Synthesis and antiallergy activity of [1,3,4]thiadiazolo[3,2-a]-1,2,3-triazolo[4,5-d]pyrimidin-9 (3H)-one derivatives. I
Suzuki, N; Miwa, T; Aibara, S; Kanno, H; Takamori, H; Tsubokawa, M; Ryokawa, Y; Tsukada, W; Isoda, S
| HERO ID | 4932906 |
|---|---|
| In Press | No |
| Year | 1992 |
| Title | Synthesis and antiallergy activity of [1,3,4]thiadiazolo[3,2-a]-1,2,3-triazolo[4,5-d]pyrimidin-9 (3H)-one derivatives. I |
| Authors | Suzuki, N; Miwa, T; Aibara, S; Kanno, H; Takamori, H; Tsubokawa, M; Ryokawa, Y; Tsukada, W; Isoda, S |
| Journal | Chemical and Pharmaceutical Bulletin |
| Volume | 40 |
| Issue | 2 |
| Page Numbers | 357-363 |
| Abstract | A series of 6-substituted [1,3,4]thiadiazolo[3,2-a]-1,2,3-triazolo[4,5-d]pyrimidin-9(3H)-one derivatives 4a--z were synthesized from 5-substituted 1,3,4-thiadiazol-2-amines 5 by the following consecutive reactions: pyrimidine ring closure with bis(2,4,6-trichlorophenyl) malonate, nitration, chlorination, amination, hydrogenation and diazotization. The structure of 4 was confirmed by an alternate synthesis of 4, involving reaction of 5-substituted 2-azido-1,3,4-thiadiazole 13 with ethyl cyanoacetate, followed by the Dimroth rearrangement and ring closure. The antiallergic activities (anti-passive peritoneal anaphylaxis, anti-passive cutaneous anaphylaxis and anti-slow reacting substance of anaphylaxis activities) of the products were evaluated. |
| Pmid | 1606631 |
| Is Certified Translation | No |
| Dupe Override | No |
| Is Public | Yes |
| Language Text | English |