scholarly journals Toward the Identification of Novel Antimicrobial Agents: One-Pot Synthesis of Lipophilic Conjugates of N-Alkyl d- and l-Iminosugars

Marine Drugs ◽  
2020 ◽  
Vol 18 (11) ◽  
pp. 572
Author(s):  
Anna Esposito ◽  
Daniele D’Alonzo ◽  
Stefano D’Errico ◽  
Eliana De Gregorio ◽  
Annalisa Guaragna

In the effort to improve the antimicrobial activity of iminosugars, we report the synthesis of lipophilic iminosugars 10a–b and 11a–b based on the one-pot conjugation of both enantiomeric forms of N-butyldeoxynojirimycin (NBDNJ) and N-nonyloxypentyldeoxynojirimycin (NPDNJ) with cholesterol and a succinic acid model linker. The conjugation reaction was tuned using the established PS-TPP/I2/ImH activating system, which provided the desired compounds in high yields (94–96%) by a one-pot procedure. The substantial increase in the lipophilicity of 10a–b and 11a–b is supposed to improve internalization within the bacterial cell, thereby potentially leading to enhanced antimicrobial properties. However, assays are currently hampered by solubility problems; therefore, alternative administration strategies will need to be devised.

2017 ◽  
Vol 13 (2) ◽  
pp. 6006-6020
Author(s):  
Amira A. El-Sayed ◽  
Maher El-HAshash ◽  
Sameh Rizk

One pot synthesis and reaction of triazinthione and triazinohydrazide derivatives with different electrophilic reagents in ordered to synthesis of some interesting non-mixed heterocyclic compounds. Structures of thiazolotriazine, triazolotriazine, pyrimidinyltriazine, and triazinotriazine derivatives were established via spectroscopic data and elemental analysis. The synthesized compounds were screened for their antimicrobial activity.


2013 ◽  
Vol 6 (1) ◽  
pp. 150-156
Author(s):  
Pramod S. Kulkarni ◽  
Dasharath D. Kondhare ◽  
Ravi Varala ◽  
Pudukulathan K. Zubaidha

Abstract Calcium hydroxide was found to be an efficient mild base for the one-pot synthesis of curcumin and its analogues obtained by condensation of one equivalent of acetyl acetone with two equivalents of corresponding aromatic aldehyde. The present protocol offers various advantages such as high yields, inexpensive easily available mild base, easy workup and eco-friendly method.


2019 ◽  
Vol 63 (4) ◽  
Author(s):  
ASHOK DONGAMANTI ◽  
Nagaraju Nalaparaju ◽  
Sarasija Madderla ◽  
Vijaya Lakshmi Bommidi

In the present work, we report the one pot synthesis of tetrazole based 3-hydroxy-4H-chromen-4-ones 3(a-g) from  4-(1H-tetrazol-5-yl)benzaldehyde and 2-hydroxy acetophenone using KOH and H2O2 by modified Algar-Flynn-Oyamada reaction under conventional and microwave irradiation conditions. In this technique, flavonols are synthesized without isolating chalcones, in good yields. All the synthesized compounds were characterized by IR, NMR, MS and elemental. All newly synthesized compounds were screened for their in-vitro antimicrobial activity against strains such as Staphylococcus aurous, Bacillus subtilis, Klebsiella pneumonia, Escherichia coli, Aspergillus Niger, Aspergillus flavus, and Fusarium oxysporum. The results of antimicrobial studies revealed that most of the compounds exhibit good activity.


Molecules ◽  
2017 ◽  
Vol 22 (12) ◽  
pp. 2218 ◽  
Author(s):  
Magdi El Fergani ◽  
Natalia Candu ◽  
Simona Coman ◽  
Vasile Parvulescu

2014 ◽  
Vol 2014 ◽  
pp. 1-5 ◽  
Author(s):  
Naser Montazeri ◽  
Taghva Noghani ◽  
Mona Ghorchibeigy ◽  
Rozita Zoghi

Pentafluoropropionic acid (PFPA) efficiently catalyzes the one-pot, three-component reaction of aromatic aldehyde, malononitrile, and dimedone to yield tetrahydrobenzo[b]pyran derivatives in high yields. This method is of great value because of its easy processing, short reaction time, environmentally, and high yields.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Sougata Santra ◽  
Matiur Rahman ◽  
Anupam Roy ◽  
Adinath Majee ◽  
Alakananda Hajra

A green and highly efficient method has been developed for the one-pot synthesis of tetrahydrobenzo[b]pyrans via a three-component condensation of aldehydes, 1,3-cyclic diketones, and malononitrile under MW irradiation without using any catalyst and solvent. This transformation presumably occurs by a sequential Knoevenagel condensation, Michael addition, and intramolecular cyclization. Operational simplicity, solvent and catalyst-free conditions, the compatibility with various functional groups, nonchromatographic purification technique, and high yields are the notable advantages of this procedure.


2009 ◽  
Vol 7 (3) ◽  
pp. 550-554 ◽  
Author(s):  
Lakshman Gadekar ◽  
Shivshankar Mane ◽  
Santosh Katkar ◽  
Balasaheb Arbad ◽  
Machhindra Lande

AbstractNatural scolecite has been found as an effective catalyst for the one-pot synthesis of 2,4,5-triarylimidazole derivatives via a three component reaction using benzil or benzoin, aldehydes and ammonium acetate. This method provides several advantages such as being environmentally benign, reusable, possessing high yields with increased variations of the substituents in the product and preparative simplicity.


2015 ◽  
Vol 68 (10) ◽  
pp. 1529 ◽  
Author(s):  
Mehdi Rimaz

Two efficient regioselective approaches for the one-pot synthesis of 3-arylpyridazino[4,3-c]quinolin-5(6H)-one derivatives are reported, by the three-component reaction of arylglyoxal monohydrates, quinoline-2,4-diol, and hydrazinium dihydrochloride or hydrazine hydrate in ethanol and pyridine. In ethanol, the reactions were catalyzed by 1,4-diazobicyclo[2,2,2]octane. The features of both procedures are high regioselectivity, mild reaction conditions, good to high yields, and operational simplicity.


Synthesis ◽  
2021 ◽  
Author(s):  
Darío C. Gerbino ◽  
H. Sebastián Steingruber ◽  
Pamela Mendioroz ◽  
María A. Volpe

AbstractAn efficient palladium-catalyzed tandem reaction for the one-pot synthesis of 9H-carbazoles under microwave irradiation is developed. This approach involves a sequential Buchwald–Hartwig amination and a direct arylation from affordable and inexpensive anilines and 1,2-dihaloarenes. For the development of this purpose, a novel and magnetically recoverable palladium nanocatalyst supported on a green biochar under ligand-free conditions is used. Compared to other existing palladium-based protocols, the present synthetic methodology shows a drastic reduction in reaction times and excellent compatibility with different functional groups allowing to obtain a small library of 9H-carbazoles in high yields and with good regioselectivity. This procedure represents the first example in the direct synthesis of carbazoles using a heterogeneous palladium nanocatalyst from commercial precursors. To examine the application of this protocol, a direct and scalable synthesis of the bioactive carbazole alkaloid clausenalene from commercially available starting materials is described.


2010 ◽  
Vol 75 (3) ◽  
pp. 299-305 ◽  
Author(s):  
Hassan Ghasemnejad-Bosra ◽  
Mohammad Faraje ◽  
Setareh Habibzadeh ◽  
Farhad Ramzanian-Lehmali

N-Bromosuccinimide was found to efficiently catalyze the synthesis of highly functionalized, tetra-substituted furan derivatives in the one-pot reactions of but-2-ene-1,4-diones and acetoacetate esters in the presence of i-PrOH as solvent under mild and neutral conditions at 80-90?C for 3-7 h in high yields (87-94%).


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