scholarly journals PYRIMIDINE INCORPORATED SCHIFF BASE OF ISONIAZID WITH THEIR SYNTHESIS, CHARACTERIZATION AND IN VITRO BIOLOGICAL EVALUATION

2017 ◽  
Vol 10 (10) ◽  
pp. 209 ◽  
Author(s):  
Hetal I Soni ◽  
Navin B Patel
Keyword(s):  
Pyridine Ring ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Biological Evaluation ◽  
Resonance Spectroscopy ◽  
Antituberculosis Activity ◽  
Aspergillus Clavatus ◽  
Pyrimidine Derivatives ◽  
In Vitro Antibacterial Activity

  Objective: Versatile biological activities of nitrogen containing heterocycles in medicinal chemistry, mainly pyrimidine and pyridine ring based heterocyclic moieties are very important. Pharmaceutical important of pyrimidine and isoniazid moiety prompted us to synthesize isoniazid clubbed pyrimidine derivatives and evaluated for antimicrobial and antituberculosis activity.Method: 2-(2-(3-bromo benzylidene)-1-isonicotinoyl hydrazinyl)-N-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) acetamide 2(A-J) have been synthesized by condensation reaction of 2-chloro-N-[4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl] acetamide and N’-[(E)- (3-bromophenyl) methylidene]pyridine-4-carbohydrazide. All newly synthesized compounds were screened for in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus pyogenes, antifungal against Candida albicans, Aspergillus niger, and Aspergillus clavatus, and antituberculosis activity against Mycobacterium tuberculosis H37RV.Results: Majority of the compounds exhibited good antibacterial, antifungal, and antituberculosis activity. All titled compounds were characterized by spectral analyses (infrared spectroscopy, nuclear magnetic resonance spectroscopy, and mass spectroscopy).Conclusion: 2-(2-(3-bromo benzylidene)-1-isonicotinoyl hydrazinyl)-N-(4-(substituted phenyl)-6-(substituted aryl) pyrimidin-2-yl) acetamide 2(A-J) showed good antimicrobial activity and comparatively good antituberculosis activity. Hence, all the compounds of this series considered for future investigation mainly in area of antibacterial, antifungal study.

scholarly journals Synthesis, Characterization and Preliminary Biological Evaluation of New 3 and 4-nitro Isoindoline-1, 3-dione/phthalimide Analogues

2021 ◽  
pp. 20-27
Author(s):  
Sharad Sankhe ◽  
Nitesh Chindarkar
Keyword(s):  
Antifungal Activity ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Agar Dilution Method ◽  
Bacterial Strains ◽  
In Vitro Antibacterial Activity ◽  
Nmr Techniques ◽  
Antibacterial And Antifungal

Aims: To synthesize new nitroisoindoline-1,3-diones analogues and evaluate their preliminary biological activities Methodology: New isoindoline-1,3-diones analogues were synthesized by coupling phthalic anhydride derivatives with appropriate aromatic amines. Newly synthesized heterocyclic compounds were evaluated for their in vitro antibacterial activity against gram-positive bacterial strains and gram-negative bacterial strains. They were also tested for their in vitro antifungal activity against fungi strains. Determination of the preliminary antibacterial and antifungal activity were investigated using agar-dilution method. The structures of newly synthesized analogues were elucidated by 1H and 13C-NMR techniques. Results: Bioassay indicated that some of the newly synthesized isoindoline-1,3-dione analogues shows moderate biological activities. Conclusion: Newly synthesized analogues can be used as antibacterial or antifungal agents on modifications.

Green synthesis, characterization, biological evaluation and docking study of some pyrazoline and pyrimidine derivatives

2021 ◽  
Vol 25 (12) ◽  
pp. 88-97
Author(s):  
H.A. Al-Ghulikah ◽  
A.S. El-Azab ◽  
M.S. AL-Saleem ◽  
M.S. AL-Towayan ◽  
S.A. Al-Issa
Keyword(s):  
Ultrasonic Method ◽  
Guanidine Hydrochloride ◽  
Acid Hydrazide ◽  
Docking Study ◽  
Biological Evaluation ◽  
High Yield ◽  
Pyrimidine Derivatives ◽  
New Synthesis ◽  
In Vitro Antibacterial Activity

Green and classical techniques have been utilized for preparing of a variety of aryl - substituted pyrazoline and pyrimidine derivatives (2-8). Reactions of chalcones 1 with semicarbazide and thiosemicarbazide, nicotinic acid hydrazide and amino guanidine hydrochloride afforded the corresponding N-substituted pyrazoline derivatives 2-5. Pyrimidine derivatives 6-8 were achieved via reaction of chalcone derivatives 1 with several reagents namely: guanidine nitrate, thiourea and 6-amino-2-thioxo-2,3- dihydropyrimidin-4(1H)-one under conventional and ultrasonic conditions. Ultrasonic method was found to be an easy work-up procedure and it gave high yield in comparison with conventional method. The structures of new synthesis compounds were characterized by elemental and spectral analyses. Some of newly compounds were tested in vitro antibacterial activity against some gram–positive and gram–negative. The antimicrobial results displayed favorable antimicrobial activity. Molecular docking has been perfomed for compound 5b using MOE 2008.10, The data results obtained are quite promising.

Chalcones: As potent α-amylase enzyme inhibitors; synthesis, in vitro, and in silico studies

2020 ◽  
Vol 16 ◽  
Author(s):  
Mahboob Ali ◽  
Momin Khan ◽  
Khair Zaman ◽  
Abdul Wadood ◽  
Maryam Iqbal ◽  
...  
Keyword(s):  
In Silico ◽  
Enzyme Inhibitors ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Type Ii Diabetes Mellitus ◽  
Spectroscopic Techniques ◽  
Chalcone Derivatives ◽  
In Silico Studies ◽  
Wide Range

: Background: The inhibition of α-amylase enzyme is one of the best therapeutic approach for the management of type II diabetes mellitus. Chalcone possesses a wide range of biological activities. Objective: In the current study chalcone derivatives (1-17) were synthesized and evaluated their inhibitory potential against α-amylase enzyme. Method: For that purpose, a library of substituted (E)-1-(naphthalene-2-yl)-3-phenylprop-2-en-1-ones was synthesized by ClaisenSchmidt condensation reaction of 2-acetonaphthanone and substituted aryl benzaldehyde in the presence of base and characterized via different spectroscopic techniques such as EI-MS, HREI-MS, 1H-, and 13C-NMR. Results: Sixteen synthetic chalcones were evaluated for in vitro porcine pancreatic α-amylase inhibition. All the chalcones demonstrated good inhibitory activities in the range of IC50 = 1.25 ± 1.05 to 2.40 ± 0.09 μM as compared to the standard commercial drug acarbose (IC50 = 1.34 ± 0.3 μM). Conclusion: Chalcone derivatives (1-17) were synthesized, characterized, and evaluated for their α-amylase inhibition. SAR revealed that electron donating groups in the phenyl ring have more influence on enzyme inhibition. However, to insight the participation of different substituents in the chalcones on the binding interactions with the α-amylase enzyme, in silico (computer simulation) molecular modeling analyses were carried out.

scholarly journals Hemisynthesis and Biological Evaluation of Cinnamylated, Benzylated, and Prenylated Dihydrochalcones from a Common Bio-Sourced Precursor

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 620
Author(s):  
Anne Ardaillou ◽  
Jérôme Alsarraf ◽  
Jean Legault ◽  
François Simard ◽  
André Pichette
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Cytotoxic Potential ◽  
Naturally Occurring

Several families of naturally occurring C-alkylated dihydrochalcones display a broad range of biological activities, including antimicrobial and cytotoxic properties, depending on their alkylation sidechain. The catalytic Friedel–Crafts alkylation of the readily available aglycon moiety of neohesperidin dihydrochalcone was performed using cinnamyl, benzyl, and isoprenyl alcohols. This procedure provided a straightforward access to a series of derivatives that were structurally related to natural balsacones, uvaretin, and erioschalcones, respectively. The antibacterial and cytotoxic potential of these novel analogs was evaluated in vitro and highlighted some relations between the structure and the pharmacological properties of alkylated dihydrochalcones.

scholarly journals Green Synthesis andIn VitroBiological Evaluation of Heteroaryl Chalcones and Pyrazolines of Medicinal Interest

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Vishal Banewar
Keyword(s):  
Green Synthesis ◽  
Elemental Analysis ◽  
Broad Spectrum ◽  
Spectroscopic Data ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Active Compounds

Pyrazolines are well known and important nitrogen containing 5-membered heterocyclic compounds. In the present investigation, a series of various heteroaryl chalcones and pyrazolines were synthesized by condensing formylquinolines with diverse ketones. The newly synthesized 2-pyrazolines were characterized on the basis of elemental analysis and spectroscopic data. All of the newly synthesized target compounds were selected by the NCI forin vitrobiological evaluation. These active compounds exhibited broad spectrum of various biological activities. Most of the compounds showed potent activity.

Synthesis and Biological Evaluation of Novel 4-Phenylaminobenzofuro[2,3-d]pyrimidine Derivatives

2020 ◽  
Vol 42 (4) ◽  
pp. 564-564
Author(s):  
Ju liu Ju liu ◽  
Jun Li Jun Li ◽  
Jian tao Shi Jian tao Shi ◽  
Jie Li Jie Li ◽  
Xue chen Hao Xue chen Hao ◽  
...  
Keyword(s):  
Cell Lines ◽  
A549 Cells ◽  
Positive Control ◽  
Biological Evaluation ◽  
Dependent Manner ◽  
Pyrimidine Derivatives ◽  
Concentration Dependent Manner ◽  
Ic50 Value ◽  
Synthesis And Biological Evaluation

A series of novel 4-phenylaminobenzofuro[2,3-d]pyrimidine derivatives had been prepared and assessed for their in vitro antiproliferative activities against three lung cancer cell lines (A549, H460 and H1975). The bioassay results showed most of the designed compounds exhibited potential antiproliferation activities. Among them, compound 8f exhibited remarkable inhibitory activity against A549 and H460 cell lines with IC50 value of 2.54 μM and 2.68 μM, respectively, which was comparable to that of the positive control sorafenib (IC50 = 2.69 μM for A549 and 3.71 μM for H460). AO/EB staining suggests that compound 8f could induce apoptosis in A549 cells. Furthermore, cell cycle analyses show that compound 8f increased G0/G1 A549 cells arrest in a concentration-dependent manner. The preliminary structure-activity relationships (SARs) studies indicated that mono-electron-withdrawing groups (mono-EWGs) on the phenyl ring are positive on the antitumor activity.

scholarly journals Synthesis and Spectral Studies of 4,4′-(Hydrazine-1,2-diylidenedimethylylidene)-bis-(2- methoxyphenol) and Its Transition Metal Complexes with Promising Biological Activities

2020 ◽  
Vol 32 (7) ◽  
pp. 1768-1772
Author(s):  
Anita Rani ◽  
Manoj Kumar ◽  
Hardeep Singh Tuli ◽  
Zahoor Abbas ◽  
Vinit Prakash
Keyword(s):  
Schiff Base ◽  
Transition Metal ◽  
Metal Complexes ◽  
Transition Metal Complexes ◽  
Schiff Base Ligand ◽  
Biological Activities ◽  
Condensation Reaction ◽  
Analytical Techniques ◽  
Spectral Studies

The study describes the synthesis, characterization and biological activity of a novel Schiff base ligand and its transition metal complexes. The Schiff base ligand was obtained by a condensation reaction between 4-hydroxy-3-methoxybenzaldehyde (p-vanillin) and hydrazine hydrate using ethanol as solvent. A new series of Ni(II) and Fe(III) complexes were also derived by reaction of prepared Schiff base ligand with NiCl2 and FeCl3. Both the ligand and its metal complexes were characterized by solubility, melting point and elemental analysis. These compounds were further identified by analytical techniques, FTIR, NMR and mass spectrometry. The ligand and its transition metal complexes were also subjected to in vitro biological activities i.e. antimicrobial, antiangiogenic and DNA photo cleavage. For antimicrobial activity compounds were tested against two strains of bacteria and two strains of fungi. Different concentrations of prepared compounds were treated with fertilized chicken eggs and plasmid DNA to find out antiangiogenic and DNA photocleavage activity, respectively.

scholarly journals Chemical Composition, Nutritional Value, and Biological Evaluation of Tunisian Okra Pods (Abelmoschus esculentus L. Moench)

Molecules ◽  
2020 ◽  
Vol 25 (20) ◽  
pp. 4739 ◽  
Author(s):  
Mariem Haj Romdhane ◽  
Hassiba Chahdoura ◽  
Lillian Barros ◽  
Maria Inês Dias ◽  
Rúbia Carvalho Gomes Corrêa ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Dietary Fiber ◽  
High Performance ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Abelmoschus Esculentus ◽  
Volatile Components ◽  
Total Dietary Fiber ◽  
Insoluble Dietary Fiber

The aim of this work was to perform an unprecedented in-depth study on the bioactive phytochemicals of Abelmoschus esculentus L. Moench Tunisian landrace (Marsaouia). For this purpose, its nutritional, aroma volatile, and phenolic profiles were characterized, and sundry biological activities were assessed in vitro. The approximate composition revealed that total dietary fiber as the most abundant macronutrient, mainly insoluble dietary fiber, followed by total carbohydrates and proteins. In addition, okra pods were rich in K, Ca, Mg, organic acids, tocopherols, and chlorophylls. Gas Chromatography-Electron Impact Mass Spectrometry (GC-EIMS) analysis showed that oxygenated monoterpenes, sesquiterpene hydrocarbons, and phenylpropanoids were the predominant essential volatile components in A. esculentus pods. A total of eight flavonols were detected by High-Performance Liquid Chromatography coupled to a DAD detector and mass spectrometry by electrospray ionization (HPLC-DAD-MS/ESI); with quercetin-3-O-glucoside being the majority phenolic component, followed by quercetin-O-pentosyl-hexoside and quercetin-dihexoside. This pioneering study, evidences that Tunisian okra display promising antioxidant and cytotoxic actions, in addition to relevant inhibitory effects against α-amylase and α-glucosidase enzymes, and interesting analgesic activity.

scholarly journals Ultrasonication-Induced Synthesis and Antimicrobial Evaluation of Some Multifluorinated Pyrazolone Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Anil Gadhave ◽  
Shashikant Kuchekar ◽  
Bhausaheb Karale
Keyword(s):  
Fungal Pathogens ◽  
Condensation Reaction ◽  
Ultrasound Irradiation ◽  
Conventional Heating ◽  
Aspergillus Clavatus ◽  
H Nmr ◽  
Pyrazolone Derivatives ◽  
Knoevenagel Condensation Reaction ◽  
Antimicrobial Evaluation

A series of novel fluorine containing pyrazole-pyrazolone (4a–j) and chromone-pyrazolone (5a–i) was synthesized from multifluorinated pyrazolone by the Knoevenagel condensation reaction. All compounds were synthesized by conventional heating as well as ultrasound irradiation technique. It was found that ultrasonication method was more efficient than conventional heating method. The newly synthesized compounds were subjected forin vitroantimicrobial screening against four bacterial pathogens, namely,Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli,andPseudomonas aeruginosaand three fungal pathogensCandida albicans, Aspergillus niger,andAspergillus clavatus, using broth microdilution (MIC) method (CLSI guidelines). Among them, some compounds exhibited promising antibacterial activity against the tested strains. All synthesized compounds were characterized by IR,1H-NMR, mass, and elemental analysis.

Biological Evaluation of Some Selected Cyclic Imides: Mitochondrial Effects and in vitro Cytotoxicity

2004 ◽  
Vol 59 (9-10) ◽  
pp. 663-672 ◽  
Author(s):  
Silvia Regina Tozado Prado ◽  
Valdir Cechinel-Filho ◽  
Fátima Campos Buzzi ◽  
Rogério Corrêa ◽  
Silvia Maria Correia Suter Cadena ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Cell Viability ◽  
Cell Line ◽  
Biological Activities ◽  
General Structure ◽  
Peritoneal Macrophages ◽  
Biological Evaluation ◽  
Rat Liver Mitochondria ◽  
Cyclic Imides

Abstract Cyclic imides such as succinimides, maleimides, glutarimides, phthalimides and their derivatives contain an imide ring and a general structure -CO-N(R)-CO- that confers hydrophobicity and neutral characteristic. A diversity of biological activities and pharmaceutical uses have been attributed to them, such as antibacterial, antifungal, antinociceptive, anticonvulsant, antitumor. In spite of these activities, much of their action mechanisms at molecular and cellular levels remain to be elucidated. We now show the effects of several related cyclic imides: maleimides (S2, S2.1, S2.2, S3), glutarimides (S4, S5, S6), 4-aminoantipyrine derivatives (L1, F1, AL1, F1.14, F1.2) and sulfonated succinimides (RO1, FA, FE, FD, MC, DMC) on isolated rat liver mitochondria, B16-F10 melanoma cell line, peritoneal macrophages and different bacterial streams. The effects on mitochondrial respiratory parameters, cell viability and antibacterial activity were also evaluated. The results indicated that S3, S5 and S6 caused an increased oxygen consumption in the presence of ADP (state III) or its absence (state IV), while all other compounds decreased those parameters at different degrees of inhibition. All the compounds decreased the respiratory control coefficient (RCC). Loss of cell viability of peritoneal macrophages and the B16- F10 cell line was observed, L1 and S2.1 being more effective. S1, S2, S3, L1 and F1 compounds showed antibacterial activity at experimental concentrations.

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