On November 30, 2020, Milisiunaite, Vaida; Kadlecova, Alena; Zukauskaite, Asta; Dolezal, Karel; Strnad, Miroslav; Voller, Jiri; Arbaciauskiene, Egle; Holzer, Wolfgang; Sackus, Algirdas published an article.Category: chlorides-buliding-blocks The title of the article was Synthesis and anthelmintic activity of benzopyrano[2,3-c]pyrazol-4(2H)-one derivatives. And the article contained the following:
A series of benzopyrano[2,3-c]pyrazol-4(2H)-one derivatives I [R1 = Me, Ph; R2 = H, F; R3 = H, F, Cl, etc.; R4 = H, F] were synthesized from readily available 1-phenyl- and 1-methyl-1H-pyrazol-3-ols by sequentially employing O-acylation, Fries rearrangement and potassium carbonate-induced cyclization. The anthelmintic properties of the obtained compounds were investigated in-vivo in a model nematode, Caenorhabditis elegans. Five compounds, I [R1 = Ph, R2 = R3 = R4 = H; R1 = Ph, R2 = R4 = H, R3 = F; R1 = Ph, R2 = R4 = H, R3 = Cl; R1 = Ph, R2 = R4 = H, R3 = Br; R1 = Ph, R2 = F, R3 = R4 = H] altered the development of C. elegans. While the activities of I [R1 = Ph, R2 = R3 = R4 = H; R1 = Ph, R2 = F, R3 = R4 = H] were rather modest, compounds I [R1 = Ph, R2 = R4 = H, R3 = F; R1 = Ph, R2 = R4 = H, R3 = Cl; R1 = Ph, R2 = R4 = H, R3 = Br] inhibited the growth of the worms at concentrations of approx. 1-3μM. At these concentrations, the compounds did not kill the worms, but they strongly inhibited their development, with the majority of larvae never progressing past the L1 stage. Moreover, testing in non-cancer human cell lines showed that, with exception of 7-bromo derivative I [R1 = Ph, R2 = R4 = H, R3 = Br], the active compounds showed favorable toxicity profiles. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).Category: chlorides-buliding-blocks
The Article related to benzopyranopyrazolone preparation anthelmintic activity cytotoxicity sar, anthelmintic activity, benzopyrano[2,3-c]pyrazol-4(2h)-ones, caenorhabditis elegans, cytotoxicity, pyrazole and other aspects.Category: chlorides-buliding-blocks
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics