3619-19-0Relevant academic research and scientific papers
Synthesis and biological evaluation of a novel class as antileishmanial agent
Saudi,El-Semary,Elbayaa,Jaeda,Eissa,Amer,Baddour
experimental part, p. 257 - 267 (2012/09/05)
Leishmaniases are a group of diseases caused by the protozoan parasites of the genus Leishmania. Despite the tremendous progress made in the understanding of the biochemistry and molecular biology of the parasite, the first choice treatment for leishmaniases still relies on pentavalent antimonial developed more than 50 years ago. These drugs are potentially toxic and often ineffective. The spread of drug resistance, combined with other shortcoming of the available antileishmanial drugs, emphasizes the importance of developing new effective, and safe drugs against leishmaniasis. The study reported here was undertaken to examine the antileishmanial activity of novel substituted 1,2,3,4- tetrahydropyrimidine-5-carboxamide (I) or cabohydrazide (II) analogs both in vivo and in vitro against Leishmania major. All tested compounds showed in vitro antileishmanial activity, but only four compounds showed in vivo activity in Swiss strain albino mice model as revealed by clinical cure of the cutaneous lesion, parasitologically by marked reduction in parasitic load and by histopathological changes. Springer Science+Business Media, LLC 2010.
Benzylidene/2-chlorobenzylidene hydrazides: Synthesis, antimicrobial activity, QSAR studies and antiviral evaluation
Kumar, Davinder,Judge, Vikramjeet,Narang, Rakesh,Sangwan, Sonia,De Clercq, Erik,Balzarini, Jan,Narasimhan, Balasubramanian
experimental part, p. 2806 - 2816 (2010/08/20)
A series of benzylidene hydrazides (1-20) was synthesized and tested, in vitro, for antibacterial, antifungal and antiviral activities. The microbial screening results indicated that compounds having chloro and nitro substituents were the most active ones. The antiviral evaluation depicted that compounds 9 and 19 were active against Vesicular stomatitis virus (VSV) in HeLa cell cultures. QSAR investigations indicated that the multi-target QSAR model was effective in describing the antimicrobial (antibacterial and antifungal) activity over the one-target QSAR models. Further the mt-QSAR model indicated that the topological parameters, second order molecular connectivity index (2χ) and third order Kier's alpha shape index (κα3) are effective in describing the antimicrobial activity of synthesized hydrazides.
