Design and Synthesis of New Aminoglycoside Antibiotics Containing Neamine as an Optimal Core Structure:  Correlation of Antibiotic Activity with in Vitro Inhibition of Translation

1999 ◽  
Vol 121 (28) ◽  
pp. 6527-6541 ◽  
Author(s):  
William A. Greenberg ◽  
E. Scott Priestley ◽  
Pamela S. Sears ◽  
Phil B. Alper ◽  
Christoph Rosenbohm ◽  
...  
Keyword(s):  
Antibiotic Activity ◽  
Core Structure ◽  
Aminoglycoside Antibiotics ◽  
Design And Synthesis ◽  
Structure Correlation ◽  
In Vitro Inhibition

Structure-based synthesis: From natural products to drug prototypes

2009 ◽  
Vol 81 (6) ◽  
pp. 1085-1091 ◽  
Author(s):  
Stephen Hanessian
Keyword(s):  
Natural Products ◽  
Total Synthesis ◽  
Design Element ◽  
X Ray ◽  
Design And Synthesis ◽  
Highly Active ◽  
In Vitro Inhibition ◽  
Inhibitory Activities ◽  
Active Natural

X-ray crystallographic data available from complexes of natural and synthetic molecules with the enzyme thrombin has led to the design and synthesis of truncated and hydrid molecules exhibiting excellent inhibition in vitro. The design element has also been extended to the synthesis and in vitro inhibition of a series of achiral molecules deploying aromatic and heterocyclic core motifs with appropriately functionalized appendages that provide excellent binding interactions at the S1, S2, and S3 sites of thrombin. Excellent selectivity for thrombin over trypsin has also been observed. Thus, studies in total synthesis of highly active natural aeruginosins have inspired further work toward truncated and hybrid analogs with excellent inhibitory activities. Structure-based organic synthesis has guided our research from natural products toward unnatural drug-like prototypes.

SAR directed design and synthesis of novel β(1-4)-Glucosyltransferase inhibitors and Their In vitro inhibition studies

2002 ◽  
Vol 10 (4) ◽  
pp. 1129-1136 ◽  
Author(s):  
Asish K Bhattacharya ◽  
Florian Stolz ◽  
Jürgen Kurzeck ◽  
Wolfgang Rüger ◽  
Richard R Schmidt
Keyword(s):  
Design And Synthesis ◽  
In Vitro Inhibition ◽  
Directed Design ◽  
Inhibition Studies

ChemInform Abstract: SAR-Directed Design and Synthesis of Novel β(1-4)-Glucosyltransferase Inhibitors and Their in vitro Inhibition Studies.

ChemInform ◽  
2010 ◽  
Vol 33 (20) ◽  
pp. no-no
Author(s):  
Asish k. Bhattacharya ◽  
Florian Stolz ◽  
Juergen Kurzeck ◽  
Wolfgang Rueger ◽  
Richard R. Schmidt
Keyword(s):  
Design And Synthesis ◽  
In Vitro Inhibition ◽  
Directed Design ◽  
Inhibition Studies

scholarly journals Retention of antibiotic activity against resistant bacteria harbouring aminoglycoside-N-acetyltransferase enzyme by adjuvants: a combination of in-silico and in-vitro study

2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Shamim Ahmed ◽  
Sabrina Amita Sony ◽  
Md. Belal Chowdhury ◽  
Md. Mahib Ullah ◽  
Shatabdi Paul ◽  
...  
Keyword(s):  
Binding Affinity ◽  
Bacterial Resistance ◽  
Selection Process ◽  
Bacterial Species ◽  
In Vitro Study ◽  
Antibiotic Activity ◽  
Aminoglycoside Antibiotics ◽  
Resistant Bacteria ◽  
Acetyl Coa

Abstract Interference with antibiotic activity and its inactivation by bacterial modifying enzymes is a prevailing mode of bacterial resistance to antibiotics. Aminoglycoside antibiotics become inactivated by aminoglycoside-6′-N-acetyltransferase-Ib [AAC(6′)-Ib] of gram-negative bacteria which transfers an acetyl group from acetyl-CoA to the antibiotic. The aim of the study was to disrupt the enzymatic activity of AAC(6′)-Ib by adjuvants and restore aminoglycoside activity as a result. The binding affinities of several vitamins and chemical compounds with AAC(6′)-Ib of Escherichia coli, Klebsiella pneumoniae, and Shigella sonnei were determined by molecular docking method to screen potential adjuvants. Adjuvants having higher binding affinity with target enzymes were further analyzed in-vitro to assess their impact on bacterial growth and bacterial modifying enzyme AAC(6′)-Ib activity. Four compounds—zinc pyrithione (ZnPT), vitamin D, vitamin E and vitamin K-exhibited higher binding affinity to AAC(6′)-Ib than the enzyme’s natural substrate acetyl-CoA. Combination of each of these adjuvants with three aminoglycoside antibiotics—amikacin, gentamicin and kanamycin—were found to significantly increase the antibacterial activity against the selected bacterial species as well as hampering the activity of AAC(6′)-Ib. The selection process of adjuvants and the use of those in combination with aminoglycoside antibiotics promises to be a novel area in overcoming bacterial resistance.

Effekte von Substanz P und Neurotensin auf die Kontraktilität des Ileums der Maus in vitro: Inhibition durch STW 5

2007 ◽  
Vol 45 (08) ◽  
Author(s):  
D Hagelauer ◽  
O Kelber ◽  
D Weiser ◽  
S Laufer ◽  
H Heinle
Keyword(s):  
Substanz P ◽  
In Vitro Inhibition

Design and Synthesis of (E)-4-(2-Phenyl-2H-chromen-3-yl)but-3-en-2-ones and Evaluation of their In Vitro Antimicrobial Activity

2015 ◽  
Vol 12 (5) ◽  
pp. 352-358 ◽  
Author(s):  
Sabita Nayak ◽  
Subhendu Chakroborty ◽  
Sujitlal Bhakta ◽  
Pravati Panda ◽  
Seetaram Mohapatra ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Design And Synthesis
Sign in / Sign up

Export Citation Format

Share Document