Benzimidazole, benzoxazole and benzothiazole derivatives as 5HT 2B receptor ligands. Synthesis and preliminary pharmacological evaluation

Article abstract of DOI:10.1007/s00044-005-0125-z

2-Phenethylbenzimidazole, 2-phenethylbenzoxazole and 2- phenethylbenzothiazole derivatives were synthesized to explore the structural features of the serotonin 5-HT_2B receptor antagonists. Those molecules were designed to recognize the 5-HT_2B receptor and to discriminate it from the 5-HT_2A and 5-HT_2c subtypes. All compounds were characterized by binding affinity determination for 5-HT _2A and 5-HT_2c subtypes and antagonistic activity for 5-HT_2B receptor in rat stomach fundus. None of the new compounds showed affinity for 5-HT_2A and 5-HT_2c subtypes, but some of them displayed antagonistic activity in rat stomach fundus at micromolar concentrations. Birkhaeuser Boston 2005.

Full text of DOI:10.1007/s00044-005-0125-z

Med Chem Res 14:2 (2005) 57–73
௠ Birkha¨user Boston 2005

58

59

60

61

62

63

64

65

66

67

68

69

70

71

72

Received:
03-03-05
Accepted: 07-04-05
73