Application of SBA-Pr-NH2 in one-pot three-component reaction of methylene-carbonyl compounds, acenaphthenequinone, malononitriles and exploration of its antimicrobial activity

2014 ◽  
Vol 12 (1) ◽  
pp. 57-65 ◽  
Author(s):  
P. Hajiabbasi ◽  
G. Mohammadi Ziarani ◽  
A. Badiei ◽  
A. Abolhasani Soorki
2021 ◽  
Vol 6 (3) ◽  
pp. 222-227
Author(s):  
Krishna A. Bhensdadia ◽  
Prakash L. Kalavadiya ◽  
Nilam H. Lalavani ◽  
Shipra H. Baluja

A novel series of dihydropyrido[2,3-d]pyrimidine derivatives were synthesized by multicomponent domino cyclization via the one-pot three component reaction of 6-amino uracil, substituted aryl aldehydes and N-methyl-1-(methylthio)-2-nitroethenamine in the presence of PTSA 10 mol% as a catalyst. The structures of these synthesized compounds were characterized by spectral analysis. Further the synthesized compounds screened for in vitro antimicrobial activity. Among all the compounds, compound 4b containing flouro substitution exhibited good inhibition against the tested species.


2019 ◽  
Vol 21 (4) ◽  
pp. 792-797 ◽  
Author(s):  
Jiaoting Pan ◽  
Runmin Zhao ◽  
Jiami Guo ◽  
Dumei Ma ◽  
Ying Xia ◽  
...  

The first facile and efficient acid-catalyzed three-component reaction of indoles, H-phosphine oxides and carbonyl compounds has been developed, providing a general, one-pot approach to structurally diverse C3-alkylated indole derivatives.


2019 ◽  
Vol 19 (6) ◽  
pp. 527-538 ◽  
Author(s):  
Fathy M. Abdelrazek ◽  
Sobhi M. Gomha ◽  
Mohamed E.B. Shaaban ◽  
Kamal A. Rabee ◽  
Heba N. El-Shemy ◽  
...  

Background: Thiazoles and pyridines are versatile synthetic scaffolds possessing wide spectrum of biological effects including potential antimicrobial activity. Objective: In the efforts to develop suitable antimicrobia drugs, medicinal chemists have focused on thiazole derivatives. A novel series of 2-thiazolyl pyridines was prepared in a one-pot three-component reaction using 2-bromoacetyl pyridine as a starting precursor. Method: Structure of the synthesized compounds was elucidated by spectral data (FT-IR, 1H NMR, 13C NMR, and mass) and elemental analyses. The prepared compounds were screened for their in vitro antimicrobial activity. Results: The results revealed that compounds 4a,b,e-g and 12 showed promising activity. Molecular docking studies using MOE software were carried out for compounds 4a and 4b which exhibited potent activities indicated by the diameter zones (4a; 3.6, 4.0, 1.2 mm) (4b; 4.2, 3.5, 1.5 mm) and the binding affinities (4a; -5.7731, -5.3576, -4.6844 kcal mol-1) (4b; -5.9356, -2.8250, -5.3628 kcal mol-1) against Candida albicans, Bacillus subtilis and Escherichia coli, respectively. Conclusion: This paper describes a facile and efficient MCR for synthesis of 2-thiazolyl pyridines from reaction of 2-bromoacetyl pyridine with different reagents. There was an agreement between the values of binding affinities and interactions and the data obtained from the practical antimicrobial screening of the tested compounds.


2018 ◽  
Vol 24 (6) ◽  
pp. 317-325 ◽  
Author(s):  
Serpil Demirci ◽  
Neslihan Demirbaş ◽  
Meltem Menteşe ◽  
SerapBaşoğlu Özdemir ◽  
Şengül A. Karaoğlu

Abstract Norfloxacin-azole hybrids 3 and 6a,b were synthesized starting from norfloxacin. The treatment of these compounds with amines as a one-pot three-component reaction produced the corresponding amino derivatives 4a,b, 7a–g and 8a,b in good yields. The conventional and microwave-assisted methods were used with the latter method being more efficient. The structures of the synthesized compounds were characterized by elemental analysis, IR, 1H NMR, 13C NMR and MS. All compounds were screened for their antimicrobial activities. Most of them exhibit excellent antibacterial activity but are not active against selected fungi.


2020 ◽  
Vol 13 (1) ◽  
pp. 227-231
Author(s):  
Marapala Kumara Swamy ◽  
N. Venkatesh ◽  
M. Swapna ◽  
P. Venkateswar Rao

A microwave assisted green synthetic methodoloy was developed for the synthesis various substituted pyrrolidinones derivatives by the one-pot three component reaction of aromatic aldehydes, aniline with dialkylbut-2-ynedioate in the presence of p-TsOH in water medium. The compounds were screened for their in vitro antimicrobial activity against four bacterial organism and two fungal organisms, resulted moderate to good activity with compared to their standard drug.


2020 ◽  
Vol 17 (6) ◽  
pp. 438-442
Author(s):  
Xiaofang Ma ◽  
Shunxi Li ◽  
Samrat Devaramani ◽  
Guohu Zhao ◽  
Daqian Xu

The elimination of volatile organic solvents in organic synthesis is the most important goal in “Green” chemistry. We report a simple, efficient and facile method for the addition of progargyl bromide to carbonyl compounds using Mg metal as a mediator under solvent-free conditions which could regioselectively generate homopropargyl alcohols efficiently in good to excellent yields. The procedure has advantages such as short reaction time, operationally simple, excellent product yields, high regioselectivity and organic solvent-free.


2014 ◽  
Vol 10 (6) ◽  
pp. 951-960
Author(s):  
Orazio Attanasi ◽  
Luca Bianchi ◽  
Maurizio D’Auria ◽  
Gianfranco Favi ◽  
Fabio Mantellini ◽  
...  

2020 ◽  
Vol 17 ◽  
Author(s):  
Visarapu Malathi ◽  
Pedavenkatagari Narayana Reddy ◽  
Pannala Padmaja

Abstract:: An efficient method has been developed for the synthesis of new pyrano[3,2-c] and pyrano[3,2-a]carbazole de-rivatives via a three component reaction of 4-hydroxycarbazole or 2-hydroxycarbazole, isocyanides, and dialkylacetylenedi-carboxylates. Noteworthy features of this protocol include mild reaction conditions, catalyst-free, high atom-economy and high yields.


Sign in / Sign up

Export Citation Format

Share Document