946151-04-8Relevant articles and documents
Synthesis and antiviral activity of some pyrrolonyl substituted heterocycles as additives to enhance inactivated Newcastle disease vaccine
Elsafty, Mounir M.,Morsy, Alaa R. I.,Ramadan, Sayed K.
, (2020)
This research reported the design and synthesis of some influential new pyrrolone derivatives bearing a pyrazole scaffold with the evaluation of their antiviral activity against Newcastle disease virus (NDV) in specific pathogen free (SPF) chicken embryos and immune boosting properties of these substances in SPF chicks. The building block synthon was the pyrazolyl acid hydrazide, derived from 2(3H)-furanone, which was reacted with some carbonyl compounds, e.g., salicylaldehyde, furfural, 1,3-diphenylpyrazole-4-carbaldehyde, 2-chloroquinoline-3-carbaldehyde, chromone-3-carbaldehyde, and 3-acetylcoumarin. The results revealed that pyrazole derivative 6, quinoline derivatives 7 and 8 exhibited 100% protection against NDV while the hydroxyphenyl derivative 3 showed 95% protection. In turn, chromone derivative 10 and coumarin derivative 11 exhibited 90% protection. The structures of all products were established on the basis of their elemental analyses and spectroscopic techniques.
Synthesis and antitumor activity evaluation of some N-heterocycles derived from pyrazolyl-substituted 2(3H)-furanone
Abou-Elmagd, Wael S. I.,EL-Ziaty, Ahmed K.,Elzahar, Magdy I.,Ramadan, Sayed K.,Hashem, Ahmed I.
, p. 1197 - 1208 (2016)
Pyrazolyl-substituted 2(3H)-furanone was allowed to react with different nitrogen nucleophiles such as hydrazine hydrate, ethylenediamine, ethanolamine, and anthranilic acid to give pyrrolone and benzoxazinone derivatives. The acid hydrazide 3 was reacted with some carbonyl compounds such as 4-chlorobenzaldehyde, chloroacetyl chloride, and acetic anhydride to give thiazolidinone, oxadiazole, and pyridazinone derivatives. Selected examples of the synthesized compounds were evaluated as anticancer agents against three types of carcinoma cell lines (HePG 2, HCT116, and PC3), using Doxorubicin as a reference drug. The result revealed that some of the new compounds showed high activities. Compound 6a was more potent than the standard drug. A docking study using MOE 2008.10 program was performed.
Facile and expedient synthesis and anti-proliferative activity of diversely pyrrolones bearing 1,3-diphenylpyrazole moiety
Ramadan, Sayed K.,Shaban, Safaa S.,Hashem, Ahmed I.
, p. 185 - 196 (2020)
A series of some pyrrolone derivatives were synthesized from the acid hydrazide, derived from a pyrazolyl-2(3H)-furanone, through treating with some carbonyl reagents such as 1-phenyl-3-(thiophen-2-yl)-1H-pyrazole-4-carbaldehyde, formic acid, lauroyl chloride, succinoyl chloride, propionic anhydride, as well as, ethoxymethylene malononitrile. All compounds were obtained in good yields and characterized by their microanalytical and spectral data. The synthesized products were evaluated for their in vitro antitumor activity against two human carcinoma cell lines (HCT-116 and MCF7) using doxorubicin as a reference drug by MTT assay. The results revealed that some compounds exhibited significant potency. Noteworthy, the N-propionyl hydrazide derivative was the most potent against both cell lines.
Novel synthesis of some isatin hydrazones and pyridazinophthalazines
Abou-Elmagd, Wael S.I.,Hashem, Ahmed I.
, p. 1083 - 1091 (2013/03/28)
The acid hydrazides bearing furyl, pyrazolyl, and indolyl rings 2 condense with isatin to give the corresponding hydrazones 3. Ring closure of the latter in an HCl=AcOH mixture led to the construction of a new pyrrolinone ring 4. The hydrazides 2 condensed also with phthalic anhydride to give the corresponding pyridazinophthalazines 5.
