tetano
Editor, Senior Moderator
Eur J Med Chem. 2015 Aug 5;102:266-276. doi: 10.1016/j.ejmech.2015.08.005. [Epub ahead of print]
[h=1]Synthesis and antiviral activity of some new bis-1,3-thiazole derivatives.[/h] Dawood KM[SUP]1[/SUP], Eldebss TM[SUP]2[/SUP], El-Zahabi HS[SUP]3[/SUP], Yousef MH[SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Treatment of 3-phenyl-1,3-thiazolidin-4-one derivative 1 with phenylisothiocyanate in DMF, in the presence of potassium hydroxide, at room temperature gave the non-isolable potassium salt 2. The in-situ reaction of 2 with differently substituted N-aryl hydrazonoyl chlorides 3, 7a-d and 14a-d afforded the corresponding 2-(pyrazolyl)thiazolylimino-5-(thiadiazolylidene)thiazolidin-4-one derivatives 6, 10a-d and 17a-d, respectively. Reaction of 2 with further α-haloketones yielded the 4-(pyrazolyl)thiazolylimino-bis-thiazolidine derivatives 22, 25 and 26. Single crystal X-ray analysis was used in structure elucidation of the products. The in-vitro antiviral screening against four viruses (Poliovirus, Influenza A (H1N1) virus, Hepatitis B virus and Hepatitis C virus) for the obtained compounds was examined. Structure activity relationship (SAR) was also studied. The goal of the work was achieved in discovering a very active compound 10a as anti HCV agent (EC[SUB]50[/SUB] 0.56 μM).
Copyright ? 2015. Published by Elsevier Masson SAS.
[h=4]KEYWORDS:[/h] 1,3,4-Thiadiazole; 1,3-Thiazole; Antiviral activity; Pyrazole; SAR
PMID: 26291036 [PubMed - as supplied by publisher]
[h=1]Synthesis and antiviral activity of some new bis-1,3-thiazole derivatives.[/h] Dawood KM[SUP]1[/SUP], Eldebss TM[SUP]2[/SUP], El-Zahabi HS[SUP]3[/SUP], Yousef MH[SUP]2[/SUP].
[h=3]Author information[/h]
[h=3]Abstract[/h] Treatment of 3-phenyl-1,3-thiazolidin-4-one derivative 1 with phenylisothiocyanate in DMF, in the presence of potassium hydroxide, at room temperature gave the non-isolable potassium salt 2. The in-situ reaction of 2 with differently substituted N-aryl hydrazonoyl chlorides 3, 7a-d and 14a-d afforded the corresponding 2-(pyrazolyl)thiazolylimino-5-(thiadiazolylidene)thiazolidin-4-one derivatives 6, 10a-d and 17a-d, respectively. Reaction of 2 with further α-haloketones yielded the 4-(pyrazolyl)thiazolylimino-bis-thiazolidine derivatives 22, 25 and 26. Single crystal X-ray analysis was used in structure elucidation of the products. The in-vitro antiviral screening against four viruses (Poliovirus, Influenza A (H1N1) virus, Hepatitis B virus and Hepatitis C virus) for the obtained compounds was examined. Structure activity relationship (SAR) was also studied. The goal of the work was achieved in discovering a very active compound 10a as anti HCV agent (EC[SUB]50[/SUB] 0.56 μM).
Copyright ? 2015. Published by Elsevier Masson SAS.
[h=4]KEYWORDS:[/h] 1,3,4-Thiadiazole; 1,3-Thiazole; Antiviral activity; Pyrazole; SAR
PMID: 26291036 [PubMed - as supplied by publisher]