Synthesis, lipophilicity and antimicrobial activity evaluation of some new thiazolyl-oxadiazolines.
نویسندگان
چکیده
BACKGROUND AND AIMS Synthesis of new potential antimicrobial agents and evaluation of their lipophilicity. METHODS Ten new thiazolyl-oxadiazoline derivatives were synthesized and their structures were validated by 1H-NMR and mass spectrometry. The lipophilicity of the compounds was evaluated using the principal component analysis (PCA) method. The necessary data for applying this method were obtained by reverse-phase thin-layer chromatography (RP-TLC). The antimicrobial activities were tested in vitro against four bacterial strains and one fungal strain. RESULTS The lipophilicity varied with the structure but could not be correlated with the antimicrobial activity, since this was modest. CONCLUSIONS We have synthesized ten new heterocyclic compounds. After their physical and chemical characterization, we determined their lipophilicity and screened their antimicrobial activity.
منابع مشابه
Synthesis and Antimicrobial Activity of Some 2-[(4-Substituted-Phenyl-3-Chloro-Azetidin-2-One)-5-(2'-Methylamino-4-Phenyl-1', 3'-Thiazolyl-]-1, 3,4-Thiadiazoles
A new 2-[(4-substituted-phenyl-3-chloroazetidin-2-one)-5-(2'-methylamino 4-phenyl-1', 3'-thiazolyl-]-1, 3, 4-thiadiazoles, 5(a-n) were synthesized from 2-substituted-benzylideneamino-5-[2'-methylamino-4'-phenyl-1',3'-thiazolyl]-1,3, 4-thiadiazole, 4(a-n) using 2-amino-4phenyl-1, 3-thiazole as a starting material. The synthesised compounds have been screened in vitro for their antimicrobial acti...
متن کاملSynthesis and Pharmacological Evaluation of Some Novel Isatin Derivatives for Antimicrobial Activity
In the present work, a series of new 5-substituted-3-(4-arylimino)-1-[5-mercapto(1,3,4-oxadiazolyl)]-methyl-indol-2-one (4a-g) have been synthesized by heterocyclization of 5-substituted-3-(4-arylimino)-2-oxo-1-indole acetylhyrazide (3a-g) on treatment with CS2 in ethanolic KOH. The compound 4a was characterized by its elemental analysis, IR, 1HNMR and Mass Spectroscopy. The synthesized compoun...
متن کاملSynthesis of New Pyridine Based 4-Thiazolidinones Incorporated Benzothiazoles and Evaluation of Their Antimicrobial Activity
Substituted Schiff bases (hydrazones) 5a-j have been prepared from the starting material 2-chloro pyridine-3-carboxylic acid 1 by a sequence of reactions like reaction with 2-amino-6-nitro benzothiazole (Ullamann condensation), thionyl chloride, hydrazine hydrate and different aromatic aldehydes. On cyclocondensation of 5a-j with thioglycolic acid in dry 1,4-dioxane furnished desired compounds ...
متن کاملSynthesis and evaluation of the antimicrobial activity of spiro-4H-pyran derivatives on some gram positive and gram negative bacteria
Infections are one of the most important causes of death, disability and inappropriate conditions for millions of people around the world. Therefore, the development in prognosis, prevention and treatment of infectious diseases made a considerable progress in designing and synthesis of new antimicrobial drugs. Nowadays, due to the increase in microbial resistance, discovery of new compounds wit...
متن کاملSynthesis and evaluation of the antimicrobial activity of spiro-4H-pyran derivatives on some gram positive and gram negative bacteria
Infections are one of the most important causes of death, disability and inappropriate conditions for millions of people around the world. Therefore, the development in prognosis, prevention and treatment of infectious diseases made a considerable progress in designing and synthesis of new antimicrobial drugs. Nowadays, due to the increase in microbial resistance, discovery of new compounds wit...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
- Clujul medical
دوره 88 4 شماره
صفحات -
تاریخ انتشار 2015