The serotonin (5-hydroxytryptamine, 5-HT) transporter (SERT) is responsible for the inactivation of synaptic 5-HT and is also a target for multiple psychostimulants. Despite the critical role of SERT in 5-HT inactivation and psychostimulant response, many aspects of the transporter's recognition of ligands are poorly defined. We took advantage of sequence divergence of SERT species variants to ...

a-Chymotrypsin and trypsin were spin-labeled with 14 ortho-, meta-, and para-substituted phenylsulfonyl fluorides. These analogues of tosylfluoride were substituted with either pyrrolidinyl, pyrrolinyl, or piperidinyl nitroxide moieties. A complete description of their synthesis and the enzyme inhibition studies is presented in the following paper (WONG, S. S., QUIGGLE, K., TRIPLETT, C., AND BE...

Bacterial elongation factor Tu (EF-Tu) and EF-Ts are interacting proteins involved in polypeptide chain elongation in protein biosynthesis. A novel scintillation proximity assay for the detection of inhibitors of EF-Tu and EF-Ts, as well as the interaction between them, was developed and used in a high-throughput screen of a chemical library. Several compounds from a variety of chemical series ...

Near-infrared (NIR) organic dyes have become important for many biomedical applications, including in vivo optical imaging. Conjugation of NIR fluorescent dyes to photosensitizing molecules (photosensitizers) holds strong potential for NIR fluorescence image guided photodynamic therapy (PDT) of cancer. Therefore, we were interested in investigating the photophysical properties, in vivo tumor-af...

The N‐methyl‐D‐aspartate (NMDA) receptor as a type of ionotropic glutamatergic receptors is essential for physiological processes such as learning, memory and synaptic plasticity. A glutamate‐induced overactivation of these receptors, accompanied by increased intracellular calcium concentration, causes cell injury and leads to a large number of acute or chronic neurological disorders, such as s...

Electron-rich aza-aromatic compounds such as indoles is structures of particular interest and importancein organic chemistry. A useful procedure for the preparation of new 3-sulfenyl indole derivatives using S-alkyl or S-arylthiophthalimides as sulfenylating agents and poly(N, N′-dibromo-N-ethyl-naphthyl-2,7-disulfonamide) as novel catalyst is described. The method represents an efficient prepa...

The synthesis and reactivity of indole derivatives substituted in the benzene section was studied. Starting materials 4- and 6-iodoindole were conveniently prepared via the Batcho-Leimgruber route and purified by sublimation. Novel vicinally indolyl-substituted cyclopentanols with unexpected cis-configuration were formed by SmI2-mediated reductive dimerization of a 4-(indol-6-yl)butenone, obtai...

In an effort to develop new antibacterial drugs, some novel bisindolylmethane derivatives containing Schiff base moieties were prepared and screened for their antibacterial activity. The synthesis of the bisindolylmethane Schiff base derivatives 3-26 was carried out in three steps. First, the nitro group of 3,3'-((4-nitrophenyl)-methylene)bis(1H-indole) (1) was reduced to give the amino substit...

Ten substituted pyrrolo[2,3-d]pyrimidines were tested as cytokinins and anticytokinins in the tobacco bioassay. Eight new anticytokinins were identified and two were found to be highly active. The most potent species were 4-cyclohexylamino- and 4-cyclopentylamino-2-methylthiopyrrolo[2,3-d]pyrimidine, of which 0.05 and 0.009 muM concentrations, respectively, were required to produce detectable i...