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BIBTEX RIS

Synthesis and hypoglycemic activity of 7,8-dihydro-6H-thiopyrano(3,2-d)pyrimidine derivatives and related compounds.

1986; Pharmaceutical Society of Japan; Volume: 34; Issue: 10 Linguagem: Inglês

10.1248/cpb.34.4150

ISSN

1347-5223

Autores

Sachio Ohno, Kiyoshi Mizukoshi, Osamu Komatsu, Yasuo Kunoh, Yoshiki Nakamura, EIICHI KATOH, Mitsuaki Nagasaka,

Tópico(s)

Multicomponent Synthesis of Heterocycles

Resumo

A series of 2-amino-7, 8-dihydro-4-piperazinyl- and 4-amino-7, 8-dihydro-2-piperazinyl-6H-thiopyrano[3, 2-d]pyrimidines and related compounds were synthesized and evaluated for hypoglycemic activity. Several compounds exhibited excellent activity, and 7, 8-dihydro-2-(4-methyl-piperazinyl)-4-(1-pyrrolidinyl)- (8c, dimaleate : MTP-1307) and 2-amino-7, 8-dihydro-4-piperazinyl-6H-thiopyrano[3, 2-d]pyrimidine (18a, dimaleate : MTP-1403) were selected for further investigation.Oral administration of 8c and 18a at 50 mg/kg markedly improved oral glucose tolerance in ob/ob mice. In this test, buformin also showed activity, whereas tolbutamide produced no significant improvement.

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