scholarly journals Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

Molecules ◽  
2016 ◽  
Vol 21 (9) ◽  
pp. 1156 ◽  
Author(s):  
Hend Hafez ◽  
Abdel-Rhman El-Gazzar
Molecules ◽  
2019 ◽  
Vol 24 (3) ◽  
pp. 579
Author(s):  
Jordi Agramunt ◽  
Enrique Pedroso ◽  
Silvia Kreda ◽  
Rudolph Juliano ◽  
Anna Grandas

Addition of small molecule Retro-1 has been described to enhance antisense and splice switching oligonucleotides. With the aim of assessing the effect of covalently linking Retro-1 to the biologically active oligonucleotide, three different derivatives of Retro-1 were prepared that incorporated a phosphoramidite group, a thiol or a 1,3-diene, respectively. Retro-1–oligonucleotide conjugates were assembled both on-resin (coupling of the phosphoramidite) and from reactions in solution (Michael-type thiol-maleimide reaction and Diels-Alder cycloaddition). Splice switching assays with the resulting conjugates showed that they were active but that they provided little advantage over the unconjugated oligonucleotide in the well-known HeLa Luc705 reporter system.


Molecules ◽  
2019 ◽  
Vol 24 (19) ◽  
pp. 3520 ◽  
Author(s):  
Felicia D’Andrea ◽  
Giulia Vagelli ◽  
Carlotta Granchi ◽  
Lorenzo Guazzelli ◽  
Tiziano Tuccinardi ◽  
...  

Conjugation of known biologically active molecules to carbohydrate frameworks represents a valuable option for the preparation of hybrid, structurally-related families of compounds with the aim of modulating their biological response. Therefore, we present here a study on the preparation of d-galacto, d-manno, d-gluco, and d-lactose glycoconjugates of an established N-hydroxyindole-based (NHI) inhibitor of lactated dehydrogenase (LDH). Structural variations involved the sugar stereochemistry and size as well as the anchoring point of the NHI on the carbohydrate frame (either C-1 or C-6). In the case of the galactose anomeric glycoconjugate (C-1), intriguing solvent-dependent effects were observed in the glycosylation stereochemical outcome. The biological activity of the deprotected glycoconjugates in contrasting lactate formation and cancer cell proliferation are described.


2020 ◽  
Vol 85 (11) ◽  
pp. 1405-1415
Author(s):  
Behjat Pouramiri ◽  
Mahboobeh Zahedifar ◽  
Adileh Ayati ◽  
Farah Pouramiri ◽  
Mahdiyeh Ahmadi

A series of biologically active disubstituted benzofuran derivatives (3a?d) have been designed and synthesized via C?H bond activation reaction. The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro anti acetylcholinesterase (AChE) activities of these novel compounds were evaluated and showed low to moderate results. Among them, compound 3d moderately inhibited AChE activities with 68.12 % value.


2012 ◽  
Vol 22 (20) ◽  
pp. 6385-6390 ◽  
Author(s):  
Girish D. Hatnapure ◽  
Ashish P. Keche ◽  
Atish H. Rodge ◽  
Satish S. Birajdar ◽  
Rajesh H. Tale ◽  
...  

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (01) ◽  
pp. 50-58
Author(s):  
S. K Gupta ◽  
◽  
N. Kumar ◽  
D. Pathak

A series of biologically active benzimidazole derivatives (2a-2n) was synthesized by the reaction of o-phenylenediamine with the derivatives of benzoic acid in presence of 4N-HCl followed by the reaction with piperazine and formaldehyde to undergo Mannich reaction. The structures of all the synthesized Mannich bases were characterized by UV, FTIR, 1H NMR, mass spectroscopy and elemental analysis. The compounds were evaluated for their anthelmintic activity by the identification of paralyzing and death time by using mebendazole as standard in the concentration of 2 mg/ml. The compounds 2a, 2b, 2e and 2h were found to be most potent for anthelmintic activity. All the compounds were also evaluated for antibacterial activity against gram-positive bacterial strains like Bacillus subtilis and Streptococcus aureus, and gram-negative bacterial strains like Escherichia coli and Pseudomonas aeruginosa. The study was performed through disc diffusion method by using Ciprofloxacin as standard in the concentration of 50µg/ml. The compounds 2e, 2h, 2k, 2l and 2m were found to possess significant antibacterial activity.


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