Synthesis and Biological Activity of New 1,2,3-Triazole Acyclonucleosides Analogues of ACV

2002 ◽  
Vol 2002 (6) ◽  
pp. 264-266 ◽  
Author(s):  
Smaail Radi ◽  
Hassan B. Lazrek
Keyword(s):  
Biological Activity ◽  
Biological Evaluation ◽  
Dipolar Cycloaddition ◽  
Azido Group ◽  
Significant Activity ◽  
Acetylenic Group ◽  
Substituted 1

The synthesis of new 4,5-substituted 1-[(2-hydroxyethoxy)methyl]-1,2,3-triazole 3a–e is described. The key step is the 1,3-dipolar cycloaddition between the azido group and an acetylenic group. Biological evaluation show significant activity.

Synthesis and Biological Evaluation of Various New Substituted 1,3,4-oxadiazole-2-thiols

2008 ◽  
Vol 59 (4) ◽  
Author(s):  
Gabriela Laura Almajan ◽  
Stefania Felicia Barbuceanu ◽  
Ioana Saramet ◽  
Mihaela Dinu ◽  
Cristian Vasile Doicin ◽  
...  
Keyword(s):  
Biological Activity ◽  
Plant Growth ◽  
1H Nmr ◽  
Elemental Analysis ◽  
13C Nmr ◽  
Biological Evaluation ◽  
Ethyl Chloroacetate ◽  
Low Concentrations ◽  
Synthesis And Biological Evaluation

5-[4-(4X-phenylsulfonyl)phenyl]-1,3,4-oxadiazole-2-thiols, X=H, Cl, Br, reacted with ethyl chloroacetate to give S-alkylated compounds. Aminomethylation of the thione form of oxadiazoles yielded N(3)-derivatives. All the products have been characterized by elemental analysis, IR, 1H-NMR and 13C-NMR. The plant-growth regulating effects of the title compounds were examined. From the biological activity results, we found that most compounds showed weak stimulatory activities at low concentrations.

scholarly journals Synthesis, characterization and biological activity of organometallic derivatives of the antimalarial drug mefloquine as new antischistosomal drug candidates

MedChemComm ◽  
2018 ◽  
Vol 9 (11) ◽  
pp. 1905-1909 ◽  
Author(s):  
Faustine d'Orchymont ◽  
Jeannine Hess ◽  
Gordana Panic ◽  
Marta Jakubaszek ◽  
Lea Gemperle ◽  
...  
Keyword(s):  
Biological Activity ◽  
Antimalarial Drug ◽  
Biological Evaluation ◽  
Design Synthesis ◽  
Drug Candidates ◽  
Derivatives Of

The design, synthesis, characterization and biological evaluation of new ferrocenyl and ruthenocenyl derivatives of the antimalarial mefloquine is described.

The Synthesis and Biological Evaluation of Anithiactin A/Thiasporine C and Analogues

2015 ◽  
Vol 68 (12) ◽  
pp. 1829 ◽  
Author(s):  
Richard A. Lamb ◽  
Michael P. Badart ◽  
Brooke E. Swaney ◽  
Sinan Gai ◽  
Sarah K. Baird ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Biological Activity ◽  
Cell Lines ◽  
Breast Cancer Cell ◽  
Phenyl Group ◽  
Biological Evaluation ◽  
Breast Cancer Cell Lines ◽  
High Concentration ◽  
Structural Requirements ◽  
Synthesis And Biological Evaluation

The synthesis of anithiactin A has been achieved in four steps. Several closely related analogues were synthesised and their biological activity against colon and breast cancer cell lines evaluated. Anithiactin A was found not to be cytotoxic even at a high concentration (100 μM); however, two 4-substituted phenyl thiazoles were found to be moderately cytotoxic at 10 μM. Based on these results, 4-substitution on the phenyl group appears to be critical for cytotoxicity. However, the exact electronic and structural requirements are unclear.

scholarly journals DESIGN, SYNTHESIS, DOCKING STUDIES AND BIOLOGICAL EVALUATION OF 2-PHENYL-3-(SUBSTITUTED BENZO[d] THIAZOL-2-YLAMINO)-QUINAZOLINE-4(3H)-ONE DERIVATIVES AS ANTIMICROBIAL AGENTS

2018 ◽  
Vol 10 (10) ◽  
pp. 57
Author(s):  
Pooja Pisal ◽  
Meenakshi Deodhar ◽  
Amol Kale ◽  
Ganesh Nigade ◽  
Smita Pawar
Keyword(s):  
Antimicrobial Agents ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Fusion Reactions ◽  
Gram Positive ◽  
Gram Negative

Objective: A new series 2-phenyl-3-(substituted benzo[d] thiazol-2-ylamino)-quinazoline-4(3H)-one was prepared by the fusion method by reacting 2-phenyl benzoxazine with 2-hydrazino benzothiazole and it was evaluated for their antimicrobial activity against gram positive, gram negative bacteria and fungi.Methods: Titled compounds were synthesized by fusion reactions. These compounds were evaluated by in vitro antibacterial and antifungal activity using the minimum inhibitory concentration and zone of inhibition methods. The synthesized compounds were characterized with the help of infrared, NMR and mass spectral studies. The benzothiazole moiety and the quinazoline ring have previously shown DNA gyrase inhibition and target related antibacterial activity. Thus, molecular docking studies of synthesized compounds were carried out (PDB: 3G75) to study the possible interaction of compounds with the target. The batch grid docking was performed to determine the probable.Results: These compounds showed significant activity against gram positive and gram negative bacteria as well against the fungi. The compound A5 was found to be active against B. subtilis, P aeruginosa and C. albican at 12.5 µg/ml MIC. The compound A3 was found to be active against all microbial strains selected at 25 and 12.5 µg/ml MIC.Conclusion: Though the relationship between the activities shown by these compounds in, the antimicrobial study is still to be established, the docking studies conducted found to be consistent with antimicrobial results. Thus the results indicate that the designed structure can be a potential lead as an antimicrobial agent.

Facile Synthesis and Biological Evaluation of Cyclopropyl-Pyrazole Hybrids in [bmim][PF6]-Water Biphasic System as Antifungal Agents

2019 ◽  
Vol 4 (3) ◽  
pp. 152-158
Author(s):  
P.C. Burde ◽  
A.M. Rahatgaonkar
Keyword(s):  
Ionic Liquid ◽  
Ambient Temperature ◽  
Antifungal Agents ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Biphasic System ◽  
Facile Synthesis ◽  
Convenient Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Substituted 1

3-Cyclopropyl-5-(4-substituted)-1-phenyl-4,5-dihydro-1H-pyrazoles derived from corresponding chalcones were synthesized and evaluated for their biological activities. A convenient synthesis of a library of these compounds in 1-butyl-3-methylimidazolium hexafluorophosphate-water biphasic system at ambient temperature has been accomplished. The ionic liquid, [bmim][PF6] and water which are immiscible, has been easily recycled and reused after separation of the products without any noticeable diminution in its activity.

scholarly journals Synthesis of novel 3-deoxy-3-C-triazolylmethyl-allose derivatives and evaluation of their biological activity

2012 ◽  
Vol 10 (2) ◽  
pp. 386-394 ◽  
Author(s):  
Jekaterina Rjabova ◽  
Vitālijs Rjabovs ◽  
Antonio Moreno Vargas ◽  
Elena Clavijo ◽  
Māris Turks
Keyword(s):  
Biological Activity ◽  
Biological Activities ◽  
Dipolar Cycloaddition ◽  
Molecular Scaffolds ◽  
New Compounds

AbstractRecently, monosaccharide-triazole conjugates have proved to possess a large variety of useful biological activities. This paper describes synthesis of a new series of 3-deoxy-3-C-triazolylmethyl-allose derivatives. These new compounds are obtained from acetonide-protected 3-deoxy-3-azidomethyl allose and commercial alkynes via Cu(I) catalyzed 1,3-dipolar cycloaddition. The obtained molecular scaffolds differ from those described earlier by the presence of a methylene linker (-CH2-) between the C(3) of allose and the triazole moiety. It was demonstrated that acetonide-protected monosaccharide, 3-deoxy-3-C-(4-phenyl-1H-1,2,3-triazol-1-yl)methyl-1,2:5,6-di-O-isopropylidene-α-d-allofuranose, inhibited α-L-fucosidase for 26% at 0.1 mM concentration, but a deprotected analog, 3-deoxy-3-C-(4-(4-tert-butylphenyl)-1H-1,2,3-triazol-1-yl)methyl-β-d-allofuranose, showed 15% inhibition of β-glucosidase at 1 mM concentration.

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