scholarly journals Synthesis and Biological Evaluation of Coumarinyl Sydnone Derivatives

2011 ◽  
Vol 8 (1) ◽  
pp. 113-118 ◽  
Author(s):  
Keshav C. Patel ◽  
Himanshu D. Patel
Keyword(s):  
Antimicrobial Activity ◽  
Melting Point ◽  
Thin Layer ◽  
Biological Evaluation ◽  
Physical Methods ◽  
H Nmr ◽  
Antimicrobial Evaluation ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

A novel series of compounds containing coumarinyl sydnone derivatives from 4-methyl-7-hydroxy-8-nitro coumarin were synthesized. The formed compounds have been evaluated by physical methods (melting point, thin layer chromatography, elemental analysis) and by spectral data (IR,1H-NMR &13C NMR). The antimicrobial evaluation of the compounds showed that some of them revealed promising antimicrobial activity.

scholarly journals FeCl3-catalyzed Synthesis of Dehydrodiisoeugenol

2015 ◽  
Vol 8 (1) ◽  
pp. 1
Author(s):  
Athina Mardhatillah ◽  
Mutakin Mutakin ◽  
Jutti Levita
Keyword(s):  
Molecular Structure ◽  
Melting Point ◽  
Mobile Phase ◽  
Crystalline Form ◽  
Distilled Water ◽  
Environment Friendly ◽  
H Nmr ◽  
Abundance Peak ◽  
Layer Chromatography ◽  
C Nmr

Dehydrodiisoeugenol (DDIE) synthesis has been performed by modifying a method recommended by Leopold with a different ratio of isoeugenol and FeCl<sub>3</sub> (1.9:1). FeCl<sub>3</sub> was chosen as catalyst due to its efficiency and environment-friendly property. This modification yielded 22.93 % of product. The product, a white crystalline form, was characterized using thin layer chromatography, melting point, UV, IR, HRMS, and NMR spectroscopy, as well as HPLC, employing pure DDIE as the standard. TLC chromatogram showed Rf 0.32 using n-hexane/ethyl acetate (8:2). The crystals melted at 138-139 <sup>o</sup>C, while its UV maximum was detected at l 273 nm. IR spectrum showed a specific broad O-H stretch at 3437.15 cm<sup>-1</sup>, C-H aromatic and C-H alkene at 3163.26 and 3024.38 cm<sup>-1</sup>, C-H alkyl stretch at 2951.09 and 2927.94 cm<sup>-1</sup>. An overtone peak of aromatic was detected at 2100 to 1700 cm<sup>-1</sup>. C-O peak was detected at 1126.43 cm<sup>-1</sup>. HPLC showed that this compound was eluted at 11.886 minutes after it was injected to a C18 column 250 x 4 mm using a mixture of methanol and double distilled water (73:27) for mobile phase. HRMS spectra predicted that the molecular structure is C<sub>20</sub>H<sub>22</sub>O<sub>4</sub> as showed by abundance peak at <em>m/z </em>327.1595 of [M+H]<sup>+</sup>. <sup>1</sup>H-NMR and <sup>13</sup>C-NMR indicated that the synthesized compound contains 13 types of proton and 20 types of carbon. Herein we reported that white needle-like crystals of DDIE using FeCl<sub>3</sub> as catalyst had been synthesized, moreover the decreasing of the catalyst reduced the yield of the product.

scholarly journals Synthesis and Antimicrobial Activity of (2-Methoxy/2-Amino)-6-{4'-[(4'''-Chlorophenyl) (Phenyl) Methyl Amino] Phenyl}-4-Aryl Nicotinonitrile

2015 ◽  
Vol 49 ◽  
pp. 99-103
Author(s):  
J.V. Guna ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antimicrobial Activity ◽  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Spectral Data ◽  
Elemental Analysis ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Layer Chromatography

2- Methoxy – 6 - {4' - [(4'''- Chlorophenyl) (phenyl) methyl amino] phenyl} - 4 - aryl nicotinonitrile (3a-3l) and 2-Amino-6-{4'-[(4'''-Chlorophenyl)(phenyl)methyl amino]phenyl}-4-aryl nicotinonitrile (4a-4l) have been synthesized. The products have been assayed for their antimicrobial activity against Gram +ve, Gram -ve bacteria and fungi. The structure of the products has been elucidated by IR, 1H-NMR, mass spectral data, elemental analysis and thin layer chromatography.

scholarly journals Design, synthesis, and biological evaluation of novel urolithins derivatives as potential phosphodiesterase II inhibitors

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Long Tang ◽  
Jianchun Jiang ◽  
Guoqiang Song ◽  
Yajing Wang ◽  
Ziheng Zhuang ◽  
...  
Keyword(s):  
Small Molecules ◽  
Inhibitory Activity ◽  
Structural Modification ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Lead Compounds ◽  
Activity Test ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

AbstractA series of urolithins derivatives were designed and synthesized, and their structures have been confirmed by 1H NMR, 13C NMR, and HR-MS. The inhibitory activity of these derivatives on phosphodiesterase II (PDE2) was thoroughly studied with 3-hydroxy-8-methyl-6H-benzo[C]chromen-6-one and 3-hydroxy-7,8,9,10-tetrahydro-6H-benzo[C] chromen-6-one as the lead compounds. The biological activity test showed that compound 2e had the best inhibitory activity on PDE2 with an IC50 of 33.95 μM. This study provides a foundation for further structural modification and transformation of urolithins to obtain PDE2 inhibitor small molecules with better inhibitory activity.

Synthesis and Biological Evaluation of Flavonoids as Antiacetyl- cholinesterase Agent

2014 ◽  
Vol 69 (1) ◽  
Author(s):  
Saleh Nazifi Ibrahim ◽  
Farediah Ahmad
Keyword(s):  
Thin Layer ◽  
Thin Layer Chromatography ◽  
Inhibitory Activity ◽  
Biological Evaluation ◽  
Microplate Assay ◽  
Synthetic Compounds ◽  
Ache Inhibitory Activity ◽  
Weak Activity ◽  
Layer Chromatography ◽  
Synthesis And Biological Evaluation

A series of chalcones, a flavone and one flavanone were synthesized and elucidated structurally by IR and 1H NMR spectroscopies. The synthetic compounds were then screened for acetylcholinesterase inhibitory activity using thin layer chromatography (TLC) and microplate assays. In the TLC assay, only 2′-hydroxy-4-methoxychalcone and 2′-hydroxy-4′-O-prenyl-2,6-dichlorochalcone were found to show moderate and weak activity respectively against acetylcholinesterase (AchE) at 0.1 mM concentration compared to the control galanthamine. 4′-Hydroxy-2,6-dichlorochalcone, 2′-hydroxy-4-nitrochalcone, 2′-hydroxy-4-(dimethyl)aminochalcone and 2′-hydroxy-4-methoxychalcone showed moderate AchE inhibitory activity with percentage inhibition of 54.24, 46.14 and 49.32 % respectively in the microplate assay.

scholarly journals Synthesis and Biological Evaluation of Some Novel 1, 3, 5-Trisubstituted Pyrazolines

2010 ◽  
Vol 7 (1) ◽  
pp. 295-298 ◽  
Author(s):  
B. C. Revanasiddappa ◽  
R. Nagendra Rao ◽  
E. V. S. Subrahmanyam ◽  
D. Satyanarayana
Keyword(s):  
Antimicrobial Activity ◽  
Acetic Acid ◽  
Spectral Data ◽  
Glacial Acetic Acid ◽  
Biological Evaluation ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Synthesis And Biological Evaluation

A new series of chalcones (3a-j) were synthesized by condensation of simple aldehydes with substituted acetophenones in presence of alkali. The resulted chalcones upon cyclization in presence of glacial acetic acid with isoniazid (INH) will yields the title compounds (4a-j). The newly synthesized compounds were assigned on the basis of IR,1H NMR, and Mass spectral data. All the final compounds were evaluated for theirin vitroantimicrobial activity.

scholarly journals Synthesis and Biological Evaluation of Novel 5,7-Dichloro-1,3-benzoxazole Derivatives

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
N. D. Jayanna ◽  
H. M. Vagdevi ◽  
J. C. Dharshan ◽  
T. R. Prashith Kekuda ◽  
B. C. Hanumanthappa ◽  
...  
Keyword(s):  
Enzyme Inhibitors ◽  
Heterocyclic Ring ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
H Nmr ◽  
New Class ◽  
Synthesis And Biological Evaluation ◽  
Active Methylene ◽  
C Nmr

A new class of 5,7-dichloro-1,3-benzoxazole derivatives4–11were synthesized by fusing 5,7-dichloro-2-hydrazino-1,3-benzoxazole3nucleus with aliphatic acids, active methylene compounds, and with selected esters to form heterocyclic ring systems like 1,2,4-triazoles, pyrazoles, and triazine moieties. The compound3on diazotization reaction affords the tetrazole compound. The synthesized compounds were characterized by1H NMR, IR, Mass, and13C NMR spectral data and screened for cytotoxic, antimicrobial, antioxidant, and antilipase activities. The compounds4,5, and8have shown significant antimicrobial activities, whereas compounds6and8have been emerged as leading cytotoxic agents. The compounds9,10, and11were found to be strong enzyme inhibitors.

scholarly journals Alkaloid profiling and antimicrobial activities of Papaver glaucum and P. decaisnei

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Hawraz Jawdat Jafaar ◽  
Ovgu Isbilen ◽  
Ender Volkan ◽  
Gunay Sariyar
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Activity ◽  
Thin Layer ◽  
Preparative Thin Layer Chromatography ◽  
Antimicrobial Activities ◽  
Northern Iraq ◽  
H Nmr ◽  
Rf Values ◽  
Layer Chromatography ◽  
Strong Antimicrobial Activity

Abstract Objective Papaver decaisnei Hochst. & Steud. Ex Elkan and Papaver glaucum Boiss. & Hausskn. growing wild in Northern Iraq have been historically used for medicinal purposes. In this study, both species were evaluated for their alkaloid content and antimicrobial activities. Results Alkaloids were extracted and isolated by preparative thin-layer chromatography (TLC). Identification was carried out by comparing spectral data (UV and 1H-NMR) and TLC Rf values with those of authentic samples. Two alkaloids, proapaorphine-type mecambrine and aporphine-type roemerine were isolated from P. decaisnei. Two benzylisoquinoline type alkaloids papaverine (major alkaloid) and palaudine as well as aporphine-type N-methylasimilobine have been obtained in P. glaucum. Both P. glaucum and P. decaisnei extracts revealed strong antimicrobial activity on Pseudomonas aeruginosa ATCC 27853 and Enterococcus faecalis ATCC 29212. Collectively these results indicate that P. glaucum and P. decaisnei are promising sources of alkaloids that could further be investigated for medicinal purposes.

scholarly journals Synthesis and Antimicrobial Activity of (1-Acetyl/1-Phenyl)-3-{4'-[(4'''-Chlorophenyl) (Phenyl) Methyl Amino] Phenyl}-5-Aryl-Pyrazoline

2015 ◽  
Vol 49 ◽  
pp. 104-108
Author(s):  
J.V. Guna ◽  
V.N. Bhadani ◽  
H.D. Purohit ◽  
Dipak M. Purohit
Keyword(s):  
Antimicrobial Activity ◽  
Biological Activity ◽  
Thin Layer ◽  
Elemental Analysis ◽  
Moderate Activity ◽  
Mass Spectral Data ◽  
Mass Spectral ◽  
H Nmr ◽  
Bacteria And Fungi ◽  
Layer Chromatography

1-Acetyl-3-{4'-[(4'''-chlorophenyl) (phenyl) methyl amino] phenyl}-5-aryl-pyrazolines (3a-3l) and 1-Phenyl-3-{4'-[(4'''-chlorophenyl) (phenyl) methyl amino] phenyl}-5-aryl-pyrazolines (4a-4l) have been synthesized. The products have been assayed for their biological activity against Gram +ve, Gram -ve bacteria and fungi. Some of the compounds showed moderate activity in concentration 50 μg/ml. The structure of the products have been elucidated by IR, 1H-NMR, mass spectral data elemental analysis and Thin layer chromatography.

scholarly journals Design, Synthesis and Biological Evaluation of N-((2-phenyloxazol-4-yl)methyl) Pyrimidine Carboxamide Derivatives as Potential Fungicidal Agents

2020 ◽  
Vol 26 (1) ◽  
pp. 185-191
Author(s):  
Danling Huang ◽  
Shumin Zheng ◽  
Yong-Xian Cheng
Keyword(s):  
Sclerotinia Sclerotiorum ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
H Nmr ◽  
Structure Activity ◽  
Colletotrichum Fragariae ◽  
New Compounds ◽  
Synthesis And Biological Evaluation ◽  
Commercial Fungicide ◽  
C Nmr

Abstract Twelve N-((2-phenyloxazol-4-yl)methyl) pyrimidine carboxamide derivatives were designed, synthesized, and characterized by 1H NMR, 13C NMR, and HRMS. The fungicidal activities of these new compounds against Sclerotinia sclerotiorum, Botrytis cinereal, and Colletotrichum fragariae were evaluated. The results indicated that compounds 5b, 5f, and 5g displayed potential fungicidal activities against tested fungi, especially 5f exhibited IC50 value of 28.9 mg/L against S. sclerotiorum. Moreover, the compounds 5f and 5g showed IC50 values of 54.8 mg/L and 62.2 mg/L against C. fragariae respectively, which shows that they were more active than the commercial fungicide hymexazol. The superficial structure-activity relationships were discussed, which may be of benefit for the development of fungicides and discovery of novel fungicides.

scholarly journals Formation and Biological Evaluation of 4-Thiazolidinone Derivatives for their Pharmacological Activity

2015 ◽  
Vol 61 ◽  
pp. 84-93
Author(s):  
Kokila A. Parmar ◽  
Sarju N. Parajapati
Keyword(s):  
Antimicrobial Activity ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Schiff’S Base ◽  
Mass Spectral ◽  
H Nmr ◽  
Diffusion Technique ◽  
Bioactive Agents ◽  
C Nmr ◽  
Anhydrous Zinc Chloride

Thiazolidin-4-one is a versatile lead molecule for designing potential bioactive agents. An expeditious method for preparation of 4-thiazolidinones 7(a-h) are an important class of heterocycles, having potential biological importance due to their unique features. The process of convert of imine (Schiff’s base) to 4-thiazolidinone through an intermediate of THF mercapto acetic acid with anhydrous zinc chloride is important synthetic method for preparation of 4-thiazolidinone. The structures of the synthesized compounds were confirmed by IR, 1H-NMR, 13C NMR and Mass spectral studies. The compounds were screened for their antimicrobial activity against Bacillus subtilis, Staphylococcus aureus, Esherichia coli and Pseudomonas aeruginosa was determined by disc diffusion technique. All the synthesized compounds exhibited promising antimicrobial activity against the studied set of microorganisms.

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