Synthesis and in Vitro Antiproliferative Screening of New 2,7-naphthyridine-3-carboxylic Acid Hydrazide Derivatives.
نویسندگان
چکیده
The new pyrrolo[3,4-c]pyridines and 2,7-naphthyridine derivatives have been synthesized. 4-Hydroxy-8-methyl-l-oxo-6-phenyl-1,2-dihydro-2,7-naphthyridine-3-carboxylic acid hydrazide (4) was the key intermediate for the synthesis of the novel derivatives of various chemical structures: Schiff bases, 1,3,4-oxadiazoles, pyrazoles, carbohydrazides, semi- and thiosemicarbazides. The structures of these new compounds were confirmed by elemental analysis and IR, NMR and MS spectra. The antitumor activities of the obtained derivatives were examined. Eight of the twenty one newly synthesized compounds were qualified by the NCI (Bethesda, MD, USA) for in vito screening against 60 different human tumor cell lines. The most active proved to be the Schiff bases.
منابع مشابه
Synthesis and Characterization of Manganese (II), Cobalt (II), Complexes of New Polydentate Ligands Containing 1,8-Naphthydridine Moiety
The substituted 1,8-naphthyridines, 2-hydroxy-1,8-naphthyridine-3-carboxylic acid hydrazide (HNch) and 2-hydroxy-1,8-naphthyridine-3-carboxylic acid 0-hydroxybenzylidene hydrazide (HNCHBh) react with acetates of Mn(II), Co(II) metal ions to yield complexes of definite composition. The complexes have been characterized by elemental analysis, thermal, conductance, magnetic studies and IR, electro...
متن کاملDesign, Synthesis and Biological Evaluation of 4-Benzamidobenzoic Acid Hydrazide Derivatives as Novel Soluble Epoxide Hydrolase Inhibitors
Inhibitors of soluble epoxide hydrolase (sEH) represent one of the novel pharmaceutical approaches for treating hypertension, vascular inflammation, pain and other cardiovascular related diseases. Most of the potent sEH inhibitors reported in literature often suffer from poor solubility and bioavailability. Toward improving pharmacokinetic profile beside favorable potency, two series of 4-benza...
متن کاملDesign, Synthesis and Biological Evaluation of 4-Benzamidobenzoic Acid Hydrazide Derivatives as Novel Soluble Epoxide Hydrolase Inhibitors
Inhibitors of soluble epoxide hydrolase (sEH) represent one of the novel pharmaceutical approaches for treating hypertension, vascular inflammation, pain and other cardiovascular related diseases. Most of the potent sEH inhibitors reported in literature often suffer from poor solubility and bioavailability. Toward improving pharmacokinetic profile beside favorable potency, two series of 4-benza...
متن کاملSYNTHESES, ANTIBACTERIAL AND ANTIFUNGAL ACTIVITIES OF 2-ARYL-4- QUINOLINE- CARBOXAMIDE DERIVATIVES
Reaction of aryl methyl ketone with isatin in the presence of a base afforded 2- arylquinoline-4-carboxylic acid (3). Reaction of diazomethane with compound 3 yielded the ester 4. Compound 5 was prepared from the reaction of N, N'-dialkylethyl (or propyl) arnine with 4. Addition of hydrazine hydrate to compound 4a gave 2- (2- pyridyl) quinoline-4-carboxylic acid hydrazide (6). Reaction of l...
متن کاملFused heterocycles: synthesis of some new imidazo[1,2-a]- pyridine derivatives.
Some new thiazolidines and spirothiazolidines derived from hydrazones of 2-methylimidazo[1,2-a]pyridine-3-carboxylic acid hydrazide, a bioisosteric derivative of isoniazid, were synthesized and characterized by analytical, IR, (1)H- and (13)C-NMR and mass spectral data. Some of the newly synthesized compounds were screened for their antimycobacterial activities. None of the tested compounds sho...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Acta poloniae pharmaceutica
دوره 72 2 شماره
صفحات -
تاریخ انتشار 2015