Novel diterpenic peptide derivatives were synthesized via the Ugi four-component reaction at ambient temperature. The protocol employed a between formaldehyde, benzyl amine, corresponding diterpene acid, and ethyl 2-isocyanoacetate. anticancer properties of compounds studied in vitro.

d-Amphetamine selectively promotes release of both dopamine (DA) and norepinephrine (NE) versus serotonin (5HT), and chronic d-amphetamine treatment decreases cocaine-taking behavior in rats, nonhuman primates, and humans. However, abuse liability limits the clinical utility of amphetamine maintenance for treating cocaine abuse. One strategy to improve safety and efficacy of monoamine releasers...

Glucuronide conjugation of xenobiotics containing a tertiary amine moiety represents a unique and important metabolic pathway for these compounds in humans. Previously, human UDP-glucuronosyltransferase (UGT) 1A4 was shown to be an important enzyme for the formation of quaternary ammonium-linked glucuronides. UGT1A3 is 93% identical to UGT1A4 in primary amino acid sequence. We show that human U...

A new series of imidazo[2,1-b]thiazole analogs containing a methyl sulfonyl COX-2 pharmacophore was synthesized and evaluated for their COX-2 inhibitory activity. According to in-vitro COX-1/COX-2 inhibition data, all compounds (6a-g) were selective inhibitors of COX-2 isoenzyme with IC50 values in the highly potent 0.08-0.16 mM range. These results indicated that both potency and selectivity o...

The possibility of generating tailored surface characteristics (adhesion, biocompatibility, wettability, etc.) from plasma modified surfaces by derivatization and grafting reactions, opens up new possibilities for the creation of advanced materials. Implantation of reactive amine (primary amine) functionalities onto synthetic polymeric surfaces under cold plasma conditions one of the potential ...

wide range of quinazolinone biological properties including: antibacterial, anticancer, and anti-inflammatory activities encouraged us to synthesis some fused quinazolinone derivatives. anthranilic acid was condensed with chloro acylchloride followed by dehydration to form the benzoxazinone intermediate; subsequent addition of an amine provided the fused quinazolinones. deoxyvasicinone which wa...

The olefin moiety presents in styrylsulfonylmethyl-1,2,4-triazolylamine (1) was exploited to build up five-member heterocycle-pyrazoles. series of novel pyrazolyl-1,2,4-triazole amine derivatives (2-3) have been synthesized. All the entitles compounds were characterized by 1H and 13C NMR spectra.

riboflavin and protoporphyrin ix are two molecules that participate in oxidation and reduction reactions in the living cell. changing some functional groups of riboflavin and protoporphyrin ix can provide compounds with self-assembled monolayer properties with wide applications in designing the molecular electronic devices. in this study, the amphiphilic structure of riboflavin and protoporphyr...

The in silico identification, optimization and crystallographic characterization of a 6,7,8,9-tetrahydro-3H-pyrazolo[3,4-c]isoquinolin-1-amine scaffold as an inhibitor for the EPHA4 receptor tyrosine kinase is described. A database containing commercially available compounds was subjected to an in silico screening procedure which was focused on finding novel, EPHA4 hinge binding fragments. This...

We constructed a minilibrary using a solution-phase synthesis through coupling of three core amino compounds (5'-amino-5'-deoxy uridine, 5'-amino-2',5'-di-deoxy arabinosyl uridine, and butan-1-amine) with 30 carboxylic acids via amide bond formation. The simplified structural core compound butan-1-amine was selectively coupled with 9 carboxylic acids as control. 3-(4,5-Dimethyl-2-thiazolyl)-2,5...