scholarly journals Novel Alkyl(aryl)-Substituted 2,2-Difluoro-6-(trichloromethyl)-2H-1,3,2-oxazaborinin-3-ium-2-uides: Synthesis, Antimicrobial Activity, and CT-DNA Binding Evaluations

2020 ◽  
Vol 11 ◽  
Author(s):  
Wilian C. Rosa ◽  
Inaiá O. Rocha ◽  
Melissa B. Rodrigues ◽  
Helena S. Coelho ◽  
Laura B. Denardi ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Dna Binding ◽  
Alkyl Aryl ◽  
Ct Dna

scholarly journals Green ultrasound-assisted three-component click synthesis of novel 1H-1,2,3-triazole carrying benzothiazoles and fluorinated-1,2,4-triazole conjugates and their antimicrobial evaluation

2017 ◽  
Vol 67 (3) ◽  
pp. 309-324 ◽  
Author(s):  
Nadjet Rezki ◽  
Mohamed Reda Aouad
Keyword(s):  
Antimicrobial Activity ◽  
Cycloaddition Reaction ◽  
Dipolar Cycloaddition ◽  
Terminal Alkynes ◽  
One Pot ◽  
Alkyl Aryl ◽  
Antimicrobial Evaluation ◽  
Ultrasound Assisted ◽  
Click Synthesis

AbstractThe present study describes an efficient and ecofriendly, ultrasound, one-pot click cycloaddition approach for the construction of a novel series of 1,4-disubstituted-1,2,3-triazoles tethered with fluorinated 1,2,4-triazole-benzothiazole molecular conjugates. It involved three-component condensation of the appropriate bromoacetamide benzothiazole, sodium azide and 4-alkyl/aryl-5-(2-fluorophenyl)-3-(prop-2-ynylthio)-1,2,4-triazoles4a-ethrough a Cu(I)-catalyzed 1,3-dipolar cycloaddition reaction. This approach involvesin situgeneration of azidoacetamide benzothiazole, followed by condensation with terminal alkynes in the presence of CuSO4/Na-ascorbate in aqueous DMSO under both conventional and ultrasound conditions. Some of the designed 1,2,3-triazole conjugates6a-owere recognized for their antimicrobial activity against some bacterial and fungal pathogenic strains.

scholarly journals Ketolide Antimicrobial Activity Persists after Disruption of Interactions with Domain II of 23S rRNA

2004 ◽  
Vol 48 (10) ◽  
pp. 3677-3683 ◽  
Author(s):  
Guy W. Novotny ◽  
Lene Jakobsen ◽  
Niels M. Andersen ◽  
Jacob Poehlsgaard ◽  
Stephen Douthwaite
Keyword(s):  
Antimicrobial Activity ◽  
Ribosomal Subunit ◽  
23S Rrna ◽  
Alkyl Aryl ◽  
Interaction Sites ◽  
Enhanced Resistance ◽  
Low Levels ◽  
Domain V ◽  
Block Protein Synthesis ◽  
Do So

ABSTRACT Ketolides are the latest derivatives developed from the macrolide erythromycin to improve antimicrobial activity. All macrolides and ketolides bind to the 50S ribosomal subunit, where they come into contact with adenosine 2058 (A2058) within domain V of the 23S rRNA and block protein synthesis. An additional interaction at nucleotide A752 in the rRNA domain II is made via the synthetic carbamate-alkyl-aryl substituent in the ketolides HMR3647 (telithromycin) and HMR3004, and this interaction contributes to their improved activities. Only a few macrolides, including tylosin, come into contact with domain II of the rRNA and do so via interactions with nucleotides G748 and A752. We have disrupted these macrolide-ketolide interaction sites in the rRNA to assess their relative importance for binding. Base substitutions at A752 were shown to confer low levels of resistance to telithromycin but not to HMR3004, while deletion of A752 confers low levels of resistance to both ketolides. Mutations at position 748 confer no resistance. Substitution of guanine at A2058 gives rise to the MLSB (macrolide, lincosamide, and streptogramin B) phenotype, which confers resistance to all the drugs. However, resistance to ketolides was abolished when the mutation at position 2058 was combined with a mutation in domain II of the same rRNA. In contrast, the same dual mutations in rRNAs conferred enhanced resistance to tylosin. Our results show that the domain II interactions of telithromycin and HMR3004 differ from each other and from those of tylosin. The data provide no indication that mutations within domain II, either alone or in combination with an A2058 mutation, can confer significant levels of telithromycin resistance.

Synthesis, crystal structure, DFT/TDDFT calculation, photophysical properties and DNA binding studies of morpholino moiety ligand based two Cu(ii) complexes in combination with carboxylates

RSC Advances ◽  
2016 ◽  
Vol 6 (65) ◽  
pp. 60487-60501 ◽  
Author(s):  
Aparup Paul ◽  
Soumen Mistri ◽  
Apurba Bhunia ◽  
Soumen Manna ◽  
Horst Puschmann ◽  
...  
Keyword(s):  
Crystal Structure ◽  
Dna Binding ◽  
Dft Calculations ◽  
Photophysical Properties ◽  
Binding Constants ◽  
Binding Studies ◽  
Td Dft ◽  
Dna Binding Studies ◽  
Ct Dna

Two Cu(II) compounds have been characterized by structure analyses and DFT/TD-DFT calculations. Both the complexes potentially bind with CT-DNA and corresponding binding constants are in the order of 105 M−1.

scholarly journals Synthesis and Antimicrobial Activity of Newer Quinazolinones

2006 ◽  
Vol 3 (2) ◽  
pp. 97-102 ◽  
Author(s):  
J. A. Patel ◽  
B. D. Mistry ◽  
K. R. Desai
Keyword(s):  
Antimicrobial Activity ◽  
Diazonium Salts ◽  
Alkyl Aryl

2–alkyl–6–bromo–3,1–benzoxazine–4–one (2) is synthesized by treatingp–Bromoanthranilic acid and Acetylechoride or Benzoylchloride. Reaction of 2–alkyl–6–bromo–3,1–benzoxazine–4–one (2). with hydrazinehydrate furnish the corresponding 3–Amino–2–methyl–6–bromoquinazoline–4(3H)–one (3) which on reaction with benzaldehyde affordN,N– arylidene derivative (4). Reaction of 4 with various diazonium salts yields 6–bromo–2–alkyl/aryl–3{[phenyl(phenyldiazenyl)methylene]amino}quinazolin–4(3H)–one .

New Cd(II), Mn(II) and Ag(I) Schiff Base Complexes : Synthesis, Characterization, DNA Binding and Antimicrobial Activity

2016 ◽  
Vol 2 (3) ◽  
pp. 83-91 ◽  
Author(s):  
Laila H. Abdel-Rahman ◽  
Ahmed M. Abu-Dief ◽  
Rafat M. El-Khatib ◽  
Shimaa Mahdy Abdel-Fatah ◽  
Amin Abdou Seleem
Keyword(s):  
Antimicrobial Activity ◽  
Schiff Base ◽  
Dna Binding ◽  
Schiff Base Complexes
Sign in / Sign up

Export Citation Format

Share Document