Purified synthesized prodrugs were characterized by m.p., TLC, solubility, partition coefficients, elemental analyses, UV, FTIR, NMR and MS. Ten prodrugs of FB were synthesized by amidation with ethyl esters of amino acids, namely, glycine, L-phenylalanine, L-tryptophan, L-valine, L-isoleucine, L-alanine, L-leucine, L-glutamic acid, L-aspartic acid and b alanine. The study was aimed to retard the adverse effects of gastrointestinal origin.
#MIANA KASSIS FREE#
The essential structural features responsible for interaction with receptor site are established within a suggested pharmacophore.įlurbiprofen (FB) suffers from the general side effects of NSAIDs, owing to presence of free carboxylic acid group. Further all the compounds exhibited lesser neurotoxicity compared with standard drug. Among all the tested compounds, 4h 4-(1,3-dioxoisoindolin-2-yl)-N-(4-ethylphenyl)butanamide showed protection in various seizures model except in the scSTY model, while analog 4d was found to be the most potent compound in scPTZ model showing protection at a dose of 30 mg/kg. Most of the synthesized compounds were found to be effective in the scSTY and ipPIC models and very few compounds showed protection in the scPTZ model. Analogs 4d, 4h, and 4m displayed promising activity in scPTZ seizures model.
The compound 4a 4-(1,3-dioxoisoindolin-2-yl)-N-phenylbutanamide displayed weak anticonvulsant activity in MES test at a dose of 300 mg/kg. Anticonvulsant evaluations of all the synthesized compounds were done by using various seizures models like maximal electroshock-induced seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcutaneous strychnine (scSTY), and intraperitoneal picrotoxin (ipPIC)-induced seizure threshold tests at a dose of 30, 100, and 300 mg/kg body weight and anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration. All the synthesized compounds were confirmed and characterized by using various spectral technique like (IR, 1H NMR, 13C NMR, and mass spectroscopy) studies. The compound 3 was synthesized by treating GABA and phthalimide at high temperature under anhydrous conditions.
#MIANA KASSIS SERIES#
Key words: Imidazole, Synthesis, Biological activity.Ī series of new γ-aminobutyric acid (GABA) derivatives was obtained from 4-(1,3-dioxoisoindolin-2-yl)butanoic acid by coupling it with various substituted amines by using DCC as coupling reagent. The aim of this review is to summarize methods for synthesis of imidazole scaffold containing compounds, their chemistry and biological activity. Imidazole derivatives have been used for various biological activities as antibacterial, antifungal, anti-viral, anti-cancer, antidepressant and so on. There are numerous methods for synthesis of imidazole and its derivatives such as Debus synthesis, Ra diszewrki, Mannich, Wallach, Microwave assisted, one pot synthesis and etc. cimetidine, azomycin, ketoconazole and metronidazole. It is also present in the structure of many natural or synthetic drug molecules, i.e. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine, nucleic acid, oroidin, sceptrin, ageliferin, stevensine, dragmacydin and etc. The two nitrogen atoms are arranged in the 1st and 3rd positions. Imidazole (1,3-diaza-2,4-cyclopentadiene) with molecular formula C3H4N2, is a planar five-member heterocyclic ring system with three carbon and two nitrogen atoms.
This articles aims to review the work reported, their chemistry and biological activities of imidazole during past years. Numerous methods for the synthesis of imidazole and also their various structure reactions offer enormous scope in the field of medicinal chemistry. Imidazole drugs have broadened scope in remedying various dispositions in clinical medicines. The high therapeutic properties of the imidazole related drugs have encouraged the medicinal chemists to synthesize a large number of novel chemotherapeutic agents. The incorporation of the imidazole nucleus is an important synthetic strategy in drug discovery. Imidazole derivatives have occupied a unique place in the field of medicinal chemistry. Being a polar and ionisable aromatic compound, it improves pharmacokinetic characteristics of lead molecules and thus used as a remedy to optimize solubility and bioavailability parameters of proposed poorly soluble lead molecules. The imidazole ring is a constituent of several important natural products, including purine, histamine, histidine and nucleic acid. Imidazole is a planer five-member heterocyclic ring with 3C and 2N atom and in ring N is present in 1 st and 3 rd positions.
0 kommentar(er)
