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1.
A novel series of poly‐substituted pyridines (7‐(substituted aryl)‐3,11‐dimethoxy‐5,6,8,9‐tetrahydro‐dibenzo[c,h]acridines) were synthesized via one‐pot multicomponent approach using sulfamic acid as a catalyst and evaluated for their antimicrobial activity. The results indicate that the poly‐substituted series ( 4a , 4b , 4c , 4d , 4e , 4f , 4g , 4h , 4i ) showed weak to moderate antibacterial activity. However, compound ( 4c ) had shown good antifungal activity against Candida rugosa with standard antifungal drug Amphotericin‐B. Analogue ( 4c ) was considered to be a lead compound for subsequent standard optimization. 相似文献
2.
《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
3.
《Journal of heterocyclic chemistry》2018,55(4):1024-1032
(1) The benzoxazolyl/benzothiazolyl/benzimidazolyl pyrimidines were prepared under ultrasonication in the presence of pyridine/dimethylaminopyridine and triethylamine. (2) Better yields were recorded in 4‐(N,N‐dimethylamino)pyridine and Et3N. (3) The presence of electron withdrawing chloro, bromo, and nitro substituents enhanced antimicrobial activity ( 13c , 13e , 14e : minimum inhibitory concentration = 6.25 μg/well against Bacillus subtilis; 13e , 14e : minimum inhibitory concentration = 6.25 μg/well against Aspergillus niger). 相似文献
4.
Synthesis of Novel N‐Triazolo Methyl Substituted Fluoroquinolones and Their Antimicrobial Activity 下载免费PDF全文
A Ravi Kumar G. Sathaiah A. Chandra Shekhar K. Raju P. Shanthan Rao B. Narsaiah Y. K. Raju U. S. N. Murthy 《Journal of heterocyclic chemistry》2015,52(1):235-242
An elegant synthetic strategy was adopted for the preparation of N‐triazolo methyl substituted fluoroquinolones 4 and screened for their antimicrobial activity. The synthetic methodology starts from N‐propargylation of ethyl 7‐chloro‐6‐fluoro‐4‐hydroxyquinoline‐3‐carboxylate ( 1 ) followed by reaction with azides through click reaction under Sharpless conditions furnished triazole substituted quinolone ester 3 . The latter quinolone esters were reacted with various secondary amines to furnish the corresponding quinolone derivatives 4 . Alternatively, quinolone carboxylic derivatives 7a , 7b , 7c , 7d were prepared in two steps from triazole tagged quinolone ester. All the final products were screened against various bacterial and fungal strains. Compounds 4a , 4b , 4c and 4k showed moderate antibacterial activity, and 4f showed promising activity against fungal strains. 相似文献
5.
A series of pyrimidines were prepared by cyclocondensation of β‐bromovinyl aldehydes with amidine hydrochlorides in the presence of Et3N in excellent yields (74–95%). 相似文献
6.
Synthesis,Characterization, and Antibacterial Activity of Some Novel Substituted Imidazole Derivatives via One‐pot Three‐Component 下载免费PDF全文
Raj Kumar Ramagiri Murali Krishna Thupurani Rajeswar Rao Vedula 《Journal of heterocyclic chemistry》2015,52(6):1713-1717
A simple and highly efficient one‐pot, three‐component synthesis of novel substituted imidazole derivatives has been reported by the reaction of 3‐(2‐bromoacetyl)‐2H‐chromen‐2‐one, ammonium thiocyanate, and phenacyl aniline in the presence of acetic acid as a solvent under reflux condition with good yields. The structures of newly synthesized compounds were characterized by their analytical and spectral data. One of these compounds 4a showed good antibacterial activity against Escherichia coli gram‐negative strains. 相似文献
7.
8.
《Journal of heterocyclic chemistry》2017,54(1):524-530
A new class of azolyl pyrimidines linked by diamino sulfone moiety was prepared and studied their antimicrobial activity. Chloro‐substituted and nitro‐substituted thiazolyl pyrimidines ( 9c and 9e ) showed excellent antibacterial activity against Bacillus subtilis , while imidazolyl pyrimidines ( 10c and 10e ) exhibited promising antifungal activity against Aspergillus niger . 相似文献
9.
A Mild and Simple One‐pot Synthesis of 2‐Substituted Benzimidazole Derivatives Using DDQ as an Efficient Oxidant at Room Temperature 下载免费PDF全文
A series of 2‐substituted benzimidazoles were prepared through one‐pot reaction of o‐phenylenediamine with various aryl aldehydes in the presence of 2,3‐dichloro‐5,6‐dicyano‐1,4‐benzoquinone (DDQ) in acetonitrile as solvent at room temperature. The reactions were smoothly preceded in excellent yields and short reaction times with an easy work‐up. The pure benzimidazoles as products were confirmed and characterized by physical and spectral data. 相似文献
10.
CuII/TEMPO‐Promoted One‐Pot Synthesis of Highly Substituted Pyrimidines from Amino Acid Esters 下载免费PDF全文
Dr. Nini Zhou Tao Xie Zhongle Li Prof. Dr. Zhixiang Xie 《Chemistry (Weinheim an der Bergstrasse, Germany)》2014,20(52):17311-17314
A novel, Cu(OAc)2/TEMPO promoted one‐step approach for the preparation of fully substituted pyrimidines from readily available amino acid esters has been described. In this reaction, the amino acid esters act as the only N?C sources for the construction of corresponding pyrimidines. The mechanism of this process includes oxidative dehydrogenation, the generation of an imine radical, and a formal [3+3] cycloaddition. This methodology proves to be a high atom‐economic and straightforward strategy for the synthesis of pyrimidines and diverse substrates which are substituted by various functional groups have been afforded in moderate to good yield. 相似文献
11.
Novel ketene dithioacetals have been synthesized by a one‐pot condensation reaction of active methylene compounds with CS2 in the presence of alkyl acetylenecarboxylates. This reaction proceeds in a regioselective manner and provides products in good yields. The structures of the ketene dithioacetals were characterized by IR, 1H‐ and 13C‐NMR, and MS data, and elemental analyses. 相似文献
12.
《Journal of heterocyclic chemistry》2017,54(3):1776-1784
The regioselective spiroindoline derivatives were afforded via multi‐componant reaction. Its process was one of the green chemistry (simplicity, mild conditions, and atomic economy). The electron repelling and attracting groups affected on reactivity of the azomethine ylides (increase EHOMO value). All compound structures were confirmed by spectroscopic data and elemental analysis. The antibacterial and antioxidant activities for these synthesized compounds could be investigated; the highly antioxidant activity was observed with compounds, which proved to possess high HOMO values, and the highly antibacterial activity was observed against S . aureus , B . cereus , S . marcesens , and P . mirabilis , which proved to possess low HOMO values. 相似文献
13.
One‐Pot Synthesis of Some Dynamic 2‐Substituted Benzoxazinones and Their Corresponding Qinazolinones of Anticipated Biological Activity 下载免费PDF全文
Maher A. El‐Hashash Mohamed E. Azab Jehan M. Morsy 《Journal of heterocyclic chemistry》2016,53(1):95-101
Reactions of 6‐bromo‐2‐isopropyl‐4(3H)‐3,1‐benzoxazin‐4‐one toward mono‐ and di‐dentate nitrogen nucleophiles, e.g. primary aliphatic and aromatic amines, 1,2‐phenylenediamine, hydrazine hydrate, and formamide, have been investigated and afford the corresponding quinazolinones which are expected to have some interesting biological activity. The behavior of 3, 1‐benzoxazin‐4‐one toward active methylene compounds, namely, acetylacetone in basic medium has been studied and gave 3‐acetylquinoline. The last reaction is considered as an illustrative model of heterocyclic transformation reactions. 相似文献
14.
A new and environmentally benign multi‐component synthesis of tetra substituted 4H‐pyran derivatives is developed via the one‐pot reaction of an aromatic aldehyde, malononitrile, and 1,3‐diketone in the presence of NaOH with water as the solvent at RT. The reaction is efficient and affords excellent yields of the products. 相似文献
15.
A mild and facile Wittig reaction between N‐substituted maleimides and aldehydes has been developed. Various synthetically valuable alkylidenesuccinimides were obtained from this one‐pot reaction in high yields (up to 99%). The product was obtained by simple filtration and no extra purification was necessary. Ethanol, an environment‐benign solvent, was found to be a suitable reaction medium. 相似文献
16.
An efficient synthetic method for the preparation of pyridyl‐pyrimidines as potential inhibitors of protein–protein interactions is described. The key transformation is the reaction of a pyrimidine enaminone with phenyl ethyl acetate and NH4OAc to yield the desired pyridyl‐pyrimidine. 相似文献
17.
CMC负载稀土催化剂是由CMC和异丙氧基稀土制得。这种固体Lewis酸催化剂被用在比较温和的条件下合成取代的咪唑类化合物。相比于昂贵的稀土Lewis酸Ln(OTf)3,廉价的CMC负载稀土催化剂也显示出了很高的催化活性。此外,这种催化剂还具有易于回收和重复使用五次以上没有明显失活的优点。 相似文献
18.
An Efficient One‐pot Access to Substituted Dihydropyrrol‐2‐one Derivatives Using Sucrose as Natural,Biodegradable and Inexpensive Catalyst 下载免费PDF全文
Nourallah Hazeri Seyed Sajad Sajadikhah Malek Taher Maghsoodlou Sajad Mohamadian‐Souri Mahmoud Norouzi Maryam Moein 《中国化学会会志》2014,61(2):217-220
An efficient and simple procedure for the synthesis of highly substituted dihydropyrrol‐2‐ones has been developed via one‐pot four‐component condensation of amines, dialkyl acetylenedicarboxyaltes and formaldehyde in the presence of sucrose as an organocatalyst. The salient advantages of this method are using a natural, biodegradable and commercial available catalyst, good yields, short reaction times, simple work‐up and lack of need for column chromatography. 相似文献
19.
One‐Pot Multicomponent Synthesis of Novel Substituted Imidazo[1,2‐a]Pyridine Incorporated Thiazolyl Coumarins and their Antimicrobial Activity 下载免费PDF全文
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
20.
S. R. Lokhandwala K. R. Desai 《Phosphorus, sulfur, and silicon and the related elements》2013,188(11):2678-2684
Several Schiff base derivatives of phenophosphazines were synthesized by the reaction of amino phenophosphazines and aromatic aldehydes in equimolar ratio, using methanol as solvent. Possible structures have been proposed on the basis of elemental analysis, IR, and 1H NMR spectral studies. The antibacterial and antifungal activities of the above mentioned Schiff base derivatives have been evaluated against pathogens E. coli, S. typhi, S. aureus, B. subtilis, A. niger, and C. Albicans. 相似文献