DESIGN, SYNTHESIS, CHARACTERIZATION, AND CYTOTOXICITY EVALUATION OF NEW 4-BENZYL-1,3-OXAZOLE DERIVATIVES BEARING 4-(4-CHLOROPHENYLSULFONYL)PHENYL MOIETY

被引：6

作者：

Apostol, Theodora-Venera ^{[1
]}

Socea, Laura-Ileana ^{[1
]}

Draghici, Constantin ^{[2
]}

Olaru, Octavian Tudorel ^{[3
]}

Saramet, Gabriel ^{[4
]}

Enache-Preoteasa, Cristian ^{[5
]}

Barbuceanu, Stefania-Felicia ^{[1
]}

机构：

[1] Carol Davila Univ Med & Pharm, Fac Pharm, Organ Chem Dept, 6 Traian Vuia St, Bucharest 020956, Romania

[2] Romanian Acad, Costin D Nenitescu Inst Organ Chem, 202B Splaiul Independentei St, Bucharest 060023, Romania

[3] Carol Davila Univ Med & Pharm, Fac Pharm, Pharmaceut Bot & Cell Biol Dept, 6 Traian Vuia St, Bucharest 020956, Romania

[4] Carol Davila Univ Med & Pharm, Fac Pharm, Pharmaceut Technol & Biopharm Dept, 6 Traian Vuia St, Bucharest 020956, Romania

[5] Natl Phytosanit Lab, 11 Voluntari Blvd, Voluntari 077190, Romania

来源：

FARMACIA | 2021年 / 69卷 / 02期

关键词：

N-acyl-alpha-amino acid; 1,3-oxazol-5(4H)-one; 1,3-oxazole; cytotoxicity; BIOLOGICAL EVALUATION; NATURAL-PRODUCTS; INHIBITORS; OXAZOLE; OXAZOL-5(4H)-ONES;

D O I：

10.31925/farmacia.2021.2.17

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

This paper presents the design, synthesis, characterization, and cytotoxicity evaluation of eight organic compounds that have in their molecules the 4-(4-chlorophenylsulfonyl)phenyl moiety: four acyclic precursors derived from phenylalanine (one N-acyl-alpha-amino acid, one N-acyl-alpha-amino acyl chloride, and two N-acyl-alpha-amino ketones), and four cyclization products: one 1,3-oxazol-5(4H)-one, and three 1,3-oxazoles substituted in 5-position with phenyl, p-tolyl, and m-xylyl group, respectively. Structures of synthesized compounds were confirmed by elemental analysis and spectral methods (UV-Vis, FT-IR, MS, H-1 and C-13-NMR). The compounds purity determination was performed by RP-HPLC. Cytotoxic effect of synthesized compounds was evaluated on Daphnia magna crustacean.

引用

页码：314 / 324

页数：11

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