This work involves to synthesisnovel organic compounds and studies their pharmacological. Approach: The title compound quinazolinone derivatives were prepared by reacting 3 amino of 3-amino-2-methylquinazolin-4(3H)-one (first) with various aldehydes and ketones, and second coupling through diazonium salts with resorcinol or with ethylacetoacetate then cyclized with hydrazine. The starting material 3-amino-2-methylquinazolin-4(3H)-one was synthesized by reacting hydrazine with 2-methyl-4H-benzo[d][1,3]oxazin-4-one, which in turn was prepared from anthranilic acid. The chemical structures of the synthesized compounds were confirmed on the basis of their spectral data (FT-IR, UV/visible, ¹HNMR, spectra and CHN analyss). All synthesized compounds were tested in vitro against a number of microorganisms (Staphylococcus aurous, E.coli, Proteus vulgaris, Pseudomonas, and Klebsiella) and two fungal Aspergillus niger and Candida albicans in order to assess their antimicrobial properties. Results: The study indicates that these compunds have high activity against tested bacteria. Aim: We aim to synthesize quinazolinone derivatives having active moieties to evaluate their antimicrobial activities. Conclusion/Recommendations: Based on the reported results, it may be concluded that 3-amino-2-methyl- quinazolin-3(4H)-one act as synthones for Schiff bases and for diazonium coupling. [Researcher 2010;2(4):82-88]. (ISSN: 1553-9865).

Efficient synthesis, besides other, of dibromide, diazide, diamine and diesters derived from (11R,12R)-9,10-dihydro-9,10-ethanoanthracene-11,12-dimethanol (3), a chiral bicyclic diol with C 2 symmetry, was developed. Esterification of 3 with saturated and unsaturated carboxylic acids and acids chlorides leads to the corresponding normal-, olefinic- and acetylenic diesters in average yields of 81%. Also more efficient techniques for the preparation of starting diol 3 in higher yields as well as for a very simple separation of DCU from reactions carried out following DCC/DMAP method are described.

The electronic, structural and spectroscopic properties of the Coumarin NKX-2697 dye in gas and water solvent by the conductor-like polarizable continuum model (CPCM) to account for soulate-solvent interactions have been investigated by means of combined DFT/TD-DFT calculations. Using time dependent density functional theory (TD-DFT), we calculate excitation energies and oscillator strengths. The spectra in the range of 470-1100 nm were found to originate from transitions.We also have investigated HOMO and LUMO levels in gas and solvent phases for this dye. Inclusion of the solvent leads to important changes of the energies and composition of the molecular orbitals of the dye.

The synthesis of symmetrical and non-symmetrical 4,6-disubstituted pyrimidines was performed by one-pot or stepwise palladium-catalyzed cross-coupling reactions respectively using indium reagents.

Skin penetration enhancers are used in the formulation of transdermal delivery systems for drugs that are otherwise not sufficiently skin-permeable. The series of seven esters of 6-(2,5-dioxopyrrolidin-1-yl)-2-(2-oxoazepan-1-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.

Iminosugars are one of the most interesting discoveries in the field of natural products recent years due to their promissing biological activity. We report synthesis of 1-deoxynojirimycin building block using D-glucose as the starting material and the [3,3]-sigmatropic aza-Claisen rearrangement as the key step of our synthesis.

The enzyme thymidine phosphorylase (TPase) is involved in the metabolism of thymidine. It catalyses the phosphorolysis of several nucleoside analogues serving as antiviral or antitumour agents. Besides, it also plays an important role in the angiogenesis. Thus, inhibition of TPase activity may serve as a plausible therapeutic strategy for the treatment of cancer. In this report, the structure-based design, synthesis, and anti-TPase activity of a class of novel inhibitors of TPase are described using fused bicyclic 1,3,5-triazine-2,4-dione or 1,3,5-triazine-2-thioxo-4-one as the core scaffold, and the latter scaffold shows some activity in TPase enzyme assay.

We present here the preparation of the precursor for stereoselective synthesis of (+)-lactacystin starting from D-glucose. The first step is conversion of D-glucose to 1,2:5,6-di-O-isopropylidene-α-D-gulofuranose. The second step is introduction of a methyl group at C5 and preparation of compound 9. This compound can be used as a precursor of target molecule of (+)-lactacystin

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% due to their high hydrophilicity. Some experiments were designed to prepare co-crystals of risedronate. In the present study various mixtures of risedronate and excipients were prepared. All the prepared mixtures (solid compounds) and/or new entities were analyzed by means of FT-NIR, FT-Raman spectroscopy and solid state NMR.

A molecularly imprinted solid-phase extraction (MISPE) procedure based on precipitation polymerization was developed for the simultaneous extraction of dexamethasone (DM) and its structural isomer, betamethasone (BM), from biological matrices. A DM-imprinted polymer was synthetized using methacrylic acid as monomer and divinylbenzene as cross-linker, and the porogen was a mixture of acetonitrile and toluene (3:1). After removal of the template, loading, washing and elution steps were optimized. The maximun recovery of DM and BM was achieved when loading with toluene and washing with 5% acetonitrile in toluene, and eluting with 1% acetic acid in methanol.