scholarly journals Total Synthesis, Biological Evaluation, and Target Identification of RareAbiesSesquiterpenoids

2018 ◽  
Vol 140 (50) ◽  
pp. 17465-17473 ◽  
Author(s):  
Dexter C. Davis ◽  
Dominic G. Hoch ◽  
Li Wu ◽  
Daniel Abegg ◽  
Brandon S. Martin ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Target Identification ◽  
Biological Evaluation

Novel Thiazole-Based Thiazolidinones as Potent Anti-infective Agents: In silico PASS and Toxicity Prediction, Synthesis, Biological Evaluation and Molecular Modelling

2020 ◽  
Vol 23 (2) ◽  
pp. 126-140 ◽  
Author(s):  
Christophe Tratrat
Keyword(s):  
In Silico ◽  
Antimicrobial Agents ◽  
Target Identification ◽  
Biological Evaluation ◽  
Microbial Infection ◽  
Toxicity Prediction ◽  
Discovery Studio ◽  
Bacteria And Fungi ◽  
Multiple Drugs ◽  
Antibacterial And Antifungal

Aims and Objective: The infectious disease treatment remains a challenging concern owing to the increasing number of pathogenic microorganisms associated with resistance to multiple drugs. A promising approach for combating microbial infection is to combine two or more known bioactive heterocyclic pharmacophores in one molecular platform. Herein, the synthesis and biological evaluation of novel thiazole-thiazolidinone hybrids as potential antimicrobial agents were dissimilated. Materials and Methods: The preparation of the substituted 5-benzylidene-2-thiazolyimino-4- thiazolidinones was achieved in three steps from 2-amino-5-methylthiazoline. All the compounds have been screened in PASS antibacterial activity prediction and in a panel of bacteria and fungi strains. Minimum inhibitory concentration and minimum bacterial concentration were both determined by microdilution assays. Molecular modeling was conducted using Accelrys Discovery Studio 4.0 client. ToxPredict (OPEN TOX) and ProTox were used to estimate the toxicity of the title compounds. Results: PASS prediction revealed the potentiality antibacterial property of the designed thiazolethiazolidinone hybrids. All tested compounds were found to kill and to inhibit the growth of a vast variety of bacteria and fungi, and were more potent than the commercial drugs, streptomycin, ampicillin, bifomazole and ketoconazole. Further, in silico study was carried out for prospective molecular target identification and revealed favorable interaction with the target enzymes E. coli MurB and CYP51B of Aspergillus fumigatus. Toxicity prediction revealed that none of the active compounds was found toxic. Conclusion: Substituted 5-benzylidene-2-thiazolyimino-4-thiazolidinones, endowing remarkable antibacterial and antifungal properties, were identified as a novel class of antimicrobial agents and may find a potential therapeutic use to eradicate infectious diseases.

scholarly journals Xylochemical Synthesis and Biological Evaluation of Shancigusin C and Bletistrin G

Molecules ◽  
2021 ◽  
Vol 26 (11) ◽  
pp. 3224
Author(s):  
Leander Geske ◽  
Ulrich Kauhl ◽  
Mohamed E. M. Saeed ◽  
Anja Schüffler ◽  
Eckhard Thines ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Aromatic Substitution ◽  
Substitution Reactions ◽  
Total Syntheses ◽  
Wittig Olefination ◽  
Starting Point ◽  
Perkin Reaction ◽  
Synthesis And Biological Evaluation

The biological activities of shancigusin C (1) and bletistrin G (2), natural products isolated from orchids, are reported along with their first total syntheses. The total synthesis of shancigusin C (1) was conducted by employing the Perkin reaction to forge the central stilbene core, whereas the synthesis of bletistrin G (2) was achieved by the Wittig olefination followed by several regioselective aromatic substitution reactions. Both syntheses were completed by applying only renewable starting materials according to the principles of xylochemistry. The cytotoxic properties of shancigusin C (1) and bletistrin G (2) against tumor cells suggest suitability as a starting point for further structural variation.

Total Synthesis and Target Identification of the Curcusone Diterpenes

2021 ◽  
Author(s):  
Chengsen Cui ◽  
Brendan G. Dwyer ◽  
Chang Liu ◽  
Daniel Abegg ◽  
Zhong-Jian Cai ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Target Identification

The stereocontrolled total synthesis of altohyrtin A/spongistatin 1: fragment couplings, completion of the synthesis, analogue generation and biological evaluation

2005 ◽  
Vol 3 (13) ◽  
pp. 2431 ◽  
Author(s):  
Ian Paterson ◽  
David Y.-K. Chen ◽  
Mark J. Coster ◽  
José L. Aceña ◽  
Jordi Bach ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Spongistatin 1 ◽  
Altohyrtin A

scholarly journals Total synthesis, stereochemical elucidation and biological evaluation of Ac2SGL; a 1,3-methyl branched sulfoglycolipid from Mycobacterium tuberculosis

2013 ◽  
Vol 4 (2) ◽  
pp. 709-716 ◽  
Author(s):  
Danny Geerdink ◽  
Bjorn ter Horst ◽  
Marco Lepore ◽  
Lucia Mori ◽  
Germain Puzo ◽  
...  
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Total Synthesis ◽  
Biological Evaluation

Total synthesis and biological evaluation of Wewakazole

2017 ◽  
Vol 33 (6) ◽  
pp. 890-894 ◽  
Author(s):  
Bohua Long ◽  
Jingzhao Zhang ◽  
Xueyan Wang ◽  
Xudong Tang ◽  
Zhengzhi Wu
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Total Synthesis and Biological Evaluation of Cortistatins A and J and Analogues Thereof

2009 ◽  
Vol 131 (30) ◽  
pp. 10587-10597 ◽  
Author(s):  
K. C. Nicolaou ◽  
Xiao-Shui Peng ◽  
Ya-Ping Sun ◽  
Damien Polet ◽  
Bin Zou ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Isolation and structure of combretastatin

1982 ◽  
Vol 60 (11) ◽  
pp. 1374-1376 ◽  
Author(s):  
George R. Pettit ◽  
Gordon M. Cragg ◽  
Delbert L. Herald ◽  
Jean M. Schmidt ◽  
Prasert Lohavanijaya
Keyword(s):  
Total Synthesis ◽  
South African ◽  
Spectral Methods ◽  
Biological Evaluation ◽  
Crystallographic Analysis ◽  
Structural Elucidation ◽  
The South ◽  
X Ray

The South African tree Combretumcaffrum has been shown to contain a constituent capable of significantly reversing astrocyte formation employing the National Cancer Institute's 9ASK system. The constituent responsible for astrocyte reversal was isolated and designated combretastatin (1). Structural elucidation was initiated employing spectral methods and completed by X-ray crystallographic analysis. By this means combretastatin was assigned structure 1. Further biological evaluation and a total synthesis are now in progress.

scholarly journals Total Synthesis and Biological Evaluation of the Glycosylated Macrocyclic Antibiotic Mangrolide A

2018 ◽  
Vol 57 (34) ◽  
pp. 11020-11024 ◽  
Author(s):  
Hiromu Hattori ◽  
Joel Roesslein ◽  
Patrick Caspers ◽  
Katja Zerbe ◽  
Hideki Miyatake-Ondozabal ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Biological Evaluation ◽  
Macrocyclic Antibiotic ◽  
Synthesis And Biological Evaluation
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