Abstract: In this study the extract of the Iraqi herb Avena sativa L. (Gramineae) was done by using of 70% ethanol as a solvent, then study the antimicrobil activity of the extract (in vitro) on gram positive bacteria (Staphylococcus aureus), and gram negative bacteria (E. coli, Proteus vulgaris, Pseudomonas aerugiuosa, and Klebsiella), A. niger, and Candida extrat showed considerable activity against all bacteria and fungal.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: We report the improved synthesis of the antiviral 6-fluoro-3-hydroxy-pyrazine-2-carboxamide (T-705).

Abstract: Chalcones and their heterocyclic analogues are known to possess a broad spectrum of biological effects. The present study is devoted to the synthesis of 3,4- Dimethoxy-2'-Hydroxy-5'-methyl chalcone and its derived products i.e. flavanone, flavonol, flavone, aurone, isoxazoline, chalconeimine and acetoxy chalcone. These newly synthesized compounds were screened for their antibacterial and anti-fungal activities.

Abstract: A great deal of work has been done on the synthesis of oxazolones. We have obtained 5(4H)-oxazolones by condensing anthracene-10-carbaldehyde & furan-2- carbaldehyde with a number of substituted benzoyl glycines, and tried to design new and effective anti-bacterial agents.

Abstract: 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.

Abstract: 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.

Abstract: 5-BromoVerongamine has been successfully synthesized in 2 steps in good yield from readily available starting materials. Structural elucidation has been confirmed through direct comparison with spectroscopic data of isolated natural product. 5-BromoVerongamine has been shown to have moderate bacteriacidal activity against MRSA.

Abstract: The association constants Kb of three receptors (I-III), designed to have both enhanced hydrogen bonding donor strength and conformational preorganization, with biotin analogues (1-5) are reported. 1H-NMR titrations using the saturation conditions have been employed to determine the association constants Kb.

Abstract: In this study, a series of five ring-substituted 2-styrylquinazolin-4(3H)-one and five ring-substituted 4-chloro-2-styrylquinazoline derivatives were prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains. Several compounds showed biological activity comparable with or higher than the standard isoniazid. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed, as well as their structure-activity relationships (SAR).

Abstract: Experimental–theoretical works explain the energetics of the packing of a virus with deoxyribonucleic acid (DNA) and the injection of the DNA into a cell. Washing has a limited effect on enteric viruses in food. Alternatives are needed to acidic matrixes. Feline calicivirus is not a good control model. Various protocols are being prepared. New challenges are: new methods, impact of new technologies, significance of detection, new virus models and emergent–re-emergent viruses. The forthcoming step is to re-develop the virus to direct it and contain the most common contaminants in food: salmonella, listeria, staphylococcus and Mycobacterium tuberculosis.

Abstract: The synthesis and the physicochemical characterization of a new contrast agent for magnetic resonance imaging (MRI), Gd-C4-thyroxin-DTPA, which has a high affinity for human serum albumin (HSA), are reported. The results show that this chelate is characterized by a relatively high relaxivity, which increases moreover with the concentration. This reflects an aggregation of the molecules in solution. It is also characterized by a better stability versus the transmetallation with the zinc ion than the parent compound, the Gd-DTPA (Magnevist®, Bayer Healthcare). The study of its interaction with human serum albumin was performed by the proton relaxometry technique, which has revealed a relatively high affinity (Ka of the order of 10000 M-1, with 2 binding sites). Finally, competition experiments with ibuprofen and salicylate, of which the binding sites on HSA are known, were performed by the NMR diffusometry method. The results suggest that the chelate shares one of the binding site of ibuprofen.

Abstract: This study describes a promising one-pot synthesis of [2-(5-benzyl-4-phenyl-4H- [1,2,4]triazol-3-thio)-acetyl]-amino acid methyl esters 6a-h and dipeptides 10a-e were successfully synthesized starting from amino acid esters 5a-h, 9a-e and azides 4, 8a,b respectively. On the other hand, azide 4 underwent Curtius rearrangement to the corresponding isocyanate which subsequently reacted with selected aliphatic and/or aniline derivatives to give the corresponding urea derivatives 11 and 12a, b. Also reaction of isocyanate with secondary amines gave amide derivatives 13a, b.

Abstract: A library of 19 novel 4-(4-phenylpiperazine-1-yl)benzamidines has been synthesized and evaluated in vitro against Pneumocystis carinii. Among these compounds, N-ethyl and Nhexyl 4-(4-phenylpiperazine-1-yl)benzamidines emerged as the most promising compounds with inhibition percentages at 0.1μg/ml of 61(percent) and 56(percent) respectively.

Abstract: The synthesis of a new disazo dyes containing 4,4'-diaminostilbene-2,2'-disulfonic acid as middle component is presented. The synthesized dye was analyzed by thin layer chromatography (TLC), electronic spectra (VIS) and HPLC technique. The structure was elucidated by FT/IR and 13CNMR spectroscopy. The colouristic evaluation of the synthesized dye indicates that this dye could be ranged as a direct dye, suitable for application on cellulosic substrates. Further, an in vivo imagistic skin study was performed in order to evaluate the individual human skin tolerance for this new disazo dye.

Abstract: Skin penetration enhancers are used to allow formulation of transdermal delivery systems for drugs that are otherwise insufficiently skin-permeable. The series of seven esters of 6-(2,5-dioxopyrrolidin-1-yl)-2-(morpholin-4-yl)hexanoic acid as potential transdermal penetration enhancers was formed by multistep synthesis. The general synthetic approach of all newly synthesized compounds is presented. Structure confirmation of all generated compounds was accomplished by IR, 1H, 13C NMR and HR-MS spectroscopy. All the prepared compounds were analyzed using RP-HPLC method for the lipophilicity measurement and their lipophilicity (log k) was determined.

Abstract: A concise approach towards trisubstituted optically active azetidines, including a study of the scope and limitations of the synthetic sequence, is reported. The synthesis comprises the L-proline organocatalyzed three component reaction between substituted benzaldehydes, anilines and an enolizable aldehyde, followed by the in situ reduction of the resulting β-aminoaldehydes to the corresponding β-aminoalcohols and final intramolecular cyclization of the latter by way of the intermediate tosylates.

Abstract: A series of halogen containing 1,4-naphthoquinon derivatives (1-4,5a-f) were synthesized and studied for their antifungal activities against C. albicans ATCC10231, C. albicans 955, T. mentagrophytes and M. gypseum. The results indicate that compound 2-hydroxy-3-chloro-1,4-naphthoquinone (2), 2-(N-acetyl)- acetamido-3-chloro- 1,4-napthoquinone (3) and 2-(N-acetyl)-acetamido-3-chloro- 1,4- napthoquinone (4) have potent antifungal activity. Among these promising antifungal candidates, 2 and 4 showed better activity than that of clinically antifungal drug clotrimazole (MIC = 8 μg/ml) with MIC = 1 μg/ml and 4 μg/ml, respectively against C.albicans ATCC10231. Compound 2 also exhibited an extremely potent activity (MIC = 0.25 μg/ml) against C.albicans 955 strain compared with clotrimazole (MIC = 16 μg/ml). Structure and activity relationship (SAR) study demonstrated that replacing of 3-position in 1,4- naphthoquinon by a Cl group is essential for antifungal activity. Meanwhile, antifungal activity was decreased considerably when the hydrogen atom at position-2 in naphthoquinone structure were replaced by a bulky group (e.g. diacetyl of phenyl group).

Abstract: Polymorphism of active pharmaceutical ingredients (APIs) gets increasing attention as an important physico-chemical parameter influencing bioavailability and stability of API and pharmaceuticals. Co-crystals of API with common pharmaceutical excipients become very important as a tool to tune up solubility and absorption. Bisphosphonates (e.g. alendronate, risedronate, ibandronate) are widely used in clinical practice. They are indicated for the treatment and prevention of osteoporosis. They are powerful inhibitors of bone resorption, but their gastrointestinal adsorption is only about 1(percent) due to their high hydrophilicity. Some experiments were designed to prepare co-crystals of ibandronate. In the present study various mixtures of ibandronate and excipients were prepared. All the prepared mixtures (solid compounds) and/or new entities were analyzed by means of FT-NIR spectroscopy. The absorption of potential new co-crystals was investigated by means of the PAMPA experiments.