111628-35-4Relevant articles and documents
Non-imidazole histamine H3 ligands, part 2: New 2-substituted benzothiazoles as histamine H3 antagonists
Walczynski, Krzysztof,Guryn, Roman,Zuiderveld, Obbe P.,Timmerman, Henk
, p. 389 - 398 (1999)
New, non-imidazole histamine H3 receptor antagonists were prepared and in vitro tested as H3 receptor antagonists measured as the electrically evoked contraction of the guinea-pig jejunum. The 2-(1-piperidinyl)- and 2- (1-pyrrolidinyl)benzothiazoles show no or very poor activity; 2-[1-(4- amino)piperidinyl]- and 2-(1,2-ethanediamino)- and (2-(1,3- propanediamino)derivatives of benzothiazole possess weak activity at H3 receptors, whereas 2-(4-piperidinyl)benzothiazoles and 2-[1-(4- piperazinyl)]benzothiazoles show moderate to good activity. Lipophilic and not-too-bulky substituents like n-propyl attached to the nitrogen at the piperazine or piperidine ring lead to potent H3 receptor antagonists with pA2 values ranging from 7.0 to 7.2. The structure-activity relationships for different substitution patterns are discussed.
Arylation of amines and monoarylation of symmetrical diamines in the presence of brine solution with diheteroaryl halides
Verma, Sanjeev K.,Ghorpade, Ramarao,Kaushik
supporting information, p. 2645 - 2655 (2014/08/18)
A simple, scalable, ligand-free, and metal-free protocol for arylation of amines and monoarylation of symmetrical diamines with diheteroaryl halides in the presence of brine solution has been developed. The protocol has broad structural applicability for chemoselective monoarylation of a wide variety of symmetrical, cyclic, and acyclic aliphatic diamines. The protocol is also applicable for selective arylation of aliphatic amine in the presence of aromatic amine.
