Combinatorial Chemistry & High Throughput Screening - Volume 16, Issue 7, 2013

The aim of this study is (i) to prepare estrone-imprinted nanospheres (nano-EST-MIPs) and (ii) to integrate them into the electrochemical sensor as a recognition layer. N-methacryloyl-(l)-phenylalanine (MAPA) was chosen as the complexing monomer. Firstly, estrone (EST) was complexed with MAPA and the EST-imprinted poly(2-hyroxyethylmethacrylate-co-N-methacryloyl-(l)-phenylalanine) [EST-imprinted poly(HEMA–MAPA)] na Read More

Bioassay record of High Throughput Screening (HTS) contains compounds with high diversity. This high diversity in molecules causes an intense non-linearity into the molecular descriptors set. So to build a QSAR model covering the diversity in molecular structure is a tedious task. In the present work, a method has been proposed to extract information about pharmacophores covering a larger area in the HTS record and Read More

G protein-coupled receptors (GPCRs) are signaling molecules with a wide variety of skills. Members of this large family of membrane protein have been shown to regulate the activities of the different signaling pathways of the ligand specific manner. α2–adrenoceptors (α2-ARs) are one of the GPCRs and the stimulation of them could modulate many classical effects such as hypotension, bradycardia, etc.. Recently, α2A-AR is m Read More

TLC bioautography is a method that combines chromatographic separation and in situ biological activity determination. The antimicrobial, antioxidant and enzyme inhibitory activities can be performed on TLC bioautography. This method is mainly used for preliminary screening natural products possessing these biological activities and for the bioactivity-directed fractionation and isolation of active components from com Read More

Three-component reaction of aldehyde, 1H-indazol-6-amine and 1,3-dicarbonyl compounds in EtOH under catalyst-free conditions, generates the corresponding pyrazolo[3,4-a]acridine, cyclopenta[b]pyrazolo[3,4-f]quinoline, indeno[1,2-b]pyrazolo[3,4-f]quinoline and benzo[h]pyrazolo[3,4-a]acridine derivatives in high yields and regioselectivity, respectively. The dicarbonyl compounds include 5,5-dimethylcyclohexane-1,3-di Read More

A library of supramolecular structures formed by self-organization of N-lipidated tripeptides, dipeptides and Nacylated amino acids attached to cellulose according to the TASP concept via aminophenylamino-1,3,5-triazine was synthesized and the catalytic activity of the structures was studied. Intensive catalytic activity in solvolysis of sterically hindered Z-Aib-Aib-ONp under ambient conditions was observed for structur Read More

Four fluorescent tricyclic basic dyes with two hollow organic capsules namely cucurbit[n]urils (CB[n]), n = 7 and 8, compose the chemical tongue that is examined for α-amino acids recognition. This array is able to identify and discriminate 18 α-amino acids up to 10-4 M without the need of enzyme activation. The paper shows the importance of the classification technique employed in order to reach the highest recognition r Read More