scholarly journals Antifungal Activity of New Eugenol-Benzoxazole Hybrids against Candida spp.

2017 ◽  
Vol 2017 ◽  
pp. 1-8 ◽  
Author(s):  
Larissa Incerti Santos de Carvalho ◽  
Dalila Junqueira Alvarenga ◽  
Letícia Cruz Ferreira do Carmo ◽  
Lucas Gomes de Oliveira ◽  
Naiara Chaves Silva ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Candida Spp ◽  
Design Synthesis ◽  
Human Blood Cells ◽  
Wide Range ◽  
Synthetic Sequence ◽  
Derivatives Of ◽  
Aromatic Nitration

Eugenol is a natural allylphenol responsible for a wide range of biological activities, especially antimicrobial. Benzoxazoles are heterocycles with recognized antimicrobial activities. This paper describes the design, synthesis, and the biological results for benzoxazole type derivatives of eugenol as antifungal agents. The products were obtained in good yields by a four-step synthetic sequence involving aromatic nitration, nitroreduction, amide formation, and cycle condensation. They were evaluated against species of Candida spp. in microdilution assays, and four products (5a, 5b′, 5c, and 5d′) were about five times more active than eugenol against C. albicans and C. glabrata. Two of them (5b′ and 5d′) showed good activity against C. krusei, a species which is naturally resistant to fluconazole. Furthermore, the active products were more selective than eugenol against human blood cells, showing that they are interesting substances for further optimization.

scholarly journals SYNTHESIS OF TRANSITION METAL ION COMPLEX OF 2- AMINOBENZOXAZOLE AND ANTIFUNGAL ACTIVITY AND ROLE IN PHARMACEUTICAL CHEMISTRY

2020 ◽  
Vol 4 (12) ◽  
pp. 60-64
Author(s):  
Indu Raj ◽  
Dr.Smt. Manjul Shrivastava
Keyword(s):  
Antifungal Activity ◽  
Metal Ion ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Pharmaceutical Chemistry ◽  
Molar Ratio ◽  
Ligand Complex ◽  
Wide Range ◽  
Ft Ir ◽  
Derivatives Of

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.

Design, Synthesis, Anti-Proliferative Evaluation and Cell Cycle Analysis of Hybrid 2-Quinolones

2019 ◽  
Vol 19 (9) ◽  
pp. 1132-1140
Author(s):  
Heba A.E. Mohamed ◽  
Hossa F. Al-Shareef
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Biological Activities ◽  
Flow Cytometric Analysis ◽  
Annexin V ◽  
Cytotoxic Activities ◽  
Significant Group ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range

Background: Quinolones are a significant group of nitrogen heterocyclic compounds that exist in therapeutic agents, alkaloids, and synthetic small molecules that have important biological activities. A wide range of quinolones have been used as antituberculosis, antibacterial, anti-malarial, antifungal, anticonvulsant, anticancer agents and urease inhibitors. Methods: Ethyl 3,3-disubstituted-2-cyano propionates containing hybride quinolones derivatives were synthesized by the reaction of 1-amino-7-hydroxy-4-methylquinolin-2(1H)-one and its dibromo derivative with α, β-unsaturated carbonyl in ethanol. Results: A novel series of hybrid 2-quinolone derivatives was designed and synthesized. The compounds structures were confirmed using different spectroscopic methods and elemental analysis. The cytotoxic activities of all the compounds were assessed against HepG2 cell line in comparison with doxorubicin as a standard drug. Conclusion: Most compounds revealed superior anti-proliferative activity than the standard. Compound 4b, is the most active compound (IC50 = 0.39mM) compared with doxorubicin (IC50 = 9.23mM). DNA flow cytometric analysis of compound 4b showed cell cycle arrest at G2/M phase with a concomitant increase of cells in apoptotic phase. Dual annexin-V/ propidium iodide staining assay of compound 4b revealed that the selected candidate increased the apoptosis of HepG-2 cells more than control.

scholarly journals Synthesis, Antiproliferative Activity and Radical Scavenging Ability of 5-O-Acyl Derivatives of Quercetin

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1608
Author(s):  
Stephen Lo ◽  
Euphemia Leung ◽  
Bruno Fedrizzi ◽  
David Barker
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Breast Cancer Cell Lines ◽  
Scavenging Activity ◽  
Plant Materials ◽  
Wide Range ◽  
Derivatives Of ◽  
Acyl Derivatives

Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5-O-acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines; and their radical scavenging activity against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.

Identification of promising objects for the synthesis of thiosulphonate derivatives of benzoquinone and hydroquinone

2021 ◽  
Vol 4 (2) ◽  
pp. 47-53
Author(s):  
N. Y. Monka ◽  
◽  
N. E. Stadnytska ◽  
I. R. Buchkevych ◽  
K. O. Kaplia ◽  
...  
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Experimental Studies ◽  
New Drugs ◽  
Reduced Form ◽  
Free Form ◽  
Wide Range ◽  
On Line ◽  
Living Organisms ◽  
Derivatives Of

Benzoquinone and its reduced form hydroquinone belong to phenolic compounds and are found in living organisms in free form or in glycosides. They are active substances of some medicinal plants and have a pharmacological effect on the human body. Accordingly, their derivatives are important objects for chemical synthesis and development of new drugs. This article presents the findings of the structural design of substances with benzoquinone or hydroquinone fragment and sulfur-containing compound. By use of appropriate on-line programs a predictive screening of the biological activity and cytotoxicity of thiosulfonate derivatives of benzoquinone and hydroquinone has been conducted. It has been found that they have immense methodological potential to be synthesized by substances with a wide range of biological activities and a high value of probable activity, which substantiates the feasibility of conducting experimental studies on their biological activity, particularly anticancer.

Steroidal pyrazolines as a promising scaffold in drug discovery

2020 ◽  
Vol 12 (10) ◽  
pp. 949-959
Author(s):  
Ranju Bansal ◽  
Ranjit Singh
Keyword(s):  
Drug Discovery ◽  
Broad Spectrum ◽  
Chemical Reactivity ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Review Article ◽  
Pharmacological Activities ◽  
Neuroprotective Effects ◽  
Wide Range

Steroidal pyrazolines constitute an interesting and promising scaffold for drug discovery as they display diverse chemical reactivity and a wide range of biological activities. Literature reports indicate potent anticancer potential of steroidal pyrazolines along with broad-spectrum antimicrobial activities. Strong neuroprotective effects with steroids possessing pyrazoline moiety have also been observed. Among all the therapeutically active steroidal pyrazolines, D-ring-substituted derivatives are highly potent and the least toxic. The current and futuristic research approaches in this area are focused towards the exploration of this promising scaffold to develop molecules with widespread pharmacological activities. This review article mainly covers the synthetic and pharmacological aspects of steroidal pyrazolines, which will assist the medicinal chemists working in this area in their scientific endeavors.

scholarly journals Plant thionins: structure, biological functions and potential use in biotechnology

2018 ◽  
Vol 22 (6) ◽  
pp. 667-675 ◽  
Author(s):  
T. I. Odintsova ◽  
M. P. Slezina ◽  
E. A. Istomina
Keyword(s):  
Pathogenic Bacteria ◽  
Plant Pathogens ◽  
Biological Activities ◽  
Three Dimensional ◽  
Amino Acid Sequences ◽  
Lipid Transfer ◽  
Human Pathogens ◽  
Candida Spp ◽  
Wide Range ◽  
Bacteria And Fungi

Antimicrobial peptides (AMPs) are important components of defense system in both plants and animals. They represent an ancient mechanism of innate immunity providing rapid first line of defense against pathogens. Plant AMPs are classified into several families: thionins, defensins, nonspecific lipid-transfer proteins, hevein- and knottin-type peptides, hairpinins and macrocyclic peptides (cyclotides). The review focuses on the thionin family. Thionins comprise a plant-specific AMP family that consists of short (~5 kDA) cysteine-rich peptides containing 6 or 8 cysteine residues with antimicrobial and toxic properties. Based on similarity in amino acid sequences and the arrangement of disulphide bonds, five structural classes of thionins are discriminated. The three-dimensional structures of a number of thionins were determined. The amphipathic thionin molecule resembles the Greek letter Г, in which the long arm is formed by two antiparallel α-helices, while the short one, by two parallel β-strands. The residues responsible for the antimicrobial activity of thionins were identified. Thionins are synthesized as precursor proteins consisting of a signal peptide, the mature peptide region and the C-terminal prodomain. Thionins protect plants from pathogenic bacteria and fungi acting directly on the membranes of microorganisms at micromolar concentrations, although their precise mode of action remains unclear. In addition to plant pathogens, thionins inhibit growth of a number of human pathogens and opportunistic microorganisms, such as Candida spp., Saccharomyces cerevisiae, Fusarium solani, Staphylococcus aureus and Escherichia coli. Thionins are toxic to different types of cells including mammalian cancer cell lines. Transgenic plants expressing thionin genes display enhanced resistance to pathogens. A wide range of biological activities makes thionins promising candidates for practical application in agriculture and medicine.

scholarly journals Design, synthesis and evaluation of hydrazine and acyl hydrazone derivatives of 5-pyrrolidin-2-one as antifungal agents

2020 ◽  
Vol 30 (13) ◽  
pp. 127220
Author(s):  
Anca-Elena Dascalu ◽  
Alina Ghinet ◽  
Emmanuelle Lipka ◽  
Christophe Furman ◽  
Benoît Rigo ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Design Synthesis ◽  
Acyl Hydrazone ◽  
Derivatives Of

Synthesis and Reactions of Perimidines and Their Fused Systems

2020 ◽  
Vol 24 (15) ◽  
pp. 1669-1716 ◽  
Author(s):  
Thoraya A. Farghaly ◽  
Sami A. Al-Hussain ◽  
Zeinab A. Muhammad ◽  
Magda A. Abdallah ◽  
Magdi E. A. Zaki
Keyword(s):  
Chemical Reactions ◽  
Heterocyclic Compounds ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Lone Pair ◽  
Pharmacological Activities ◽  
Synthetic Analogs ◽  
Interesting Class ◽  
Derivatives Of

Perimidines are peri-naphtho-fused derivatives of pyrimidine. They are of particular interest as they are a rare example of an azine in which the lone pair of electrons of pyrrole-like nitrogen participates in the π-system of the molecule. Perimidine is an interesting class of heterocyclic compounds. Various synthetic analogs of perimidines have been prepared and evaluated for many pharmacological activities in different models with desired findings. They exhibit biological activities as antitumor, antiulcer, antimicrobial, and antifungal agents. This review is an attempt to organize the synthesis and chemical reactions of perimidine analogs reported to date systematically since 1955. It should be noted that this review is the first one that includes the preparation and reactions of the perimidine ring.

Benzoylthioureas: Design, Synthesis and Antimycobacterial Evaluation

2020 ◽  
Vol 16 (1) ◽  
pp. 93-103
Author(s):  
Tiago O. Brito ◽  
Lethícia O. Abreu ◽  
Karen M. Gomes ◽  
Maria C.S. Lourenço ◽  
Patricia M.L. Pereira ◽  
...  
Keyword(s):  
Benzene Ring ◽  
Biological Activities ◽  
Antitubercular Activity ◽  
Antimycobacterial Activity ◽  
New Drugs ◽  
Design Synthesis ◽  
Thiourea Derivatives ◽  
Structural Modifications ◽  
General Series ◽  
Wide Range

Background: New drugs and strategies to treat tuberculosis (TB) are urgently needed. In this context, thiourea derivatives have a wide range of biological activities, including anti-TB. This fact can be illustrated with the structure of isoxyl, an old anti-TB drug, which has a thiourea as a pharmacophore group. Objective: The aim of this study is to describe the synthesis and the antimycobacterial activity of fifty-nine benzoylthioureas derivatives. Methods: Benzoylthiourea derivatives have been synthesized and evaluated for their activity against Mycobacterium tuberculosis using the MABA assay. After that, a structure-activity relationship study of this series of compounds has been performed. Results and Discussion: Nineteen compounds exhibited antimycobacterial activity between 423.1 and 9.6 μM. In general, we observed that the presence of bromine, chlorine and t-Bu group at the para-position in benzene ring plays an important role in the antitubercular activity of Series A. These substituents were fixed at this position in benzene ring and other groups such as Cl, Br, NO2 and OMe were introduced in the benzoyl ring, leading to the derivatives of Series B. In general, Series B was less cytotoxic than Series A, which indicates that the presence of a substituent at benzoyl ring contributes to an improvement in both antimycobacterial activity and toxicity profiles. Conclusion: Compound 4c could be considered a good prototype to be submitted to further structural modifications in the search for new anti-TB drugs, since it is 1.8 times more active than the first line anti-TB drug ethambutol and 0.65 times less active than isoxyl.

scholarly journals Functionalized Derivatives of Benzo-Crown Ethers. Part 4. Antifungal Macrocyclic Supramolecular Complexes of Transition Metal Ions Acting as Lanosterol-14-α -Demethylase Ihibitors

1999 ◽  
Vol 6 (2) ◽  
pp. 101-110 ◽  
Author(s):  
Mihai Barboiu ◽  
Claudiu T. Supuran ◽  
Andrea Scozzafava ◽  
Cornelia Guran ◽  
Paula Diaconescu ◽  
...  
Keyword(s):  
Metal Ions ◽  
Coordination Compounds ◽  
Antifungal Agents ◽  
Transition Metal Ions ◽  
Supramolecular Complexes ◽  
Amino Groups ◽  
Candida Spp ◽  
Physico Chemical ◽  
Antifungal Action ◽  
Derivatives Of

Poly- and mononuclear metal complexes of 2,3,11,12-bis[4-(10-aminodecylcarbonyl)]benzo-18- crown-6 (L) and Cu(II); Ni(II); Co(II) and Cr(III) have been synthesized and characterized by standard physico-chemical procedures. In the newly prepared complexes the crown moiety oxygen atoms of the macrocyclic host did not generally interact with metal ions, whereas the two amino groups of the ligand always did. Several of the newly synthesized compounds act as effective antifungal agents against Aspergillus and Candida spp., some of them showing activities comparable to ketoconazole, with minimum inhibitory concentrations in the range of 0.3−0.5 μg/mL . The mechanism of antifungal action of these coordination compounds is probably connected to an inhibition of lanosterol-14-α -demethylase, a metallo-enzyme playing a key role in sterol biosynthesis in fungi, bacteria and eukariotes.

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