ABSTRACT
FTIR has been used broadly for its quick analytical rate, good reproducibility, low cost and no waste sample. The rule of infrared spectroscopic characteristics of nine 3-substituted phenyl-5-(3'-indolyl)-isoxazoline derivatives (containing phenyl and indolyl) was studied, and the influence of the substituted groups on the IR was indicated. All the 1H NMR chemical shifts of the nine novel compounds were discussed. The rule of change in chemical shifts is the same as that of IR. The study will provide a new way of elicitation for studies on the spectroscopy of this kind of compounds.
Subject(s)
Indoles/chemistry , Isoxazoles/analysis , Magnetic Resonance Spectroscopy/methods , Phenol/chemistry , Spectrophotometry, Infrared/methods , Isoxazoles/chemistry , Molecular StructureABSTRACT
AIM: A series of new 1,4-pentadien-3-one derivatives were synthesized to search for new Eight novel hydroxylated non-steroidal anti-inflammatory drugs (NSAIDs) with potent activity. METHODS: E,E-1-(3'-indolyl)-5-( substituted phenyl)-1,4-pentadien-3-one derivatives were synthesized by means of aldol condensation and characterized by 1H NMR, ESI-MS and element analysis. Their anti-inflammatory activity in vitro were evaluated. RESULTS: Preliminary in vitro pharmacological tests showed that all compounds exhibited anti-inflammatory activity. CONCLUSION: Compounds 4d and 4e exhibited potent anti-inflammatory activity and their anti-inflammatory activity was comparable to resveratrol, and were worthy of further study.
Subject(s)
Alkadienes/chemical synthesis , Anti-Inflammatory Agents/chemical synthesis , Indoles/chemical synthesis , Macrophages, Peritoneal/metabolism , Tumor Necrosis Factor-alpha/metabolism , Alkadienes/pharmacology , Animals , Anti-Inflammatory Agents/pharmacology , Indoles/pharmacology , Macrophages, Peritoneal/cytology , Male , MiceABSTRACT
(R/S)-4,4'-Dimethoxy-5,6,5',6'-dimethenedioxy-2,2'-di-(4(S)-methyl-oxazoline-1)-biphenyl has been synthesized from dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethenedioxy-biphenyl-2,2'-dicarboxylate, and then the diastereoisomer mixture was almost fully converted to a single diastereoisomer with S-configuration ((S)-3) through the key configuration transform promoted by CuI, which was confirmed by CD, HPLC and (13)C NMR. The C(2)-symmetric biphenyl, (S)-dimethyl-4,4'-dimethoxy-5,6,5',6'-dimethenedioxy-biphenyl-2,2'-dicarboxylate was prepared easily via the hydrolysis and ester exchange of (S)-3.
Subject(s)
Biphenyl Compounds/chemical synthesis , Dicarboxylic Acids/chemical synthesis , Biphenyl Compounds/chemistry , Cyclooctanes/chemical synthesis , Cyclooctanes/chemistry , Dicarboxylic Acids/chemistry , Lignans/chemical synthesis , Lignans/chemistry , Molecular Conformation , Polycyclic Compounds/chemical synthesis , Polycyclic Compounds/chemistry , StereoisomerismABSTRACT
AIM: To synthesize new fluoroquinolone analogues as antibacterial compounds. METHODS AND RESULTS: By reaction of acryl chloride(chloro-carbonic ester) with sodium sulfocyanate, acyl isosulfocyanic ester were easily obtained. Twelve 7-(4-acylamino-thiocarbamoyl-1-piperazinyl) fluoroquinolone analogues (1-12) were synthesized through modifying the 7-piperazine of norflorxacin and ciprofloxacin with isosulfocyanic ester synthesized above. The structures of synthesized compounds were characterized by 1HNMR, IR and elemental analysis. CONCLUSION: Antibacterial activities of the new compounds were evaluated in vitro compared with norflorxacin. Compounds 5, 7, 10 and 12 showed antibacterial activities.
