To date, four adenosine receptor AR subtypes: A₁, A_2A, A_2B and A₃ have been cloned and pharmacologically characterized.

Searching for new selective ligands we have synthesized tricyclic purinediones with oxygen or nitrogen containing annelated ring (1)(2).

As a continuation of this research two groups of compounds with N-alkyl (cycloalkyl) pyrimido and pyrazino purinediones have been synthesized and their spatial and physicochemical properties examined by X-ray structure determination and theoretical calculation.

To compare biological activity their affinity toward A₁ and A_2A AR was evaluated.

The location of N in fused ring determinated AR affinity and selectivity. Pyrimido ring is beneficial for A_2A activity.

1. A.Drabczyńska, B.Schumacher, C.E.Müller, J.Karolak-Wojciechowska, B.Michalak, E.Pękala, K.Kieć-Kononowicz: Eur. J. Med. Chem. 2003, 38, 397.
2. A.Drabczyńska, C.E.Müller, B.Schumacher, S.Hinz, J.Karolak-Wojciechowska, B.Michalak, E.Pękala, K.Kieć-Kononowicz: Bioorg. Med. Chem. 2004, 12, 4895.

Supported in part by Polish State Committee for Scientific Research (Grant № 2 P05F 022 26).

• Legal notice:
  

  Copyright (c) Pielaszek Research, all rights reserved.
  The above materials, including auxiliary resources, are subject to Publisher's copyright and the Author(s) intellectual rights. Without limiting Author(s) rights under respective Copyright Transfer Agreement, no part of the above documents may be reproduced without the express written permission of Pielaszek Research, the Publisher. Express permission from the Author(s) is required to use the above materials for academic purposes, such as lectures or scientific presentations.
  In every case, proper references including Author(s) name(s) and URL of this webpage: https://science24.com/paper/7023 must be provided.

1. Preparation of enantiopure (R)-hydroxy metabolite of denbufylline catalysed by immobilized Lactobacillus kefiri
2. THE SEARCH FOR ENANTIOSELECTIVE REDUCTION OF PROPENTOFYLLINE BY WINE^'S YEAST BIOCATALYSIS IN WATER AND IN ORGANIC SOLVENTS
3. TRIAZINO AND TRIAZEPINO[4,3-f]PURINE- DIONES AS A₁ AND A_2A ADENOSINE RECEPTOR LIGANDS
4. WHOLE CELLS OF LACTOBACILLUS KEFIRI AS BIOCATALYST FOR THE SYNTHESIS OF ENANTIOPURE 1-(5R-HYDROXYHEXYL)- 3,7-DIMETYL-XANTHINE
5. DETERMIANTION OF LIPOPHILICITY OF THE IMIDAZO-, PYRIMIDO-, AND DIAZEPINOPURINEDIONS - ADENOSINE RECEPTORS LIGANDS
6. HISTAMINE H₃ RECEPTOR ACTIVITY OF 4-N-SUBSTITUTED PIPERAZINE-1-N-ALKYL ETHERS
7. BIOTRANSFORMATION OF PRAZIQUANTEL BY HUMAN CYTOCHROME P450 3A4 (CYP 3A4)
8. NONNATURAL D-AMINO ACIDS AS A BUILDING BLOCKS OF NEW PEPTIDOMIMETICS
9. SEARCHING FOR OPTIMAL METHOD FOR SOLUBILITY PREDICTION AMONG BIOLOGICALLY ACTIVE PHENYLPIPERAZINE DERIVATIVES OF PHENYTOIN
10. LIPOPHILICITY OF ANTITUBERCULOTIC 5-ARYLIDENE DERIVATIVES OF (THIO)HYDANTOIN EVALUATED IN SILICO AND BY MEANS OF RP-TLC
11. DESIGN AND SYNTHESIS OF HAPTEN TO GENERATE CATALYTIC ANTIBODIES THAT REDUCE PENTOXIFYLLINE
12. SYNTHESIS AND ANTICONVULSANT EVALUATION OF SOME N-ALKENYL / ALKINYL PHTHALIMIDE DERIVATIVES
13. SYNTHESIS, PHYSICOCHEMICAL AND ANTICONVULSANT PROPERTIES OF NEW N-AMINOPHENYL AZASPIRANE AND PYRROLIDINE-2,5-DIONE DERIVATIVES