Synthesis and Evaluation of New Phthalazine Urea and Thiourea Derivatives as Carbonic Anhydrase Inhibitors

Arslan, Mustafa

dc.contributor.authors	Berber, N; Arslan, M; Yavuz, E; Bilen, C; Gencer, N;
dc.date.accessioned	2020-02-24T14:16:04Z
dc.date.available	2020-02-24T14:16:04Z
dc.date.issued	2013
dc.identifier.citation	Berber, N; Arslan, M; Yavuz, E; Bilen, C; Gencer, N; (2013). Synthesis and Evaluation of New Phthalazine Urea and Thiourea Derivatives as Carbonic Anhydrase Inhibitors. JOURNAL OF CHEMISTRY, , -
dc.identifier.issn	2090-9063
dc.identifier.uri	https://doi.org/10.1155/2013/742178
dc.identifier.uri	https://hdl.handle.net/20.500.12619/44945
dc.description.abstract	A new series of phthalazine substituted urea and thiourea derivatives were synthesized, and their inhibitory effects on the activity of purified human carbonic anhydrases (hCAs I and II) were evaluated. 2H-Indazolo[2,1-b]phthalazine-trione derivative (1) was prepared with 4-nitrobenzaldehyde, dimedone, and phthalhydrazide in the presence of TFA in DMF, and nitro group was reduced to amine derivative (2) with SnCl2 center dot 2H(2)O. The compound was reacted with isocyanates and isothiocyanates to get the final products (3a-p). The results showed that all the synthesized compounds inhibited the CA isoenzymes activity. 3a (IC50 = 6.40 mu M for hCA I and 6.13 mu M for hCA II) has the most inhibitory effect. The synthesized compounds are very bulky to be able to bind near the zinc ion, and they much more probably bind as the coumarin derivatives.
dc.language	English
dc.publisher	HINDAWI PUBLISHING CORPORATION
dc.subject	Chemistry
dc.title	Synthesis and Evaluation of New Phthalazine Urea and Thiourea Derivatives as Carbonic Anhydrase Inhibitors
dc.type	Article
dc.contributor.department	Sakarya Üniversitesi/Fen-Edebiyat Fakültesi/Kimya Bölümü
dc.contributor.saüauthor	Arslan, Mustafa
dc.relation.journal	JOURNAL OF CHEMISTRY
dc.identifier.wos	WOS:000324731400001
dc.identifier.doi	10.1155/2013/742178
dc.contributor.author	Arslan, Mustafa