Synthesis and evaluation of cyclic diamino benzamide based D3 receptor ligands

Synthesis, Molecular Properties Estimations, and Dual Dopamine D2 and D3 Receptor Activities of Benzothiazole-Based Ligands

Neurleptic drugs, e.g., aripiprazole, targeting the dopamine D2S and D3 receptors (D2SR and D3R) in the central nervous system are widely used in the treatment of several psychotic and neurodegenerative diseases. Therefore, a new series of benzothiazole-based ligands (3-20) was synthesized by applying the bioisosteric approach derived from the selective D3Rs ligand BP-897 (1) and its structural...

Synthesis and in vitro pharmacological evaluation of indolyl carboxylic amide analogues as D3 dopamine receptor selective ligands.

A series of substituted 1H-indolyl carboxylic acid amides that contain a N-(2-methoxyphenyl)piperazine or N-(2-fluoroethoxy)piperazine group were synthesized and their affinities for human dopamine D2, D3, and D4 receptors were determined. Two of these compounds, 14a and 14b, displayed high binding affinity at D3 (Ki = 0.18 and 0.4 nM, respectively), and selectivity for D3vs. D2 receptors (87-f...

Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands.

A series of new benzolactam derivatives was synthesized and the derivatives were evaluated for their affinities at the dopamine D(1), D(2), and D(3) receptors. Some of these compounds showed high D(2) and/or D(3) affinity and selectivity over the D(1) receptor. The SAR study of these compounds revealed structural characteristics that decisively influenced their D(2) and D(3) affinities. Structu...

synthesis of sulfides from alcohols and thiols in solvent-freeconditions and deoxygenation of sulfoxides

کاتالیست یک سنتز جدید برای تیواترها توصیف شده است. واکنش الکل ها با آریل، هتروآریل و آلکیل تیو ل ها درحضور 1،3،5- تری آزو- 2،4،6- تری فسفرین-2،2،4،4،6،6 هگزاکلراید ((tapc به عنوان یک کاتالیست موُثر، بازده های خوب تا عالی از تیواترها را حاصل می کند. علاوه براین، واکنش تحت شرایط بدون فلز و بدون حلال پیش می رود، بنابراین یک مکمل جالب برای روش های شناخته شده سنتز تیواترها ارائه می دهد. یک مکانیسم ا...

GPCR targeted library design: novel dopamine D3 receptor ligands.