4-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT(2A) receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 13, 1997, Pages 1635-1638

  Mokrosz, Maria J ^a   Duszyńska, Beata ^a   Kłodzińska, Aleksandra ^a   Dereń Wesołek, Anna ^a   Chojnacka Wójcik, Ewa ^a   Baranowski, Timothy C ^b   Abdou, Ibrahim M ^b   Redmore, Naomi P ^b   Strekowski, Lucjan ^b  

^a INSTITUTE OF PHARMACOLOGY   (Poland)

^b GEORGIA STATE UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PIPERAZINE DERIVATIVE; PYRIMIDINE DERIVATIVE; SEROTONIN 2A ANTAGONIST;

ARTICLE; DRUG ACTIVITY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG STRUCTURE; DRUG SYNTHESIS; NONHUMAN; RECEPTOR BLOCKING; STRUCTURE ANALYSIS;

EID: 0343554070     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)00291-6     Document Type: Article

References (15)

1. Niemegeers, C. J. E.; Awouters, F.; Heylen, S. L. E.; Gelders, Y. G. In Biological Psychiatry; Racagni G. et. al., Ed.; Elsevier Science Publishers B.V: Amsterdam, 1991; Vol. 1, pp 533-537.
2. Glennon, R. A.; Westkaemper, R. B.; Bartyzel, P. In Serotonin Receptor Subtypes: Basic and Clinical Aspects; Peroutka, S. J., Ed; Wiley-Liss: New York, 1991; pp 19-64.
3. Höltje, H.-D.; Jendretzki, U. K. Arch. Pharm. (Weinheim) 1995, 328, 577.
4. Höltje, H.-D.; Jendretzki, U. K. Pharm. Pharmacol. Lett. 1992, 1, 89.
5. Jendretzki, U. K.; Elz, S.; Höltje, H.-D. Pharm. Pharmacol. Lett. 1994, 3, 260.
6. Andersen, K.; Liljefors, T.; Gundertofte, K.; Perregaard, J.; Bøgesø, K. P. J. Med. Chem. 1994, 37, 950.
7. Mokrosz, J. L.; Strekowski, L.; Duszyńska, B.; Harden, D. B.; Mokrosz, M. J.; Bojarski, A. J. Pharmazie 1994, 49, 801.
8. Mokrosz, M. J.; Strekowski, L.; Kozak, W. X.; Duszyńska, B. Arch.. Pharm. (Weinheim) 1995, 328, 659.
9. Mokrosz, J. L.; Duszyńska, B.; Charakchieva-Minol, S.; Bojarski, A. J.; Mokrosz, M. J.; Wydra, R. L.; Strekowski, L. Eur. J. Med. Chem. 1996, 31, 973.
10. Strekowski, L.; Harden, D. B.; Grubb, W. B.; Patterson, S. E.; Czarny, A.; Mokrosz, M. J.; Cegła, M. T.; Wydra, R. L. J. Heterocycl. Chem. 1990, 27, 1393.
11. 2O, mp > 250°C (dec.); 9, mp 87-88.5°C; 9·2HCl, mp 245-247°C (dec.); 10, mp 101-102°C; 10·2HCl, mp 262-263°C (dec.); 11, an oil; 11·2HBr, mp > 200°C (dec.); 12, an oil; 12·2HBr, mp > 200·C (dec.).
12. Bojarski, A. J.; Cegła, M. T.; Charakchieva-Minol, S.; Mokrosz, M. J.; Maćkowiak, M.; Misztal, S.; Mokrosz, J. L. Pharmazie 1993, 48, 289.
13. Darmani, N. A.; Martin, B. R.; Pandey, V.; Glennon, R. A. Pharmacol. Biochem. Behav. 1990, 36, 901.
14. Schechter, M. D. Pharmacol. Biochem. Behav. 1983, 19, 751.
15. For the experimental evidence that the oxygen atom of furan can be involved in hydrogen bonding see: Timko, J. D.; Helgeson, R. C.; Newcomb, M.; Gokel, G. W.; Cram, D. J. J. Am. Chem. Soc. 1974, 96, 7097.