scholarly journals Synthesis and Evaluation of in Vitro Biological Activity of 4-Substituted Arylpiperazine Derivatives of 1,7,8,9-Tetrachloro-10,10-dimethoxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione

Molecules ◽  
2009 ◽  
Vol 14 (12) ◽  
pp. 5189-5202 ◽  
Author(s):  
Jerzy Kossakowski ◽  
Magdalena Pakosinska-Parys ◽  
Marta Struga ◽  
Izabela Dybala ◽  
Anna Koziol ◽  
...  
Keyword(s):  
Biological Activity ◽  
Derivatives Of

Phosphoramidate Derivatives of AZT as Inhibitors of HIV: Studies on the Carboxyl Terminus

1993 ◽  
Vol 4 (2) ◽  
pp. 97-101 ◽  
Author(s):  
C. McGuigan ◽  
R. N. Pathirana ◽  
S. S.-M. Choi ◽  
D. Kinchington ◽  
T. J. O'Connor
Keyword(s):  
Amino Acids ◽  
Biological Activity ◽  
Carboxyl Terminus ◽  
Amino Ester ◽  
Carboxy Terminus ◽  
Free Nucleotides ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Ester Lead

Novel phosphoramidate derivatives of the anti-HIV nucleoside analogue AZT have been prepared by phosphorochloridate chemistry. These materials carry carboxy-protected, amino acids, and are designed to act as membrane-soluble prodrugs of the bio-active free nucleotides. In vitro evaluation revealed the compounds to have a pronounced, selective antiviral activity. In particular, variation in the carboxy terminus region is studied. For alkyl phosphates small changes in the structure of the amino ester lead to marked changes in biological activity. However, for analogous aryl phosphates there is little dependence on the structure of the ester. This suggests a different mechanism of action for these two categories of phosphate prodrug.

scholarly journals Aspergillus flavus as a Model System to Test the Biological Activity of Botanicals: An Example on Citrullus colocynthis L. Schrad. Organic Extracts

Toxins ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 286 ◽  
Author(s):  
Francesca Degola ◽  
Belsem Marzouk ◽  
Antonella Gori ◽  
Cecilia Brunetti ◽  
Lucia Dramis ◽  
...  
Keyword(s):  
Biological Activity ◽  
Aspergillus Flavus ◽  
Folk Medicine ◽  
Inhibitory Effect ◽  
Phytopathogenic Fungus ◽  
Citrullus Colocynthis ◽  
Desert Areas ◽  
Derivatives Of ◽  
Stem Leaf

Citrullus colocynthis L. Schrader is an annual plant belonging to the Cucurbitaceae family, widely distributed in the desert areas of the Mediterranean basin. Many pharmacological properties (anti-inflammatory, anti-diabetic, analgesic, anti-epileptic) are ascribed to different organs of this plant; extracts and derivatives of C. colocynthis are used in folk Berber medicine for the treatment of numerous diseases—such as rheumatism arthritis, hypertension bronchitis, mastitis, and even cancer. Clinical studies aimed at confirming the chemical and biological bases of pharmacological activity assigned to many plant/herb extracts used in folk medicine often rely on results obtained from laboratory preliminary tests. We investigated the biological activity of some C. colocynthis stem, leaf, and root extracts on the mycotoxigenic and phytopathogenic fungus Aspergillus flavus, testing a possible correlation between the inhibitory effect on aflatoxin biosynthesis, the phytochemical composition of extracts, and their in vitro antioxidant capacities.

scholarly journals The Search for New Antibacterial Agents among 1,2,3-Triazole Functionalized Ciprofloxacin and Norfloxacin Hybrids: Synthesis, Docking Studies, and Biological Activity Evaluation

2021 ◽  
Vol 90 (1) ◽  
pp. 2
Author(s):  
Halyna Hryhoriv ◽  
Illia Mariutsa ◽  
Sergiy M. Kovalenko ◽  
Victoriya Georgiyants ◽  
Lina Perekhoda ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Biological Activity ◽  
Antibacterial Agents ◽  
Docking Studies ◽  
Synthetic Method ◽  
Bacillus Subtilis Atcc ◽  
Resistant Strains ◽  
Derivatives Of

Among all modern antibiotics, fluoroquinolones are well known for their broad spectrums of activity and efficiency toward microorganisms and viruses. However, antibiotic resistance is still a problem, which has encouraged medicinal chemists to modify the initial structures in order to combat resistant strains. Our current work is aimed at synthesizing novel hybrid derivatives of ciprofloxacin and norfloxacin and applying docking studies and biological activity evaluations in order to find active promising molecules. We succeeded in the development of a synthetic method towards 1,2,3-triazole-substituted ciprofloxacin and norfloxacin derivatives. The structure and purity of the obtained compounds were confirmed by 1H NMR, 13C NMR, 19F NMR, LC/MS, UV-, IR- spectroscopy. Docking studies, together with in vitro research against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Bacillus subtilis ATCC 6633, Pseudomonas aeruginosa ATCC 27853, Candida albicans NCTC 885-653 revealed compounds in which activity exceeded the initial molecules.

Synthesis and In Vitro Biological Activity Evaluation of Novel Imidazo [2,1-B][1,3,4] Thiadiazole as Anti-Alzheimer Agents

2020 ◽  
Vol 17 (5) ◽  
pp. 610-617
Author(s):  
Sara Azimi ◽  
Omidreza Firuzi ◽  
Aida Iraji ◽  
Afsaneh Zonouzi ◽  
Mahsima Khoshneviszadeh ◽  
...  
Keyword(s):  
Biological Activity ◽  
Inhibitory Activity ◽  
Phenyl Ring ◽  
Activity Evaluation ◽  
Butyryl Cholinesterase ◽  
Thiadiazole Derivatives ◽  
Derivatives Of

Background: Considering that AD is multifactorial in nature, novel series of imidazo [2,1-b][1,3,4] thiadiazole derivatives were designed to address the basic factors responsible for the disease. <p> Methods: These compounds were investigated as inhibitors of beta-site APP cleaving enzyme 1, acetylcholinesterase and butyryl cholinesterase. <p> Results: The BACE1 inhibitory results indicated that nitro phenyl substituted derivatives of imidazo [2,1-b][1,3,4] thiadiazole scaffold (R2 = m-NO2) demonstrated superior BACE1 inhibitory activity compared to other substituted moieties. In the BuChE assay, compounds 4h and 4l carrying meta NO2 at R2 of phenyl ring turned out to be potent inhibitors. <p> Conclusion: In conclusion, these novel synthesized derivatives seem to be promising anti-Alzheimer agents.

Synthesis and biological activity of nucleoside analogs involving modifications in the carbohydrate ring

1985 ◽  
Vol 63 (8) ◽  
pp. 2149-2161 ◽  
Author(s):  
Walter A. Szarek ◽  
B. Mario Pinto ◽  
Masaharu Iwakawa
Keyword(s):  
Biological Activity ◽  
Cell Growth ◽  
Antitumor Activity ◽  
Nucleoside Analogs ◽  
Hela Cell Line ◽  
Biological Screening ◽  
Naturally Occurring ◽  
Derivatives Of ◽  
Substituted 1

The synthesis of a variety of nucleoside analogs involving modifications in the carbohydrate ring is described. In particular, 6-substituted purin-9-yl derivatives of 1-oxa-4-thiacyclohexane and 1,4-dioxacyclohexane have been synthesized. A number of 6-chloropurin-9-yl derivatives of substituted 1-oxa-4-thiacyclohexane have also been derived from the parent compounds by way of a Pummerer rearrangement. A route to nucleoside analogs of 1-oxa-4-thiacyclohexane from naturally occurring nucleosides is illustrated for the case of inosine. A route to nucleoside analogs in which the carbohydrate moiety is replaced by an acyclic moiety bearing α,β-unsaturated esters is also illustrated for the case of uridine. The results of biological screening of these analogs and others previously synthesized in our program against leukemia L-1210 cells in vitro are presented; some of these compounds showed marginal antitumor activity. The screening results of selected compounds against the human HeLa cell line in vitro are also presented; none of the compounds that were tested showed significant inhibitory activity of cell growth.

scholarly journals RETRACTED ARTICLE: Further in vitro biological activity evaluation of amino-, thio- and ester-derivatives of avarol

2015 ◽  
Vol 31 (4) ◽  
pp. 684-686
Author(s):  
Giuseppina Tommonaro ◽  
Boris Pejin ◽  
Carmine Iodice ◽  
Antonietta Tafuto ◽  
Salvatore De Rosa
Keyword(s):  
Biological Activity ◽  
Activity Evaluation ◽  
Retracted Article ◽  
Derivatives Of

scholarly journals Syntheses and In Vitro Biological Activity of Some Derivatives of C-9154 Antibiotic

2012 ◽  
Vol 2012 ◽  
pp. 1-6
Author(s):  
Isaac Asusheyi Bello ◽  
George Iloegbulam Ndukwe ◽  
Joseph Olorunju Amupitan ◽  
Rachael Gbekele Ayo ◽  
Francis Oluwole Shode
Keyword(s):  
Biological Activity ◽  
Minimum Inhibitory Concentration ◽  
Functional Group ◽  
Inhibitory Concentration ◽  
2D Nmr ◽  
Esterification Reaction ◽  
New Antibiotics ◽  
Derivatives Of ◽  
Better Than

In our continued attempts at designing new antibiotics based on the structure of the C-9154 antibiotic, to simultaneously improve activity and lower toxicity, an analogue to the C-9154 antibiotic and six derivatives of this analogue were synthesized. The approach was to significantly reduce the polarity of the synthesized analogue in the derivatives to achieve increased permeability across cell membranes by conversion of the highly polar carboxylic group to an ester functional group. The compounds were synthesized using a two-step reaction which involved an additional reaction between benzyl amine and maleic anhydride and then conversion of the terminal carboxylic acid functional group to an ester functional group using a thionyl chloride mediated esterification reaction. The compounds were fully characterized using Infrared, GC-MS, and 1D and 2D NMR experiments. The in vitro biological activity of the compounds showed that the derivatives were more active than the analogues as was anticipated with minimum inhibitory concentration in the range 0.625–5 μg/mL. The analogue had minimum inhibitory concentration in the range 2.5–10 μg/mL. These values are significantly better than that obtained for the original C-9154 antibiotic which had activity in the range 10–>100 μg/mL.

Haloalkyl Phosphate Derivatives of AZT as Inhibitors of HIV: Studies in the Phosphate Region

1994 ◽  
Vol 5 (3) ◽  
pp. 162-168 ◽  
Author(s):  
C. McGuigan ◽  
S. Turner ◽  
S. R. Nicholls ◽  
T. J. O'Connor ◽  
D. Kinchington
Keyword(s):  
Biological Activity ◽  
Alkyl Chain ◽  
Antiviral Action ◽  
Alkyl Phosphate ◽  
Free Nucleotides ◽  
Order Of Magnitude ◽  
Derivatives Of ◽  
Anti Hiv ◽  
Hiv 1

Novel haloalkyl phosphate derivatives of the anti-HIV nucleoside analogue AZT were prepared by phosphorochloridate chemistry. These materials were designed to act as labile membrane-soluble prodrugs of the bio-active free nucleotides. In vitro evaluation revealed the compounds to have a pronounced and selective antiviral action, which varied greatly with the structure of the phosphate moiety. By comparison to simple dialkyl phosphates, which are inactive against HIV-1, the introduction of halogen atoms into the alkyl (phosphate) chains led to anti-HIV activity. Although halogen substitution in just one alkyl chain was sufficient for biological activity, substitution in the second alkyl chain further enhanced activity. Conversely, stabilization of the second chain, by conversion to a phosphonate, led to a reduction in activity. In one case, the diastereo-isomers resulting from mixed stereochemistry at the phosphate centre were separated, and found to differ in activity by one order of magnitude. Lastly, the bis(mono- and di-chloroethyl) phosphates were prepared and found to display moderate anti-HIV activity.

scholarly journals Syntheses and Biological Activity of Some Derivatives of C-9154 Antibiotic

2012 ◽  
Vol 2012 ◽  
pp. 1-7
Author(s):  
Isaac Asusheyi Bello ◽  
George Iloegbulam Ndukwe ◽  
Joseph Olorunju Amupitan ◽  
Rachael Gbekele Ayo ◽  
Francis Oluwole Shode
Keyword(s):  
Biological Activity ◽  
Functional Group ◽  
Marked Effect ◽  
2D Nmr ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
New Antibiotics ◽  
Agricultural Use ◽  
Derivatives Of

This research was undertaken to design several new antibiotics, by structurally modifying the C-9154 antibiotic, simultaneously improving its activity and lowering toxicity. This was achieved by synthesizing an analogue to the C-9154 antibiotic and seven derivatives of this analogue. The approach was to significantly reduce the polarity of the synthesized analogue in the derivatives to achieve increased permeability across cell membranes by conversion of the highly polar carboxylic group to an ester functional group. The compounds were fully characterized using infrared, GC-MS, and 1D and 2D NMR experiments. The in vitro biological activity of the compounds showed that the derivatives were more active than the analogue as was anticipated and both were more active than the standard drugs used for comparison. Work is ongoing to establish applications for the compounds as antiplasmodials, antivirals, anticancers/tumours, antitrypanosomiasis, anthelminthic, and as general antibiotics for human, veterinary, and even agricultural use as they had marked effect on both Gram-positive and Gram-negative bacteria and some fungi.

MEMBRANSTABILIZING ACTIVITY OF HUMIC SUBSTANCES AS THE INTEGRAL INDEX OF THEIR HEPATOPROTECTIVE PROPERTIES

2018 ◽  
Vol 1 (3) ◽  
pp. 83-87
Author(s):  
E. V. Kuzminova ◽  
◽  
M. P. Semenenko ◽  
D. V. Antipova ◽  
I. S. Zholobova ◽  
...  
Keyword(s):  
Biological Activity ◽  
Animal Husbandry ◽  
Test System ◽  
Feed Additive ◽  
Cell Level ◽  
Protective Properties ◽  
Membrane Protective Properties ◽  
A Cell ◽  
Derivatives Of

The article presents the results of the development of technology for obtaining and evaluating the biological activity of a feed additive containing humic acids. The technology of obtaining humic derivatives of high quality and with high stability of components from organic livestock wastes has been optimized. A humic feed additive has been developed and an estimation of its biological activity in vitro using a cell level test system (Paramecium caudatum) has been made. The presence of membrane-protective properties in humic derivatives has been revealed, which discovers the prospects of their use in animal husbandry and veterinary medicine as the means, possessing a hepatoprotective orientation and increasing the resistance of the organism to various unfavorable factors.

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