scholarly journals Synthesis and Biological Evaluation of New N-Acyl-α-amino Ketones and 1,3-Oxazoles Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 5019
Author(s):  
Theodora-Venera Apostol ◽  
Luminita Gabriela Marutescu ◽  
Constantin Draghici ◽  
Laura-Ileana Socea ◽  
Octavian Tudorel Olaru ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Large Family ◽  
Biological Evaluation ◽  
Reversed Phase ◽  
Bioactive Substances ◽  
Nmr Data ◽  
In Silico Studies ◽  
Ft Ir ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

In order to develop novel bioactive substances with potent activities, some new valine-derived compounds incorporating a 4-(phenylsulfonyl)phenyl fragment, namely, acyclic precursors from N-acyl-α-amino acids and N-acyl-α-amino ketones classes, and heterocycles from the large family of 1,3-oxazole-based compounds, were synthesized. The structures of the new compounds were established using elemental analysis and spectral (UV-Vis, FT-IR, MS, NMR) data, and their purity was checked by reversed-phase HPLC. The newly synthesized compounds were evaluated for their antimicrobial and antibiofilm activities, for toxicity on D. magna, and by in silico studies regarding their potential mechanism of action and toxicity. The 2-aza-3-isopropyl-1-[4-(phenylsulfonyl)phenyl]-1,4-butanedione 4b bearing a p-tolyl group in 4-position exhibited the best antibacterial activity against the planktonic growth of both Gram-positive and Gram-negative strains, while the N-acyl-α-amino acid 2 and 1,3-oxazol-5(4H)-one 3 inhibited the Enterococcus faecium biofilms. Despite not all newly synthesized compounds showing significant biological activity, the general scaffold allows several future optimizations for obtaining better novel antimicrobial agents by the introduction of various substituents on the phenyl moiety at position 5 of the 1,3-oxazole nucleus.

Synthesis and biological evaluation of some new pyrimidine bearing 2,5-disubstituted 1,3,4-oxadiazole derivatives as cytotoxic agents

2016 ◽  
Vol 42 (2) ◽  
Author(s):  
Betül Kaya ◽  
Zafer Asım Kaplancıklı ◽  
Leyla Yurttaş ◽  
Gülşen Akalın Çiftçi
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Cytotoxic Agents ◽  
Phenacyl Bromide ◽  
Cytotoxic Activities ◽  
Pyridine Moiety ◽  
Oxadiazole Derivatives ◽  
Ft Ir ◽  
New Compounds ◽  
Synthesis And Biological Evaluation

AbstractObjective:As a result of adverse effects including drug-resistance, toxicity and low bioavailability, there has been a crucial need for novel anticancer agents. In this present study, some novel 2,5-disubstituted 1,3,4-oxadiazole derivatives bearing pyridine moiety were synthesized and their potential cytotoxic activities were examined.Materials and methods:A series of seven new compounds of 2-[(5-(3-(pyrimidin-2-yl)thio)propyl)-1,3,4-oxadiazol-2-yl)thio)]-1-(4-substituted)ethan-1-one derivatives were synthesized by reacting 5-[(3-(pyrimidin-2-yl)thio)propyl]-1,3,4-oxadiazole-2-thiol and 4-substituted phenacyl bromide derivatives in acetone with potassium carbonate. The structures of the obtained compounds were elucidated using FT-IR,Results:Among the tested compounds, compoundConclusions:It was determined that some of synthesized compounds had considerable anticancer activity against the A549 cell lines. Compound

scholarly journals Synthesis and Biological Evaluation of Novel Piperazine Containing Hydrazone Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-7 ◽  
Author(s):  
Betül Kaya ◽  
Yusuf Özkay ◽  
Halide Edip Temel ◽  
Zafer Asım Kaplancıklı
Keyword(s):  
Aromatic Aldehydes ◽  
Biological Evaluation ◽  
Standard Drug ◽  
H Nmr ◽  
Chemical Structures ◽  
Ft Ir ◽  
Inhibition Potency ◽  
New Compounds ◽  
Synthesis And Biological Evaluation ◽  
C Nmr

Some hydrazone derivatives were synthesized and their potential anticholinesterase activities were examined. A series of eleven new compounds of N′-(2,4-disubstitutedbenzylidene)-2-(4-(4-nitrophenyl)piperazin-1-yl)acetohydrazide derivatives were obtained via reaction of 2-[4-(4-nitrophenyl)piperazin-1-yl]acetohydrazide with aromatic aldehydes. The chemical structures of the compounds were enlightened by FT-IR,1H-NMR,13C-NMR, and HRMS (ESI) spectral data. The inhibition potency of the compounds3a–kagainst AChE and BuChE was measured and evaluated using a modification of Ellman’s spectrophotometric method. Among the tested compounds, compound3cwas assigned to be the most active derivative. Galantamine was used as a standard drug.

scholarly journals Synthesis and biological evaluation of triphenyl-imidazoles as a new class of antimicrobial agents

2018 ◽  
Vol 9 (4) ◽  
pp. 369-374 ◽  
Author(s):  
Anupam Anupam ◽  
Mohammed Al-Bratty ◽  
Hassan Ahmad Alhazmi ◽  
Shamim Ahmad ◽  
Supriya Maity ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Dilution Method ◽  
Serum Glutamic Oxaloacetic Transaminase ◽  
Active Compounds ◽  
Lead Compounds ◽  
New Class ◽  
Diffusion Technique ◽  
Ft Ir

Newer triphenyl-imidazole derivatives (4a-h) were synthesized in good yields by the reaction of benzil and substituted benzaldehydes in equimolar quantities and refluxing the product with acetyl chloride thereafter. Structures were confirmed by using FT-IR, 1H NMR and 13C NMR spectroscopic methods. All the synthesized compounds were tested for their antimicrobial activity using agar diffusion technique against Gram positive (Staphhylococcus aureus and Bacillus subtilis), Gram negative (Escherichia coli and Pseudomonas aureginosa) as well as Fungal strain (Candida albicans). Interestingly compounds 4a, 4b, 4f and 4h showed significant antibacterial activity, whereas compound 4b was found to have remarkable activity against the fungal strain. The Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC) of most active compounds were determined by broth dilution method and compound 4b emerged to have potent activities against most of the strains having MIC in the range of 25-200 µg/mL. To check the possible toxicities of the most active compounds, they were orally administered in rats and the concentration of liver enzymes serum glutamic-oxaloacetic transaminase (SGOT), serum glutamic pyruvic transaminase (SGPT) and alkaline phosphatase (ALKP) were determined. Compound 4h showed significant increase in the enzymes level depicting the hepatotoxicity. The structure-activity relationship studies showed the importance of electron withdrawing groups at the distant phenyl ring at ortho and para positions as the compounds having chloro or nitro at these positions tend to be more active than the compounds with electron releasing groups such as methoxy. These compounds may act as lead compounds for further studies and appropriate modification in their structure may lead to agents having high efficacy with lesser toxicity.

scholarly journals New Benzoxazole Derivatives as Antiprotozoal Agents: In Silico Studies, Synthesis, and Biological Evaluation

2021 ◽  
Vol 2021 ◽  
pp. 1-11
Author(s):  
Mohamed A. Abdelgawad ◽  
Mohammad M. Al-Sanea ◽  
Mohamed A. Zaki ◽  
Enas I. A. Mohamed ◽  
Shabana I. Khan ◽  
...  
Keyword(s):  
Antimicrobial Agents ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Docking Study ◽  
Antimicrobial Activities ◽  
Biological Evaluation ◽  
Molecular Docking Study ◽  
Chromatographic Separations ◽  
Major Mechanism ◽  
In Silico Studies

Background. Benzoxazole derivatives have different biological activities. In pursuit of designing novel chemical entities with antiprotozoal and antimicrobial activities, benzoxazolyl aniline was utilized as a privileged scaffold of a series of (3-benzoxazole-2-yl) phenylamine derivatives, 3-benzoxazoloyl acetamide, and butyramide derivatives. Methods. These novel analogs were synthesized in straightforward simple chemistry without any quantitative chromatographic separations in reasonable yields. The biological evaluation of all target compounds as potential antimalarial, antileishmanial, antitrypanosomal, and antimicrobial agents was performed by various well-established cell-based methods. Results. Compounds 6d and 5a showed promising biological screening data. The amidation of 3-benzoxazolyl aniline 1 with the chloroacetyl functional group resulted in a good antimalarial activity and showed moderate inhibitory activities against leishmanial and trypanosomal spp. Moreover, chloroacetyl functionalization of benzoxazolyl aniline serves as a good early goal for constructing and synthesizing new antimicrobial and antiprotozoal agents. The molecular docking study rationalizes the relative inhibitory activity of compound 5a as an antimalarial agent with the deregulation of PfPNP activity which has emerged as a major mechanism of these targets.

ROOM TEMPERATURE SYNTHESIS AND BIOLOGICAL EVALUATION OF SOME 2,5-DISUBSTITUTED-1,3,4-OXADIAZOLES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (05) ◽  
pp. 11-15
Author(s):  
R. R Somani ◽  
◽  
P. K Chaskar ◽  
P. M. Patil
Keyword(s):  
Heterocyclic Compounds ◽  
Room Temperature ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Spectroscopic Techniques ◽  
Temperature Synthesis ◽  
Room Temperature Synthesis ◽  
Synthetic Reactions ◽  
Resistant Strains ◽  
Synthesis And Biological Evaluation

One of the principles of green chemistry emphasises on minimisation of environmental and economic impacts by developing synthetic reactions at ambient temperature and pressure.The rise of resistant strains of microorganisms is an issue of regularly expanding seriousness. Therefore, the development of new antimicrobial agents will remain a challenge for chemists. we herein report room temperature synthesis of newer heterocyclic compounds belonging to 1,3,4-oxadiazole scaffold. Their structures were confirmed using various spectroscopic techniques. These compounds were evaluated for antifungal, antibacterial and antitubercular activities.

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