Letters in Drug Design & Discovery - Volume 9, Issue 7, 2012

In this study we present synthesis and biological evaluation of derivatives of 4-fluorobenzoic acid and 2,3- dihydro-1H-cyclopenta[b]quinoline towards inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Synthesis of acquired molecules involved the reaction of condensation between the activated 4-fluorobenzoic acid and amino derivatives of 2,3-dihydro-1H-cyclopenta[b]quinoline. Biological test Read More

A series of 2-thiohydantoins were prepared as somatostatin subtype 4 (sst4) ligands. Reaction of a Nsubstituted- L-tryptophan methyl ester with an isothiocyanate in the presence of triethylamine readily afforded the target compounds. The 2-thiohydantoins were evaluated for binding affinities in cell lines expressing somatostatin receptor subtypes 2A (sst2A) and 4 (sst4). Compared to the thiourea NNC-26-9100 (3), all 2-thiohydan Read More

Ingested L-serine reduces the locomotor activity of socially isolated rats, but its effects on brain function and its underlying mechanisms of action have not yet been fully clarified. D-Serine is synthesized from L-serine by serine racemase and intraperitoneal injection of this D-amino acid attenuates depressive-like behavior in rats. We therefore hypothesized that oral intake of L-serine would stimulate the metabolism of L-s Read More

Human Topoisomerase IIα (htopoIIα) is an approved and validated target for designing anticancer agents. Among the various methods to block the functions of htopoIIα, targeting ATP site for its competitive inhibition has been relatively less investigated. Therefore, to identify some novel htopoIIα inhibitors to target the ATP-binding site, we designed and synthesized a small library of 5-aryl-1,3,4-thiadiazole coupled phthali Read More

This study evaluated the antioxidant activity of five resveratrol analogs using the DPPH method. The molecules activity was related with their chemical structure. Besides descriptive statistics, the analysis of variance (ANOVA) followed by Tukey’s post hoc test were performed (p<0.05). The antioxidant activity of analogs A and B was statistically similar with each other and from the reference standard resveratrol, possibly du Read More

Sixteen C-2-substituted quinolines were tested in both human cancer cell lines (MCF-7, H-460 and SF-268) and normal cell lines (Vero and THP-1). Preliminary results indicate that 2-α-furyl- and 2-γ-pyridinyl quinoline derivatives 1, 13 and 14 are active against three human cancer cell lines and, at the same time, were devoid of cytotoxic effect on normal cells. Biological activity and SAR results were compared with different mole Read More

A new series of 1,2,4-triazole derivatives 3a-i of (E)-4-(4-substitutedbenzylideneamino)-3-((5-phenyl-1,3,4- oxadiazol-2-yl)methyl)-1H-1,2,4-triazole-5(4H)-thione (2) were synthesized, deriving from 4-amino-3-((5-phenyl-1,3,4- oxadiazol-2-yl)methyl-1H-1,2,4-triazole-5(4H)-thione (1). The compounds were elucidated by IR, 1H NMR, 13C NMR, MS and elemental analyses. These compounds were screened for their antimicro Read More

There is a need to develop new antischistosomal compounds when the only available therapeutic agents praziquantel large-scale used in the world. A series of novel aminoalcohol derivatives bearing 4-phenylphenol moiety were designed and synthesized. The structures of all the newly synthesized compounds were identified by elemental analysis, 1H-NMR, 13C-NMR and LC-MS. Their biological activities were evaluated a Read More

Leishmaniasis is a poverty related disease caused by protozoan parasites belonging to the genus Leishmania. No effective vaccine is presently available to treat this disease. The present study identifies specific epitopes in highly antigenic peptides of Leishmania infantum. Interestingly we found amastin like surface proteins as relevant markers for vaccine development for design of epitopes. A major glycoprotein GP63 leis Read More

Lipinski’s rule of five is well received throughout the world and widely used as one of the basic filters to screen ligands for their druggability. In this direction, we have studied 148 biologically active natural products which are available as drugs. Physicochemical parameters such as molecular weight, logP, hydrogen bond donors, hydrogen bond acceptors, number of aromatic rings, molar refractivity and Gibbs free energy wer Read More

A new series of 2,3-disubstituted thiazolidin-4-ones were synthesized from the appropriate amines, substituted aldehyde, and mercaptoacetic acid in the presence of DCC in anhydrous THF by microwave irradiation. The title compounds were investigated for their anticonvulsant activity. Among the test compounds, compound 2-(4- bromophenyl)-2-methylthiazolidin-4-one-3-isonicotinamide (8) emerged as most active compound Read More