This paper describes the unexpected outcome of the lithium hydroxide hydrolysis of the NXO-compound Boc-NPheO-OMe (1) and an independent synthesis of the product thus obtained, as well as the synthesis of 1,2,5 triazine-3,4,7- trione from 1. We submit these results for discussion to ECSOC 13 and hope to receive constructive comments and suggestions.

The preparation of 3-O-methyl-1,2-O-(S)-trichloroethylidene-α-D-xylo-furanuronic acid and 3-O-methyl-1,2-O-(R)-trichloroethylidene-α-D-xylo-furanuronic acid starting from β-chloralose and α-chloralose are described. All new products were characterized by 1H NMR, 13C NMR and FTIR. Antibacterial potency of the product (6b) was determined in term of inhibition zone diameter and results showed that this compound showed moderate activity against the tested microorganisms with inhibition zones ranging from 10 to 22 mm.

Objectives: NL197 is a derivative from 4(3H)- quinazolinon and it has been reported to possess central and peripheral effect as well as learning and memory enhancing effect in vivo test. In this present study, we focus on the anticonvulsant effect of NL197 on pentylentetrazol or strychnine induced- seizure mice. Methods: The anticonvulsive activity of NL197 is investigated in experimental seizure models in mice inducing by chemo-convulsant such as pentylenetetrazole (PTZ) 100 mg/kg, SC or strychnine (STN) 2 mg/kg, SC. The anticonvulsive potent of NL197 is also made comparison with that of diazepam 5 mg/kg, PO. Results: In PTZ induced- seizure model, anticonvulsant activity of NL197 NL was determined at the dose of 50 mg/kg, 73.2 mg/kg, and 100 mg/kg. In strychnine induced- seizure model, NL 197 had anticonvulsant activity at dose of 50mg/kg, 73.2mg/kg. No effect was determined with NL197 at dose of 37mg/kg. The protective potent of NL197 againsts PTZ- or STN induced seizures is equal to that of diazepam 5mg/kg, PO at the dose of 73.2 mg/kg and 50 mg/kg, SC, respectively. Conclusions: These present results provided evidence that NL197 has potential anticonvulsant activity in pentylentetrazol or strychnine induced-seizure model in mice as well as diazepam, a standard antiepileptic drug.

Background: Abelmoschus esculentus L. Malvaceae is used for a long time as a daily food in many countries because of its nourishing components. Extracts from Abelmoschus esculentus have been known to ameliorate not only hyperglycemia but also hyperlipidemia in diabetic mice induced by alloxan and streptozocin. However, its hypolipidemic activity has not yet been studied clearly. Objective: Hypolipidemic activity of the extracts from total plant by dichloromethan (AE1), methanol (AE2) and from fruit by dichloromethan (AE3) and methanol (AE4) was studied and compared to that of simvastatin (Zocor®). Methods: Hyperlipidemia in mice was induced by single intra-peritoneal injection of 300 mg/kg of Tyloxapol. Studied extracts were orally administered at dose equivalent to 30g of dry extract/kg immediately after Tyloxapol injection. Results: Cholesterol levels decreased 56.45(percent), 55.65(percent), 41.13(percent), 40.50(percent) and 53.63(percent) respectively in groups orally administered AE1, AE2, AE3, AE4 and simvastatin as compared to the tyloxapol injected group. Triglycerids levels in treated groups had no significant difference as compared to simvastatine group except methanolic extract from fruit (AE4) administered group. Conclusion: Abelmoschus esculentus is also useful in diminishing cholesterol and triglycerids levels in hyperlipidemic mice.

Five benzo[a]phenoxazinium dyes containing alkyl chains with twenty carbon atoms on 5- or 9-positions of the tetracyclic ring were efficiently synthesised and characterised by UV/Visible and fluorescence spectroscopy. The absorption and emission maxima in ethanol lie in the range 627-641 nm and 645-676 nm, respectively, with quantum yields varying from 0.14 to 0.38. Preliminary photophysical studies in zwitterionic (2,3-bis(palmitoyloxy)propyl 2- (trimethylammonio)ethyl phosphate, DPPC) and cationic (N,N-dimethyl-Noctadecyloctadecan- 1-aminium bromide, DODAB) vesicles are reported showing that these molecules are able to detect the gel to liquid-crystalline lipid phase transition through variations either in H-aggregation extent or in an acid-base equilibrium.

Several fluorescent benzo[a]phenoxazinium chlorides possessing undecylamino chains with non-functionalised (methyl group) or functionalised terminals (hydroxyl, carboxylic acid and the ester group) as substituents at the 5-position of the heterocycles were used in photophysical studies with DNA. It was found that the functionalised terminal has a dramatic influence on the type of interaction with the hydroxyl group promoting intercalation, while the ester group promotes groove binding.

A series of five chrysin derivatives was synthesized and examinated for their antiinflammatory activities. The in vivo anti-inflammatory activity of synthetic compounds was carried out using the model of carrageenan induced mice paw edema. The results showed that methylation of 5,7- dihydroxyl groups of chrysin resulted to increase the in vivo bioactivity in comparison with the corresponding chrysin derivatives having two free hydroxyl groups. The introduction two halide groups into B ring at 6 and 8 positions of chrysin did not to improve any significant increase positive effect on the in vivo bioactivity.

With the aim to find out the structural features for the MAO inhibitory activity and selectivity, in the present communication we report the design, synthesis and pharmacological evaluation of a new series of 8-bromo-6-methyl-3-phenylcoumarin derivatives without substituent and with different number of methoxy substituent in the 3-phenyl ring. The substituent in this new scaffold was introduced in the 3', 4' and/or 5' positions of the 3-phenyl ring of the coumarin moiety. The synthesized compounds 3-6 were evaluated as MAO A and B inhibitors using R-(-)-deprenyl (selegiline) and Iproniazide as reference inhibitors, showing, most of them, MAO-B inhibitory activities in the nanomolar range. Compounds 3 (11.05±0.81 nM), 4 (3.23±0.49 nM) and 5 (7.12±0.01 nM) show higher activity than selegiline (IC50 = 19.60 nM), and high MAO-B selectivity with 9,050- fold, 30,960-fold and 14,045-fold inhibition levels, with respect to the MAO-A isoform.

The present work shows the syntheses, characterizations and investigations of the thermal-oxidative properties by TG-DTG of two phosphorus compounds derived from Cashew Nut Shell Liquid (CNSL). The phosphorus compounds obtained show significant thermal stability resistance: Ti (compound 1, main degradation step) = 202 °C and Ti (compound 2) = 231 °C. The degradation of lubricant commences at 91 °C, and after synthesized compounds incorporation, the degradation commences at 152 and 156 °C, respectively.

Background: Epilepsy is one of the most common neurological disorders, affecting about 1% of the world's population. The currently available anticonvulsants are effective in reducing the severity and number of seizures in less than 70% of patients. Moreover, their usage is associated with undesirable side effects ranging from cosmetic (gingival hyperplasia) to life threatening (hepatotoxicity, megaloblastic anemia). Therefore, the continued search for the safer and more effective antiepileptic drugs is urgently necessary. Literature survey reveals that various derivatives of quinazolinone, thienopyrimidine and pyridopyrimidine shown very promising anticonvulsant activity along with other pharmacological activities. So we concentrate our aim to screen novel quinazolinone fused with thienopyrimidine/pyridopyrimidine. Result: A novel series of 1,2,9,11-tetrasubstituted-7H-thieno[2',3':4,5]pyrimido[6,1-b]-quinazolin-7-ones (1–15) and 1,3,10,12- tetrasubstituted-8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-ones (16-36) were synthesized by reported method. The anticonvulsant activity of all the new compounds (1-15 and 16-36) was evaluated against Maximum Electroshock (MES) induced seizures and against subcutaneous pentylenetetrazole (scPTZ) induced seizures model in mice. The neurotoxicity was assessed using the Rotorod procedure. All the compounds tested were administered intraperitoneally at a various dose levels ranging from 15-175 mg/Kg body weight and the median toxic dose (TD50) and the protection index (PI) values were determined. All test compounds exhibited good activity. The structure–activity relationships based on the results obtained for these series were also studied. Conclusion: The present study indicates that fused quinazolinones shown very good anticonvulsant agents. In both series, electronwithdrawing substitutions showed more activity. Among all the tested compounds, 10,12-dibromo-1-(4-chloro-phenyl)-3-(4-tolyl)- 8H-pyrido[2',3':4,5]pyrimido[6,1-b]quinazolin-8-one 29 and 10,12-dibromo-3-(4-chloro-phenyl)-1-phenyl-8H-pyrido[2',3':4,5] pyrimido[6,1-b]quinazolin-8-one 25 were found to be most potent.