IN SILICO AND EXPERIMENTAL STUDIES FOR THE DEVELOPMENT OF NOVEL OXAZOL-5(4H)-ONES WITH PHARMACOLOGICAL POTENTIAL

被引：6

作者：

Rosca, Elena Valentina ^{[1
]}

Apostol, Theodora Venera ^{[1
]}

Chifiriuc, Mariana Carmen ^{[2
,3
]}

Pircalabioru, Gratiela Gradisteanu ^{[2
,3
]}

Draghici, Constantin ^{[4
]}

Socea, Laura Ileana ^{[1
]}

Olaru, Octavian Tudorel ^{[5
]}

Nitulescu, George Mihai ^{[6
]}

Pahontu, Elena Mihaela ^{[7
]}

Hrubaru, Madalina ^{[4
]}

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] Univ Bucharest, Res Inst, ICUB, 1-3 Portocalelor Alley, Bucharest 060101, Romania

[3] Univ Bucharest, Fac Biol, Microbiol Dept, 1-3 Portocalelor Alley, Bucharest 060101, Romania

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

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

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

[7] Carol Davila Univ Med & Pharm, Gen & Inorgan Chem Dept, Fac Pharm, 6 Traian Vuia St, Bucharest 020956, Romania

来源：

FARMACIA | 2020年 / 68卷 / 03期

关键词：

oxazol-5(4H)-one; spectral characterization; cytotoxicity; antimicrobial activity; CYTOTOXICITY EVALUATION; ANTIBACTERIAL ACTIVITY; HETEROCYCLIC-COMPOUNDS; BIOLOGICAL EVALUATION; THIAZOLE SYNTHESIS; DERIVATIVES; OXAZOLE; DESIGN; 1,3,4-THIADIAZOLE; 1,2,4-TRIAZOLE;

D O I：

10.31925/farmacia.2020.3.10

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

New 2-(4-(4-X-phenylsulfonyl)phenyl)-4-(3-bromo/3-bromo-4-methoxy-benzylidene)oxazol-5(4H)-ones have been synthesized by reaction of some 2-(4-(4-X-phenylsulfonyl)benzamido)acetic acids derivatives with 3-bromobenzaldehyde or 3-bromo-4-methoxybenzaldehyde. The structures of the newly obtained heterocycles were elucidated by IR, H-1-NMR, C-13-NMR, mass spectra and elemental analysis. The cytotoxicity of the new oxazolones was evaluated using Artemia salina and Daphnia magna organisms and the in vitro antimicrobial activity was assessed on Gram-positive and Gram-negative bacterial and fungal strains.

引用

页码：453 / 462

页数：10

共 50 条

[41] ZnCl2-CATALYSED SYNTHESIS OF NOVEL 4-ARYLAZO-3-METHYL-1-(H/PHENYL)-1H-PYRAZOL-5(4H)-ONES
Thakre, Wasudha
Meshram, Jyotsna
INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2009, 19 (02) : 185 - 186
[42] KNOEVENAGEL CONDENSATION OF HETEROAROMATIC ALDEHYDES WITH 1-PHENYL-1H-PYRAZOL-5(4H)-ONES
Endait, Rupali S.
Karale, Bhausaheb K.
Akolkar, Hemantkumar N.
Randhavane, Pratibha V.
INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY, 2016, 26 (3-4) : 141 - 146
[43] Azidoacetic Acid Amides in the Synthesis of Substituted Arylidene-1-H-imidazol-5-(4H)-ones
Zaitseva, Snizhana O.
Golodukhina, Svetlana, V
Baleeva, Nadezhda S.
Levina, Evgenia A.
Smirnov, Alexander Yu
Zagudaylova, Marina B.
Baranov, Mikhail S.
CHEMISTRYSELECT, 2018, 3 (30): : 8593 - 8596
[44] Design and Development of Oxazol-5-Ones as Potential Partial PPAR-γ Agonist Against Cancer Cell Lines
Pal, Tanushree
Joshi, Hardik
Ramaa, C. S.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY, 2014, 14 (06) : 872 - 883
[45] Synthesis and Biological Properties of N-Acylaminoacryloylhistamines and the Corresponding 4-Arylideneimidazol-5(4H)-ones
Topuzyan, V. O.
Hovhannisyan, A. A.
Tosunyan, S. R.
Makichyan, A. T.
Hovhannisyan, N. A.
Shahkhatuni, A. A.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2023, 93 (06) : 1352 - 1359
[46] Organocatalytic Enantioselective Mannich-type Addition of 5H-Oxazol-4-ones to Isatin Derived Ketimines
Huang Qiuhong
Li Wenjun
Li Xin
CHEMICAL JOURNAL OF CHINESE UNIVERSITIES-CHINESE, 2022, 43 (08):
[47] An Efficient Synthesis of 4-Arylmethylidene-3-substituted-Isoxazol-5(4H)-ones in Aqueous Medium
Chavan, Abhijit P.
Pinjari, Avinash B.
Mhaske, Pravin C.
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2015, 52 (06) : 1911 - 1915
[48] Design, Synthesis, Pharmacological Evaluation, In silico Modeling, Prediction of Toxicity and Metabolism Studies of Novel 1-(substituted)-2-methyl-3-(4-oxo-2-phenyl quinazolin-3(4H)-yl)isothioureas
Sulthana, M. T.
Alagarsamy, V
Chitra, K.
MEDICINAL CHEMISTRY, 2021, 17 (04) : 352 - 368
[49] Synthesis of 2-Aryl-2H-1,2,3-triazoles via P(OMe)3-Promoted Intramolecular Transannulation of 4-Diazenylisoxazol-5(4H)-ones
Sakharov, Pavel A.
Koronatov, Alexander N.
Khlebnikov, Alexander F.
Petrovskii, Stanislav K.
Luginin, Maksim E.
Grachova, Elena V.
Novikov, Mikhail S.
ADVANCED SYNTHESIS & CATALYSIS, 2024, 366 (24) : 5073 - 5081
[50] Highly enantioselective allylic alkylation of 5H-oxazol-4-ones with Morita-Baylis-Hillman carbonates
Xu, Han
Sha, Feng
Wu, Xin-Yan
TETRAHEDRON, 2018, 74 (32) : 4331 - 4338

← 1 2 3 4 5 →