Letters in Drug Design & Discovery - Volume 9, Issue 5, 2012

We previously reported that the phenanthroindolizidine alkaloid 3 and its derivatives had markedly potent in vitro cytotoxicity. However, they had low in vivo antitumor activities and high in vivo toxicities, which was a serious problem for further development. Based on the finding that antitumor activity and toxicity could be improved by acetylation of 3, we synthesized new derivatives of 3, which possessed various acyl groups, an Read More

The new series of N-(methylene-4-oxo coumarinyl)anilines 1-13 was synthesised and screening of different solvents led to the discovery of high boiling alcohols as the suitable candidate for one pot efficient three component reaction. Particularly in 2-butanol the product was precipitated out in excellent yields without the hassle of purification. The product distribution of Z and E-isomers was established by 1HNMR. These comp Read More

Several 4H-pyrano[3,2-h]quinoline 3,4,7-9, 7H-pyrimido[4',5':6,5]pyrano[3,2-h]quinoline 10a,b and 14Hpyrimido[ 4',5':6,5]pyrano[3,2-h][1,2,4]triazolo[1,5-c]quinoline 11a-c derivatives were obtained by treatment of (E) 2-(4- chlorostyryl)-8-hydroxyquinoline 1, (E) 2-amino-4-(4-chlorophenyl)-9-(4-chlorostyryl)-4H-pyrano[3,2-h]quinoline-3- carbonitr-ile 3 or (E) 9-amino-7-(4-chlorophenyl)-2-(4-chlorostyryl)-8-imino- Read More

A new series N-substituted -2-piperidine-4-yl-2H-benzotriazole (6a-6r) have been synthesized from 4-oxopiperidine- 1-carbaxylic acid tert-butyl ester. The new compounds were screened for their antibacterial activity against Gram positive bacteria (Bacillus subtilis, Bacillus megaterium, Bacillus pumilis, Staphylococcus aurius, Enterobactor aerogens and Streptococcus pyrogens) and Gram negative bacteria (Escherichia c Read More

In the present study, a series of chalcone derivatives were designed based on QSAR analysis. The designed compounds were synthesized by Claisen Schmidt condensation and evaluated for anti-inflammatory, antioxidant and antiulcer activities. The results of the best 2D & 3D QSAR models suggested that by introducing electron releasing groups at R2 and introducing heteroatom with increasing bulkiness at R4 in the benzyli Read More

Irritable bowel syndrome is the most common functional gastrointestinal disorder characterized by chronic abdominal pain or discomfort in association with a change in bowel habit. 5-HT receptor modulators have been developed as IBS therapeutic agents and proved to be effective in the treatment of the disease. In this letter, 12 berberine derivatives were designed and synthesized as 5-HT receptor modulators. Prelim Read More

This study focuses on the physico-chemical characterization of surfactant nanovectors according to the evidence that the knowledge of nanocarrier properties is a necessary step to translate their potentiality to nanomedicine applications. In particular, in this investigation we have prepared deformable surfactant vesicles (dSV) and characterized them in terms of dimensions, zeta-potential, deformability index and stability. Al Read More

The five dose comparative CNS Cancer Cell Line cytotoxicity profiles of N9-[4'-Chloro-2'-butynyl-1'-yl]-2,6- dichloropurine 1, Bis- 6,9-[4'-chloro-2'-butynyl-1'-yl]-thioguanine 2, Bis- 6,9-[4'-chloro-2'-butynyl-1'-yl]-mercaptopurine 3, Bis-6,9-[[o-(chloromethyl)phenyl]methyl]-thioguanine 4, Bis-6,9-[[o-(chloromethyl)phenyl]methyl]-mercaptopurine 5, 6-[4'-chloro-2'-butynyl-1'-yl]-thioguanine 6, and N9-[4'-Chloro-2'-butynyl-1'-yl]-6-(4- Read More

To improve the bioavailability of oleanolic acid (OA), OA-phospholipid complex (OA-PLC) was prepared and evaluated with solubility, differential scanning calorimetry, x-ray powder diffractometry, IR spectroscopy, dissolution study and pharmacokinetic characteristics in rats. Concentrations of OA after oral administration of OA-PLC and OA aqueous suspension in rats were determined by high-performance liquid chromatogra Read More

8-(Trifluoromethyl)-1,2,3,4,5-benzopentathiepine-6-amine 1a and its hydrochloride revealed significant analgesic activity in the acetic acid-induced writhing test, and ED50 of the compound 1a was 0.66 mg/kg. In the hot plate pain test, the reliable analgesic activity was found in hydrochloride 1a*HCl, whereas the free base 1a proved to be inactive. Based on the results of the naloxone test, the analgesic effect of the compound Read More

Our original aim was to evaluate in vivo nuclear uptake of a conjugate containing the SV40 T Antigen nuclear localization sequence (NLS), 6 aminohexanoic acids alternating with 7 arginines, the fluorescence dye fluorescein isothiocyanate (FITC) and the gadolinium chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA). During the confocal laser scanning microscopy examination of frozen sections Read More

Chemometric methods, structure-activity relationships (SAR), molecular modeling, and quantitative structureactivity relationships (QSAR) are some of the in silico methods widely used in medicinal chemistry, and that are found to be appropriate to be employed in food research. Some of these methodologies represent an attempt to correlate structural or property descriptors of compounds to several types of biological activities Read More

Leishmaniasis is caused by protozoan parasites belonging to the genus Leishmania. According to WHO, leishmaniasis occurs in four continents and is considered to be endemic in 88 countries, 72 of which are developing countries. Intensive effort to investigate novel compounds to counter the parasites that are resistant to existing drug molecules is necessary. This review intends to give an outline of the present state of knowled Read More

The broad and potent activity of 2-thioxo-imidazolidin-4-one (2-thiohydantoin) has established it as one of the biologically important scaffolds. This article highlights the medicinal chemistry investigations in search for novel 2- thioxo-imidazolidin-4-one derivatives with promising biological activities. New 2-thioxo-imidazolidin-4-one derivatives contain diaryl, triaryl, pyrimidine, cycloalkylamines and glucopyranosyl substituent Read More

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