scholarly journals New bioactive triaryl triglyceride esters: Synthesis, characterization and biological activities

2018 ◽  
Vol 13 (4) ◽  
pp. 302
Author(s):  
Tanzila Arshad ◽  
Hamdullah Khadim Sheikh ◽  
Mehdi Hassan Kazmi ◽  
Sadia Farheen ◽  
Tehmina Sohail ◽  
...  

<p class="Abstract">Four new bioactive aryl triester derivatives of glycerol and benzoic acids were synthesized. The synthetic compounds were studied for their antimicrobial and urease inhibition activities. Esterification was carried out by using carbonyldiimidazole to enhance the acyl elimination addition reaction with benzoic acid derivatives. The structure of triglycerides were studied by EI-MS, <sup>1</sup>H, <sup>13</sup>C-NMR, FT-IR and elemental analysis. All synthetic compounds showed urease inhibition activity with highest value of IC<sub>50 </sub>value 22.4 ± 0.45 μM which is nearest to standard thiourea IC<sub>50 </sub>value (21.6 ± 0.12 μM).  Except compound (3d), all other compounds exhibited antimicrobial activity against <em>Streptococcus pneumoniae, Staphylococcus epidermidis, Bacillus pumilus, Escherichia coli, Pseudomonas aeruginosa</em> and <em>Candida albican</em>.</p><p><strong>Video Clip of Methodology:</strong></p><p>7 min 59 sec   <a href="https://youtube.com/v/PvGTYUxO7-4">Full Screen</a>   <a href="https://youtube.com/watch?v=PvGTYUxO7-4">Alternate</a>  </p>

2017 ◽  
Vol 12 (2) ◽  
pp. 20 ◽  
Author(s):  
Dhineshkumar Manoharan ◽  
Kannan Kulanthai ◽  
Gnanavel Sadhasivam ◽  
Vijayan Raji ◽  
Paalvannan Thayumanavan

<p class="Abstract">Series of indoline derivatives were synthesized using N-(4-aminophenyl)indoline-1-carbothiamide as a precursor. The confirmation of synthesized compounds was done by <sup>1</sup>H-NMR, <sup>13</sup>C-NMR, LC-MS (ESI) and FT-IR. In vitro antidiabetic activity of synthesized indoline derivatives were examined by standard α-amylase inhibition assay. The compounds 4a (IC<sub>50 </sub>= 52.1 µg/mL) and 4b (IC<sub>50 </sub>= 57.7 µg/mL) showed potent α-amylase inhibition activity. The compounds 3a (IC<sub>50 </sub>= 62.2 µg/mL) and 3b (IC<sub>50 </sub>= 60.7 µg/mL) showed moderate antidiabetic activity.</p><p class="Abstract"><strong>Video Clip of Methodology</strong>:</p><p class="Abstract">19 min 21 sec   <a href="https://www.youtube.com/v/k5WdfpM-E8U">Full Screen</a>   <a href="https://www.youtube.com/watch?v=k5WdfpM-E8U">Alternate</a></p>


2013 ◽  
Vol 78 (8) ◽  
pp. 1127-1134 ◽  
Author(s):  
Ghulam Fareed ◽  
Nighat Afza ◽  
Ali Versiani ◽  
Nazia Fareed ◽  
Rasheed Mughal ◽  
...  

A series of 4-aryl methylidene-2-phenyl/methyl-5-(4H)-oxazolone derivatives (2-7) have been synthesized using the reported method by condensation of aldehydes with N-benzoyl / N-acetyl glycine in the presence of zinc oxide as a catalyst and acetic anhydride at room temperature in ethanol. The compounds (2-6) are new derivatives. The structures of compounds were evaluated on the basis of 1H-NMR, 13C-NMR, EIMS, FT-IR and elemental analysis. All the compounds were screened for their antibacterial and urease inhibition activity. Antibacterial activity was tested by agar well diffusion method using Mueller Hinton Agar medium. Compound (2) showed excellent activity against S. aureus which has 16 mm (80%) inhibition and above 24 mm (70%) against S. typhi. The most active compound against E. coli was compound (6) having 20 mm (80%) inhibition followed by compound (5) having above 18 mm (70%) inhibition. Urease inhibition activity of all the compounds was determined by indophenol method. Compounds (3, 6) and (7) showed significant inhibition against Jacks bean urease.


Author(s):  
Indu Raj ◽  
Dr.Smt. Manjul Shrivastava

In view of the fact that a large number of derivatives of benzoxazole have been found toexhibit a wide variety of antimicrobial activities. Heterocyclic compounds play an importantrole in medicinal chemistry and exhibit wide range of biological activities in pharmaceuticalchemistry. Complexes of 2-aminobenzoxazole (L) with chloride of iron (II), was synthesized.The molar ratio metal: ligand in the reaction of the complex formation was 1:2. It should benoticed, that the reaction of all the metal salts yielded bis (ligand) complex of the generalformula M (L) 2(CL) 2. The complex was characterized by elemental analysis, melting point,FT-IR, 1H NMR, spectral data. The antifungal activity against different fungai, A.niger,A.flavus, Fusarium oxysporum, paecilomyces variotii, C.albicans.


2013 ◽  
Vol 2013 ◽  
pp. 1-6
Author(s):  
Awaz Jamil Hussein ◽  
Hashim Jalal Azeez

A number of derivatives of 2-(substituted phenyl)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl) thiazolidin-4-one (3a–j) have been synthesized from the reaction of 4-(6-methylbenzo[d]thiazol-2-yl)benzenamine(1), with different substituted benzaldehydes (2a–j), followed by cyclocondensation reaction of the prepared imines with 2-meraptoacetic acid in high yields. Furthermore, the structures of the newly synthesized compounds were confirmed by FT-IR,13C-NMR,13C-DEPT, and1H-NMR spectral data. The imines and thiazolidin-4-one derivatives were evaluated for their antibacterial activity againstEscherichia colias gram negative andStaphylococcus aureusas gram positive, the results have shown significant activity against both types of bacteria.


2020 ◽  
Vol 38 (3B) ◽  
pp. 128-141
Author(s):  
Nadia A. Betti ◽  
Redha Ib. Hussain ◽  
Sahar Ab. Kadhem

New derivatives of pyrrolidine-2-one have been synthesized through lactamization of γ –butyrolactone (GBL) by hydrazine hydrate (80%), ethylene diamine and ethanol amine to afford compounds (1-aminopyrrolidin-2-one), (1-(2-aminoethyl)pyrrolidine-2-one) and (1-(2-hydroxyethyl)pyrrolidine-2-one), respectively. Compound (1-aminopyrrolidin-2-one) underwent several reactions to synthesize the rest of these derivatives. All synthesized compounds were approved by their FT-IR, 1H-NMR and some by Mass spectra. The biological activities of these derivatives were evaluated against Escherichia coli and Staphylococcus aureus. Many of these derivatives showed moderate biological activity against one or both kind of bacteria in comparison to amoxicillin and some showed no biological activity at all.


2017 ◽  
Vol 12 (2) ◽  
pp. 25 ◽  
Author(s):  
Aamer Saeed ◽  
Danish Shahzad ◽  
Fayaz Ali Larik ◽  
Pervaiz Ali Channar ◽  
Haroon Mahfooz ◽  
...  

<p>A series of 4-aryl-2,6-dimethyl-3,5-bis-N-(aryl)-carbamoyl-1,4-dihydropyri-dines 6a-6h were prepared by using the one-pot three component synthetic method. The target compounds 6a-6h were synthesized by reacting two molar equivalents of ketone functionality and one mole of aromatic aldehydes in ammonium acetate to obtain the desired products. The structures of newly synthesized compounds were characterized by FT-IR, 1H-NMR, 13C-NMR, and elemental analysis. All the synthesized compounds were screened for their elastase inhibition and antioxidant activity. Almost all of the com-pounds 6a-h showed good to excellent activities against elastase enzyme more than the reference drug. Compounds 6d and 6b at 0.2 ± 0.0 µM and 0.2 ± 0.0 µM were found to most potent derivatives against elastase enzyme. Compound 6a exhibited prominent free radical scavenging activity. From the results of the biological activity, we infer that some derivatives can serve as lead molecules in pharmacology.</p><p><strong>Video Clip of Methodology</strong>:</p><p>3 min 13 sec   <a href="https://youtube.com/v/gPLdpGpZhR8">Full Screen</a>   <a href="https://youtube.com/watch?v=gPLdpGpZhR8">Alternate</a></p>


2020 ◽  
Vol 23 (4) ◽  
pp. 5-12
Author(s):  
Nadia A. Betti ◽  
◽  
Redha Ib. Hussain ◽  
Sahar Ab. Kadhem ◽  
Abdul Jabar Kh. Atia ◽  
...  

New derivatives of pyrrolidine-2-one have been prepared by lactamization of -butyrolactone GBL with hydrazine hydrate (NH2NH2(80%)) to afford (1-aminopyrrolidin-2-one) which undergo many reactions to prepare the other derivatives. The prepared derivatives were determined by utilizing their FT-IR,1H-NMR and some by Mass spectrum. These derivatives were evaluated biologically against (Staphylococcus aureusand E. coli).Some of these derivatives exhibited good biological activity against one or both kind of bacteria while some exhibited no biological activity at all.


2017 ◽  
Vol 12 (6) ◽  
pp. 1934578X1701200 ◽  
Author(s):  
Edgar Caamal-Fuentes ◽  
Daniel Robledo ◽  
Yolanda Freile-Pelegrín

Crude and alkali treated carrageenan from the cultivated marine alga Solieria filiformis (Rhodophyta) were obtained, characterized and evaluated for their cytotoxic and antiprotozoal activities. Yields, molecular weights and chemical composition of carrageenans were determined. Their structures were elucidated through spectroscopic techniques including FT-IR and CP-MAS 13C NMR spectra. Crude and alkali treated carrageenan seems to be chemically similar to the iota-family carrageenan. Crude carrageenan showed antiprotozoal activity against Giardia intestinalis.


2019 ◽  
Author(s):  
Chem Int

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.


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