3,4-Disubstituted-1,2,3,4,5,6,7,8-octahydroquinazoline-2-thiones: Synthesis, Antimicrobial Evaluation and QSAR Investigations Using Hansch Analysis

2008 ◽  
Vol 341 (4) ◽  
pp. 231-239 ◽  
Author(s):  
Maninder Minu ◽  
Ananda Thangadurai ◽  
Sharad R. Wakode ◽  
Shyam S. Agrawal ◽  
Balasubramanian Narasimhan
Keyword(s):  
Hansch Analysis ◽  
Antimicrobial Evaluation

Synthesis and Antimicrobial Evaluation of Some New Pyrazoline Derivatives

2011 ◽  
Vol 3 (8) ◽  
pp. 72-73 ◽  
Author(s):  
Kendre M. M Kendre M. M ◽  
◽  
M. A. Baseer M. A. Baseer
Keyword(s):  
Antimicrobial Evaluation

Synthesis and Antimicrobial Evaluation of Amphipathic Peptide Models

2016 ◽  
Vol 13 (7) ◽  
pp. 715-724 ◽  
Author(s):  
Marianna Sakka ◽  
Alexandra Balliou ◽  
Asimina Marianou ◽  
Dimitris Krikorian ◽  
Margarita Tsirogianni ◽  
...  
Keyword(s):  
Amphipathic Peptide ◽  
Peptide Models ◽  
Antimicrobial Evaluation

Design, Synthesis, Antimicrobial Evaluation and Molecular Modeling Study of New 2-mercaptoimidazoles (Series-III)

2019 ◽  
Vol 16 (5) ◽  
pp. 512-521 ◽  
Author(s):  
Nidhi Rani ◽  
Randhir Singh
Keyword(s):  
Sulfonic Acid ◽  
Docking Study ◽  
Molecular Docking Study ◽  
One Pot ◽  
Design Synthesis ◽  
Toluene Sulfonic Acid ◽  
Antimicrobial Evaluation ◽  
Bacteria And Fungi ◽  
High Yields ◽  
Antimicrobial Potency

Background: A series of novel substituted 2-mercaptoimidazoles was synthesised efficiently and in high yields using one-pot synthesis from m-hydroxyacetophenones. Methods: The structures of the newly synthesized compounds were established, their molecular activity was investigated against some bacteria and fungi were further validated using molecular docking study. Results: Reaction of o-hydroxyphenacylbromide (2) with substituted aniline and KSCN, in the presence of catalyst p-toluene sulfonic acid afforded 4(a-r) in good yield. The structure of compounds (4a-r) was confirmed by IR, NMR and MS. Conclusion: The compounds exhibited excellent antimicrobial potency against the tested microorganism.

A New Reactive Ketenaminal: Synthesis, Coupling Reaction, Tautomeric Study, Docking and Antimicrobial Evaluation of the Products

2020 ◽  
Vol 16 (6) ◽  
pp. 761-773
Author(s):  
Huda K. Mahmoud ◽  
Hanadi A. Katouah ◽  
Marwa F. Harras ◽  
Thoraya A. Farghaly
Keyword(s):  
Binding Site ◽  
Antimicrobial Agents ◽  
Coupling Reaction ◽  
Docking Study ◽  
Binding Mode ◽  
Binding Energies ◽  
Simple Method ◽  
Antimicrobial Evaluation ◽  
New Compounds ◽  
Active Methylene

Background: One of the most successful reagents used in the synthesis of the reactive enaminone is DMF-DMA, but it is very expensive with harmful effects on the human health and reacts with special compounds to generate the enaminone such as active methylene centers. Aim: In this article, we synthesized a new ketenaminal by simple method with inexpensive reagents (through desulfurization in diphenylether). Methods: Thus, a novel reactive ketenaminal (enaminone) was synthesized from the desulfurization of 2-((2-(4-chlorophenyl)-2-oxoethyl)thio)-5,7-bis(4-methoxyphenyl)pyrido[2,3-d]pyrimidin- 4(3H)-one with diphenylether. The starting keteneaminal was coupled with diazotized anilines via the known coupling conditions to give a new series of 2-(4-chlorophenyl)-1-(2-(arylhydrazono)-2- oxoethyl)-5,7-bis(4-methoxy-phenyl)pyrido[2,3-d]pyrimidin-4(1H)-ones. Results: The structures of the new compounds were elucidated based on their IR, 1H-NMR, 13CNMR, and Mass spectra. Moreover, the potency of these compounds as antimicrobial agents has been evaluated. The results showed that some of the products have high activity nearly equal to that of the used standard antibiotic. Additionally, the docking study was done to get the binding mode of the synthesized compounds with the binding site of the DHFR enzyme. The results of molecular docking of the synthesized arylhydrazono compounds are able to fit in DHFR binding site with binding energies ranging from -4.989 to -8.178 Kcal/mol. Conclusion: Our goal was achieved in this context by the synthesis of new ketenaminal from inexpensive reagents, which was utilized in the preparation of bioactive arylhydrazone derivatives.

Synthesis and Antimicrobial Evaluation of (Z)-5-((3-phenyl-1H-pyrazol-4- yl)methylene)-2-thioxothiazolidin-4-one Derivatives

2016 ◽  
Vol 12 (8) ◽  
pp. 751-759 ◽  
Author(s):  
Zhi-Yu Wei ◽  
Jia-Chun Liu ◽  
Wen Zhang ◽  
Ya-Ru Li ◽  
Chao Li ◽  
...  
Keyword(s):  
Antimicrobial Evaluation

Substituted Naphthalen-1-yl-Acetic Acid Hydrazides: Synthesis, Antimicrobial Evaluation and QSAR Analysis

2013 ◽  
Vol 9 (2) ◽  
pp. 249-274 ◽  
Author(s):  
Rakesh Narang ◽  
Balasubramanian Narasimhan ◽  
Sunil Sharma ◽  
Erik De Clercq ◽  
Christophe Pannecouque ◽  
...  
Keyword(s):  
Acetic Acid ◽  
Qsar Analysis ◽  
Antimicrobial Evaluation
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