scholarly journals Design and microwave-assisted synthesis of a novel Mannich base and conazole derivatives and their biological assessment

2021 ◽  
Vol 27 (1) ◽  
pp. 100-111
Author(s):  
Yıldız Uygun Cebeci ◽  
Şengül Alpay Karaoğlu

Abstract 4-Amino-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one (1) was converted to the corresponding Schiff base (2) by treatment with salicylaldehyde. 1,2,4-Triazoles were then converted to the corresponding Mannich bases containing fluroquinolone core using a one-pot three-component procedure. Moreover, the synthesis of six compounds, which can be considered as conazole analogues, was performed starting from 1,2,4-triazole-3-one compounds via three steps by either conventional or microwave-mediated conditions. All the newly synthesized compounds were screened for their antimicrobial activities. Most exhibited good to moderate antibacterial and/or antifungal activity. The structural assignments of the new compounds were based on elemental analysis and spectral (IR, 1H NMR, 13C NMR, and LC-MS) data.

Quimica Hoy ◽  
2012 ◽  
Vol 2 (2) ◽  
pp. 4
Author(s):  
Erika Loredo Calderón ◽  
Carolina Martínez Lejía ◽  
Susana López Cortina ◽  
Blanca Muñoz Flores ◽  
Eugenio Hernández Fernández ◽  
...  

Toe synthesis of new unsymmetrical A,B porphyrin, 5,10,15-tri(4-methoxyphenyl)-20-(4-chlorophenyl)-21H, 23H-porphyrin, 1, and its Zinc(II) complex, 5, 1 O, 15-tri( 4-methoxyphenyl)-20-( 4-chlorophenyl)-21, 23- Zinc(II)-porphine, l, was accomplished using both conventional and "one pot" solventless microwave assisted methods with interesting comparative results. The obtained molecules were characterized by 'H NMR, UV-Vis and MS. These molecules are considered to represent new compounds with potential application as photosensitizers in photodynamic therapy.


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.


2012 ◽  
Vol 2012 ◽  
pp. 1-4 ◽  
Author(s):  
F. Taktak ◽  
I. Bulduk

An efficient one-pot microwave-assisted hydrogenation of codeine was achieved in aqueous solution. This technique is simple, fast, environmentally friendly, and highly efficient. Structure of produced dihydrocodeine was approved by using FT-IR, 1H NMR, 13C NMR, EIMS, and elemental analysis technique. Its purity analysis was performed by using HPLC and assay analysis was performed by using potentiometric titration methods.


2007 ◽  
Vol 72 (2) ◽  
pp. 109-117 ◽  
Author(s):  
S.J. Vaghasia ◽  
V.H. Shah

The synthesis of thiazolo[5,4-d]pyrimidines can be achieved from different 5- thiazolidinones, 2-butyl-1H-imidazole-5-carbaldehyde and thiourea using microwave irradiation within 5 min. The structures of the products were supported by FTIR, PMR and mass spectral data. The in vitro antimicrobial activity of the synthesized thiazolo[5,4-d]pyrimidines 1a-j, having substituents at the 1- and 3-positions, were determined by the cup-plate method against several standard strains chosen to define the spectrum and potency of the new compounds. The antimicrobial activities of the thiazolo[5,4-d]pyrimidines 1a-j are compared with those of known chosen standard drugs, viz. ampicillin, chloramphenicol, ciprofloxacin, norfloxacin and griseofulvin. .


2009 ◽  
Vol 6 (2) ◽  
pp. 323-331
Author(s):  
D. Ashok ◽  
K. Aravind

A series of 1-{2, 4-dihydroxy-5-[5-(aryl)-1-pyridine/pyrimidine-4-carbonyl)-4, 5-dihydro-1H-pyrazol-3-yl]-phenyl}-3-(aryl)-propenones (2a-h) have been synthesized from 1-[2,4-dihydroxy-5-(aryl acryloyl)phenyl]-aryl propenones(1a-h)by Micheal addition with isoniazide/pyrazinic acid hydrazide under microwave irradiation and classical heating. The synthesized compounds were characterized by IR,1H-NMR,13C-NMR and Mass spectral data. All the compounds were screened for their Antibacterial activity.


Crystals ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 117
Author(s):  
Yousef Hijji ◽  
Rajeesha Rajan ◽  
Hamdi Ben Yahia ◽  
Said Mansour ◽  
Abdelkader Zarrouk ◽  
...  

The(3R,4R,6R)-3-(((E)-2-hydroxybenzylidene)amino)-6-(hydroxymethyl)tetrahydro-2H-pyran-2,4,5-triol water-soluble Glucose amine Schiff base (GASB-1) product was made available by condensation of 2-hydroxybenzaldehyde with (3R,6R)-3-amino-6-(hydroxymethyl)-tetra-hydro-2H-pyran-2,4,5-triol under mono-mode microwave heating. A one-pot 5-minute microwave-assisted reaction was required to complete the condensation reaction with 90% yield and without having byproducts. The 3D structure of GASB-1 was solved from single crystal X-ray diffraction data and computed by DFT/6-311G(d,p). The Hirshfeld surface analysis (HSA), molecular electronic potential (MEP), Mulliken atomic charge (MAC), and natural population analysis (NPA) were performed. The IR and UV-Vis spectra were matched to their density functional theory (DFT) relatives and the thermal behavior was resolved in an open-room condition via thermogravimetry/Derivative thermogravimetry (TG/DTG) and differential scanning calorimetry (DSC). The highest occupied molecular orbital/lowest unoccupied molecular orbital (HOMO/LUMO), density of state (DOS), and time-dependence TD-DFT computations were correlated to the experimental electron transfer in water and acrylonitrile solvents.


e-Polymers ◽  
2009 ◽  
Vol 9 (1) ◽  
Author(s):  
Saeed Zahmatkesh ◽  
Abdol Reza Hajipour

AbstractPyromellitic dianhydride (1) was reacted with L-leucine (2) to result in [N,N'-(pyromellitoyl)-bis-L-leucine diacid] (3). This compound (3) was converted to N,N'-(pyromellitoyl)-bis-L-leucine diacid chloride (4) by reaction with thionyl chloride. The microwave-assisted polycondensation of this diacid chloride (4) with polyethyleneglycol-diol (PEG-200) and/or three synthetic bisphenols furnish a series of new PEIs and Co-PEIs in a laboratory microwave oven (Milestone). The resulting polymers and copolymers have inherent viscosities in the range of 0.31- 0.53 dl g-1. These polymers are optically active, thermally stable and soluble in polar aprotic solvents such as DMF, DMSO, NMP, DMAc and sulfuric acid. All of the above polymers were fully characterized by IR spectroscopy, 1H NMR spectroscopy, elemental analyses, specific rotation and thermal analyses. Some structural characterizations and physical properties of these optically active PEIs and Co-PEIs are reported.


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