316136-35-3Relevant academic research and scientific papers
Design, synthesis and evaluation against Chikungunya virus of novel small-molecule antiviral agents
Tardugno, Roberta,Giancotti, Gilda,De Burghgraeve, Tine,Delang, Leen,Neyts, Johan,Leyssen, Pieter,Brancale, Andrea,Bassetto, Marcella
, p. 869 - 874 (2018)
Chikungunya virus is a re-emerging arbovirus transmitted to humans by mosquitoes, responsible for an acute flu-like illness associated with debilitating arthralgia, which can persist for several months or become chronic. In recent years, this viral infection has spread worldwide with a previously unknown virulence. To date, no specific antivirals treatments nor vaccines are available against this important pathogen. Starting from the structures of two antiviral hits previously identified in our research group with in silico techniques, this work describes the design and preparation of 31 novel structural analogues, with which different pharmacophoric features of the two hits have been explored and correlated with the inhibition of Chikungunya virus replication in cells. Structure-activity relationships were elucidated for the original scaffolds, and different novel antiviral compounds with EC50 values in the low micromolar range were identified. This work provides the foundation for further investigation of these promising novel structures as antiviral agents against Chikungunya virus.
Antimicrobial evaluation of imines and thiazolidinones derived from 3-phenylpropane hydrazide
Fuloria, Neeraj K.,Singh, Vijender,Yar, Mohammad Shahar,Ali, Mohammad
experimental part, p. 371 - 377 (2010/03/03)
Methyl 3-phenylpropanoate (1), after hydrazination into 3-phenylpropanehydrazide (2), was converted into N-arylidene-3-phenylpropane hydrazides (3a-e), which on cyclization with thioglycolic acid yielded N-(4-oxo-2-arylthiazolidin-3-yl)-3-phenylpropanamides (4a-e). All the proposed structures of newly synthesized compounds were in full agreement with the spectral data. Due to para substitution, compound 3a, 4a and 4b were found to be the most potent when evaluated for antibacterial and antifungal activities.
