrimidines ( 5a , 5b , 5c , 5d , 5e , 5f , 5g , 5h , 5i ) were synthesized in good yields by Suzuki–Miyaura coupling of 2,4‐dichloro‐6‐methyl‐5‐nitropyrimidine ( 3 ) with various aryl boronic esters ( 4a , 4b , 4c , 4d , 4e , 4f , 4g , 4h , 4i ) in the presence of 1,1′‐ bis(diphenylphosphino)ferrocene dichloropalladium(II) (Pd(dppf)2Cl2). Further, antibacterial and antioxidant properties were screened for the title compounds 5a , 5b , 5c , 5d , 5e , 5f , 5g , 5h , 5i . Most of the compounds possessed significant activity against Gram‐positive bacteria Staphylococcus aureus and Bacillus subtilis and Gram‐negative bacteria Escherichia coli and Klebsiella pneumoniae. The antioxidant activity of the title compounds showed significant antioxidant activity when compared with vitamin C. 相似文献
7.
Disperse Dyes Based on 5‐Arylazo‐thiazol‐2‐ylcarbamoyl‐thiophenes: Synthesis,Antimicrobial Activity and Their Application on Polyester
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A series of novel 5‐arylazo‐thiazol‐2‐ylcarbamoyl‐thiophene derivatives was synthesized, and their chemical structures were secured by elemental and spectroscopic analyses. Their versatility for pharmaceutical purposes and textile dyeing as disperse dyes were reported. The synthesized dyes were applied to polyester fabrics by using high temperature dyeing method at 130°C. The dyed polyester fabrics displayed very good washing and perspiration fastness and moderate light fastness. Finally, the synthesized compounds showed biological activities against Bacillus subtilis, Staphylococcus aureus (Gram positive bacteria), Escherichia coli, and Pseudomonas aeruginosa (Gram‐negative bacteria), while no effect had been reported against fungi. The minimum inhibitory concentration of the most active compound was evaluated. 相似文献
8.
Gülay Akyüz Fatih aban Beri Bahittin Kahveci Emre Mentee 《Journal of heterocyclic chemistry》2019,56(11):3065-3072
A new series of quinazolinones containing hydrazone moiety were synthesized, and their inhibitory activities on urease were assessed in vitro. Most of the compounds exhibited potent urease inhibitory activity. Among the synthesized compounds, molecule 4a bearing furan ring has the best inhibitory effect against urease with IC50 = 2.90 ± 0.11 μg/mL. Compounds 4f , 4g , 4h , 4i , and 4j have hydroxy group on phenyl ring. Compound 4i is the most active inhibitor among these compounds with IC50 = 5.01 ± 0.10 μg/mL, which has 3‐Cl and 4‐Br on phenyl ring. Also, newly synthesized compounds had been tested for their antimicrobial effects against three of Gram‐positive bacteria (Bacillus cereus 702 Roma, Staphylococcus aureus ATCC 25923, and Streptococcus pyogenes ATCC 19615) and three of Gram‐negative bacteria (Escherichia coli ATCC 25922, Proteus vulgaris ATCC 13315, and Pseudomonas aeruginosa ATCC 27853). Antimicrobial activity results show that compounds 4a , 4h , 4j , 4f , and 4l have the lowest minimum inhibitory concentration (MIC) value of 1000 μg/mL to all tested bacteria. The other compounds have the MIC value of >1000 μg/mL to all tested bacteria. 相似文献
9.
Synthesis,Characterization, and Biological Evaluation of Some Tri‐Substituted Imidazole/thiazole Derivatives
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A novel compound series of tri‐substituted imidazole/thiazole derivatives ( 3a , 3b , 3c , 3d , 3e , 3f , 3g , 3h , 3i ) were prepared by Radziszewski reaction. Benzil ( 1 ), ammonium acetate or ammonium thiocynate, and 1‐phenyl‐3‐(p‐substituted phenyl)‐1H‐pyrazole‐4‐carbaldehyde ( 2a , 2b , 2c , 2d , 2e , 2f , 2g ) were reacted to give the desired product. Synthesized compounds were characterized by elemental analysis (CHNS) and spectral analysis (FTIR, 1H and 13C FT NMR, and LC–MS). All the compounds were screened for their antibacterial, antifungal, and antimycobacterial activities. Antimicrobial activity was evaluated against some bacterial strains such as Escherichia coli (MTCC 443), Pseudomonas aeruginosa (MTCC 1688), Staphylococcus aureus (MTCC 96), Streptococcus pyogenes (MTCC 442), and the H37Rv strain of Mycobacterium tuberculosis, and the fungal activity was observed against strains, for example, Candida albicans (MTCC 227), Aspergillus niger (MTCC 282), and Aspergillus clavatus (MTCC 1323). All the synthesized compounds were found to possess moderate to excellent activity against the above selected strains. 相似文献
10.
Synthesis and Antimicrobial Activities of Novel Series of 3‐(4‐(2‐substituted thiazol‐4‐yl)phenyl)‐2‐(4‐methyl‐2‐substituted thiazol‐5‐yl)thiazolidin‐4‐one Derivatives
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Shivaji H. Shelke Pravin C. Mhaske Sachin Narkhade Vivek D. Bobade 《Journal of heterocyclic chemistry》2014,51(4):1151-1156
In the present investigation, a novel series of 3‐(4‐(2‐substituted thiazol‐4‐yl)phenyl)‐2‐(4‐methyl‐2‐substituted thiazol‐5‐yl)thiazolidin‐4‐one derivatives were synthesized by condensation of 2‐substituted‐4‐methylthiazole‐5‐carbaldehyde with 4‐(2‐substituted thiazol‐4‐yl)benzenamine followed by cyclo‐condensation with thioglycolic acid in toluene. All the newly synthesized compounds were characterized by spectral (IR, 1H NMR, 13C NMR, and Mass) methods. The title compounds were screened for quantitative antibacterial activity (minimal inhibitory concentration). All compounds 7a , 7b , 7c , 7d , 7e , 7f , 7g , 7h and 8a , 8b , 8c , 8d , 8e , 8f , 8g , 8h show moderate to good antimicrobial activity, whereas compounds ( 7a , 7b , 7c , 7d , 7e , 7f , 7g , 7h ) also show moderate antifungal activity. 相似文献
11.
Domenico Armenise Nicolino De Laurentis Antonio Rosato Flaviano Morlacchi 《Journal of heterocyclic chemistry》2006,43(5):1371-1378
12.
Synthesis and Antimicrobial Activities of Novel 2‐[substituted‐1H‐pyrazol‐4‐yl] Benzothiazoles,Benzoxazoles, and Benzimidazoles
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Vikas S. Padalkar Bhushan N. Borse Vinod D. Gupta Kiran R. Phatangare Vikas S. Patil Nagaian Sekar 《Journal of heterocyclic chemistry》2016,53(5):1347-1355
In an endeavor to find a new class of antimicrobial agents, a series of novel substituted benzimidazole, benzoxazole, and benzothiazole derivatives 6 containing pyrazole moiety have been synthesized by reaction of 3‐aryl‐4‐formyl pyrazole 4 with substituted phenylenediamine or o‐aminophenol or o‐aminothiophenol 5 . Reaction of phenyl hydrazine or 2‐hydrazinopyridine 1 with substituted acetophenones 2 gave the corresponding hydrazones 3 , which on Vilsmeier–Haack reaction with POCl3–DMF gave substituted 3‐aryl‐4‐formyl pyrazoles 4 . All final compounds 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j , 6k were evaluated for in vitro antibacterial activities against Escherichia coli and Staphylococcus aureus strains and in vitro antifungal activity against Candida albicans and Aspergillus niger strains by using serial dilution method. The antimicrobial activities were expressed as the minimum inhibitory concentration in µg/mL. The compound containing benzimidazole and benzoxazole moiety gave better antibacterial and antifungal activities than benzothiazole compounds. 相似文献
13.
Malath A. Al‐Qtaitat Mustafa M. El‐Abadelah Salim S. Sabri Suzan A. Matar Hana M. Hammad Mohammad S. Mubarak 《Journal of heterocyclic chemistry》2019,56(1):158-164
A number of novel bicinnolines containing piperazine moieties, 4a – o , were synthesized via polyphosphoric acid‐catalyzed intramolecular cyclization of the respective acyl amidrazone derivatives ( 3a – o ). On the other hand, the amidrazones ( 3a – o ) were prepared by reaction of N′,N″‐(biphenyl‐4,4′‐diyl)bis(2‐oxopropane hydrazonoyl chloride) ( 2 ) with the appropriate cyclic sec‐amines in the presence of trimethylamine in absolute ethanol. Structures of the newly synthesized compounds were confirmed by NMR and mass spectral data. The antitumor activity of compounds 4a – o was evaluated in vitro on human breast cancer MDA‐231 by a cell viability assay. Results revealed that compounds 4k , 4n , and 4o exhibit potential cytotoxic effects (>70%) on the cancer cells. Additionally, the antimicrobial activity of compounds 4a – o was evaluated against three clinical microbial strains: Escherichia coli (Gram‐negative bacteria), Staphylococcus aureus (Gram‐positive bacteria), and Candida albicans (fungi/yeast). Results revealed that compounds 4e and 4k exhibit good activity against all three strains included in the study and that compound 4d displays excellent activity against S. aureus strain with a minimum inhibitory concentration value of 0.187 mg/mL. 相似文献
14.
Fumiko Fujisaki Sachi Hiromatsu Yumiko Matsumura Aki Fukami Nobuhiro Kashige Fumio Miake Kunihiro Sumoto 《Journal of heterocyclic chemistry》2013,50(2):417-424
In connection with our studies on antibacterial active compounds in the class of new oxazolidinones against Gram‐positive (Staphylococcus aureus) and Gram‐negative (Escherichia coli) strains, some molecular modifications were attempted. In this study, molecular modifications of 4‐aminomethyloxazolidin‐2‐ones ( 3a ) to the corresponding 4‐acylaminomethyloxazolidin‐2‐one derivatives ( 3c–d ) and preparations of the represented twin‐drug type molecules ( 10–14 ) were investigated. Some additional 4‐dialkylaminomethyloxazolidin‐2‐ones ( 2 ) were also synthesized. The synthesized compounds were evaluated for antibacterial activity with Gram‐positive (S. aureus) and Gram‐negative (E. coli) strains. 相似文献
15.
Aleem Gangjee Ying Wang Sherry F. Queener Roy L. Kisliuk 《Journal of heterocyclic chemistry》2006,43(6):1523-1531
16.
Synthesis of New (Pyrazol‐3‐yl)‐1,3,4‐oxadiazole Derivatives by Unexpected Aromatization During Oxidative Cyclization of 4,5‐Dihydro‐1H‐pyrazole‐3‐carbohydrazones and Their Biological Activities
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K. Jagadeesh Prathap M. Himaja Sunil V. Mali D. Munirajasekhar 《Journal of heterocyclic chemistry》2014,51(3):726-732
A series of novel 2‐(4‐(4‐chlorophenyl)‐1H‐pyrazol‐3‐yl)‐5‐(Aryl)‐1,3,4‐oxadiazoles were synthesized by unexpected aromatization during oxidative cyclization of 4‐(4‐chlorophenyl)‐4,5‐dihydro‐1H‐pyrazole‐3‐carbohydrazones using chloramine‐T as an oxidant. The hydrazones were derived from 4‐(4‐chlorophenyl)‐4,5‐dihydro‐1H‐pyrazole‐3‐carbohydrazide and various substituted aldehydes. The structure of the synthesized compounds was confirmed by FTIR, 1H NMR, 13C NMR, and mass spectral data. The synthesized compounds were evaluated for their antitubercular and antioxidant activities. All the compounds 4a , 4b , 4c , 4d , 4e , 4f , 4g , 4h and 5a , 5b , 5c , 5d , 5e , 5f , 5g , 5h showed good antitubercular activity against Mycobacterium tuberculosis (minimum inhibitory concentration = 25 µg/mL for 4f and 4g , 50–100 µg/mL for the rest). However, all the compounds exhibited poor antioxidant activity against 1,1‐diphenyl‐2‐picryl‐hydrazil free radical. 相似文献
17.
《Journal of heterocyclic chemistry》2018,55(4):983-987
A series of carboxamide and cyano functionalized pyridone derivatives 4a – q have been synthesized via one‐pot synthesis of various aldehydes 1a – q , acetoacetanilide 2 , and cyanoacetamide 3 . The reaction was simple and afforded pyridone derivatives in good yield, 89 to 93%. The novel pyridone derivatives were achieved by Hantzch one‐pot synthesis. Moreover, the synthesized compounds were screened against Gram‐positive and Gram‐negative bacteria and fungi for their activity. Among them, compound 4c shows highest inhibition at 4.25 mm against Staphylococcus aureus and 3.75 mm against Escherichia coli Gram‐positive and Gram‐negative bacteria, respectively. 相似文献
18.
One‐Pot Multicomponent Synthesis of Novel Substituted Imidazo[1,2‐a]Pyridine Incorporated Thiazolyl Coumarins and their Antimicrobial Activity
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Rajitha Gali Janardhan Banothu Rajitha Bavantula 《Journal of heterocyclic chemistry》2015,52(3):641-646
A series of novel substituted imidazo[1,2‐a]pyridine incorporated thiazolyl coumarin derivatives ( 4a , 4b , 4c , 4d , 4e , 4f , 4g , 4h , 4i , 4j , 4k , 4l , 4m , 4n , 4o , 4p , 4q , 4r , 4s , 4t ) were synthesized in good yields via one‐pot multicomponent condensation of substituted imidazo[1,2‐a]pyridine‐3‐carbaldehyde ( 3a , 3b , 3c , 3d , 3e ), thiosemicarbazide ( 2 ), and substituted 3‐(2‐bromoacetyl)‐2H‐chromen‐2‐ones ( 1a , 1b , 1c , 1d )/2‐(2‐bromoacetyl)‐3H‐benzo[f]chromen‐3‐one ( 1e ) in refluxing ethanol with catalytic amount of acetic acid. All the synthesized compounds ( 4a , 4b , 4c , 4d , 4e , 4f , 4g , 4h , 4i , 4j , 4k , 4l , 4m , 4n , 4o , 4p , 4q , 4r , 4s , 4t ) have been characterized by IR, NMR, and mass spectral studies as well as elemental analyses and evaluated for their in vitro antimicrobial activity against different bacterial and fungal strains. All the compounds displayed moderate antibacterial activity with minimum inhibitory concentration 150 µg/mL, but none of the compounds have shown any antifungal activity. 相似文献
19.
N‐Phenyl‐substituted carbene precursors and their silver complexes: synthesis,characterization and antimicrobial activities
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Yetkin Gök Senem Akkoç Sevil Albayrak Mehmet Akkurt Muhammad Nawaz Tahir 《应用有机金属化学》2014,28(4):244-251
A series of unsymmetrically substituted N‐heterocyclic carbene (NHC) precursors ( 1a , 1b , 1c , 1d , 1e ) were synthesized from the reaction of N‐phenylbenzimidazole with various alkyl halides. These compounds were used to synthesize NHC–silver(I) complexes ( 2a , 2b , 2c , 2d , 2e ). The five new 1‐phenyl‐3‐alkylbenzimidazolium salts ( 1a , 1b , 1c , 1d , 1e ) and their NHC–silver complexes ( 2a , 2b , 2c , 2d , 2e ) were characterized by the 1H NMR, 13C NMR and FT‐IR spectroscopic methods and elemental analysis techniques. Also, the two NHC–silver complexes 2b and 2c were characterized by single‐crystal X‐ray crystallography, which confirmed the linear C―Ag―Cl arrangements. The antibacterial activities of the NHC precursor and NHC–silver complexes were tested against three Gram‐positive bacterial strains (Bacillus subtilis, Listeria monocytogenes and Staphylococcus aureus) and three Gram‐negative bacterial strains (Escherichia coli, Klebsiella pneumoniae and Pseudomonas aeruginosa) using the microdilution broth method. The NHC–silver complexes showed higher antibacterial activity than the NHC precursors. In addition, silver complexes 2a , 2b , 2c , 2d showed high antibacterial activity against the Gram‐positive bacteria L. monocytogenes and S. aureus compared to the standard, tetracycline. Copyright © 2014 John Wiley & Sons, Ltd. 相似文献
20.
Synthesis of Novel Fused Thiazolo[3,2‐a]pyrimidin‐3‐ols and Evaluation for their Antibacterial Activity
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Ravibabu Velpula Janardhan Banothu Rajitha Gali Rajitha Bavantula 《Journal of heterocyclic chemistry》2016,53(1):51-55
A series of novel fused thiazolo[3,2‐a]pyrimidin‐3‐ol derivatives have been synthesized by reaction of fused pyrimidine‐thiones with 4‐substituted phenacyl bromide/3(2‐bromoacetyl)coumarin in refluxing acetic acid with good yields. All the synthesized compounds were confirmed by spectral studies and screened for their in vitro antibacterial activity against Staphylococcus aureus, Bacillus thuringiensis (Gram positive), Escherichia coli, and Klebsiella pneumoniae (Gram negative) bacterial strains. Activity results revealed that all the compounds were weak to good active against the tested bacterial strains on comparing with the standard drug gentamicin. 相似文献