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This work describes the microwave assisted synthesis of twelve novel histamine H 3 receptor ligands. They display pyrrolo[2,3-d]pyrimidine derivatives with rigidized aliphatic amines as warheads. The compounds were screened for H 3 R and H 4 R binding affinities in radioligand displacement assays and the most potent compounds were evaluated for H 3 R binding properties in vitro and in docking studies. The combination of a rigidized H 3 R warhead and the pyrrolo[2,3-d]pyrimidine scaffold resulted in selective activity at the H 3 receptor with a pK i value of 6.90 for the most potent compound. A bipiperidine warhead displayed higher affinity than a piperazine or morpholine motif, while a naphthyl moiety in the arbitrary region increased affinity compared to a phenyl derivative. The compounds can be starting points for novel, simply synthesized histamine H 3 receptor ligands., (Copyright © 2018 Elsevier Ltd. All rights reserved.)

A new indole-4,9-dione and their phenoxy derivatives were synthesized and evaluated in vitro against the epimastigote form of Trypanosoma cruzi, Y strain. All of these novel compounds were found to be extremely potent and selective that the standard drug nifurtimox. Interestingly, phenoxyindole-4,9-dione 9d displayed excellent nanomolar inhibitory activity, IC50=20 nM, and high selectivity index, SI=625. In silico studies using MOE program were performed to generate a preliminary pharmacophore model., (Copyright © 2014 Elsevier Ltd. All rights reserved.)