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1.
Pharmaceuticals (Basel) ; 15(5)2022 May 04.
Artigo em Inglês | MEDLINE | ID: mdl-35631399

RESUMO

Continuing with our program to obtain new histamine H3 receptor (H3R) ligands, in this work we present the synthesis, H3R affinity and in silico studies of a series of eight new synthetically accessible purine derivatives. These compounds are designed from the isosteric replacement of the scaffold presented in our previous ligand, pyrrolo[2,3-d]pyrimidine ring, by a purine core. This design also considers maintaining the fragment of bipiperidine at C-4 and aromatic rings with electron-withdrawing groups at N-9, as these fragments are part of the proposed pharmacophore. The in vitro screening results show that two purine derivatives, 3d and 3h, elicit high affinities to the H3R (Ki values of 2.91 and 5.51 nM, respectively). Both compounds are more potent than the reference drug pitolisant (Ki 6.09 nM) and show low toxicity with in vitro models (IC50 > 30 µM on HEK-293, SH-SY5Y and HepG2 cell lines). Subsequently, binding modes of these ligands are obtained using a model of H3R by docking and molecular dynamics studies, thus determining the importance of the purine ring in enhancing affinity due to the hydrogen bonding of Tyr374 to the N-7 of this heterocycle. Finally, in silico ADME properties are predicted, which indicate a promising future for these molecules in terms of their physical−chemical properties, absorption, oral bioavailability and penetration in the CNS.

2.
Neotrop. entomol ; 37(6): 735-738, Nov.-Dec. 2008. mapas, tab
Artigo em Português | LILACS | ID: lil-507034

RESUMO

Este trabalho apresenta a distribuição de Trichoptera ao longo da Bacia do Rio Paranã, GO, com novos registros para gênero. Foram estabelecidas 18 estações de coleta ao longo da bacia durante as estações chuvosa (março e dezembro/2003) e seca (julho/2003 e agosto/ 2004). Foram utilizadas redes de bentos do tipo Surber e " D" , para a coleta dos organismos nos diversos ambientes.


Distribution of Trichoptera along Paranã River Basin, Goiás State, with new records for genera, is presented. Eighteen sample sites were made along the basin during the rain (March and December/2003) and dry (July/2003 and August/2004) seasons. Surber and D net were used for sampling all habitats.


Assuntos
Animais , Insetos/classificação , Brasil , Rios
3.
Neotrop Entomol ; 37(6): 735-8, 2008.
Artigo em Português | MEDLINE | ID: mdl-19169565

RESUMO

Distribution of Trichoptera along Paranã River Basin, Goiás State, with new records for genera, is presented. Eighteen sample sites were made along the basin during the rain (March and December/2003) and dry (July/2003 and August/2004) seasons. Surber and D net were used for sampling all habitats.


Assuntos
Insetos/classificação , Animais , Brasil , Rios
4.
Cad. saúde pública ; Cad. Saúde Pública (Online);22(10): 2033-2034, out. 2006.
Artigo em Inglês | LILACS | ID: lil-434018
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