178672-11-2

Upstream product

• 501-53-1 benzyl chloroformate 
• 35386-24-4 1-(2-Methoxyphenyl)piperazine 
• 39945-54-5 benzyl N-(3-bromopropyl)carbamate 

Downstream Products

• 20529-23-1 3-(4-(2-methoxyphenyl)piperazin-1-yl)propylamine 

Relevant academic research and scientific papers

Discovery of naphthalimide conjugates as fluorescent probes for α1-adrenoceptors

α1-Adrenoceptors (α1-ARs), including at least three subtypes, α1A, α1B and α1D, which play essential roles in G protein-coupled receptors (GPCRs), can convey multiple pivotal extracellular signals in varied tissues and organs. In this research, a series of napthalimide-based small-molecule fluorescent probes (1a–1f) for α1-ARs, including two parts, a pharmacophore (quinazoline and phenylpiperazine) for α1-AR recognition and a fluorophore (naphthalimide) for visualization, were designed and synthesized successfully. These compounds display excellent fluorescence property and high affinity to receptors, which were used successfully for in vitro visualization of α1-adrenoceptors.

[3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy]-pyridine, pyrimidine and benzene derivatives as α1 -adrenoceptor antagonists

The present invention relates to novel α 1 -adrenoceptor antagonists of Formula I: STR1 in which: p is 0 or 1;t is 0, 1 or 2;X is O, S or NR 6 (in which R 6 is hydro or (C 1-6)alkyl);Y and Z are independently CH or N;R 1 is hydro, hydroxy, halo, nitro, amino, cyano, (C 1-4)alkylthio, acetylamino, trifluoroacetylamino, methylsulfonylamino, (C 1-6)alkyl, (C 3-6)cycloalkyl, (C 3-6)cycloalkyl (C 1-4)alkyl, oxazol-2-yl, aryl, heteroaryl, aryl (C 1-4)alkyl, heteroaryl (C 1-4)alkyl, (C 1-6)alkyloxy, (C 3-6)cycloalkyloxy, (C 3-6)cycloalkyl (C 1-4)alkyloxy, 2-propynyloxy, aryloxy, heteroaryloxy, aryl (C 1-4)alkyloxy or heteroaryl (C 1-4)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms and aryl or heteroaryl is optionally substituted with one to two substituents independently selected from halo and cyano);R 2 is hydro, hydroxy, halo, cyano, (C 1-6)alkyl or (C 1-6)alkyloxy (wherein alkyl is optionally substituted with one to three halo atoms);R 3 is -C (O)R 7 (wherein R 7 is (C 1-6)alkyl, (C 3-6)cycloalkyl, di(C 1-4)alkylamino, N-(C 1-4)alkyl-N-(C 1-4)alkyloxyamino, (C 1-4)alkyl((C 1-4)alkyloxy)amino, pyrrolidin-1-yl, piperidin-1-yl, morpholin-4-yl or piperazin-1-yl);R 4 is halo, hydroxy, cyano, (C 1-6)alkyl or (C 1-6)alkyloxy; andR 5 is (C 1-6)alkyl; and the pharmaceutically acceptable salts and N-oxides thereof.