Synthesis and antimicrobial evaluation of novel 4-amino-6-(1,3,4-oxadiazolo/1,3,4-thiadiazolo)-pyrimidine derivatives
Shetty, P; Praveen, BM; Raghavendra, M; Manjunath, K; Cheruku, S
| HERO ID | 3539050 |
|---|---|
| In Press | No |
| Year | 2016 |
| Title | Synthesis and antimicrobial evaluation of novel 4-amino-6-(1,3,4-oxadiazolo/1,3,4-thiadiazolo)-pyrimidine derivatives |
| Authors | Shetty, P; Praveen, BM; Raghavendra, M; Manjunath, K; Cheruku, S |
| Journal | Molecular Diversity |
| Volume | 20 |
| Issue | 2 |
| Page Numbers | 391-398 |
| Abstract | A series of novel 4-amino-6-(1,3,4-oxadiazolo/1,3,4-thiadiazolo)-pyrimidine derivatives of biological interest were prepared by sequential amination, hydrazide formation, and hydrazine carbothioamidination followed by cyclization. All the synthesized compounds (6a-6h and 7a-7f) were screened for antibacterial and antifungal activity. From this group, compound 7f (MIC (μg/mL μg/mL )/Inhibition (mm): 6.25/23-30) showed good antibacterial and antifungal activity. Reagents and conditions: (a) Ethyl acetoacetate, 60% NaH, 1,4-dioxane, 60°C, 6 h; (b) DIPEA, 1,4-dioxane, 100°C, 14 h; (c) NH2NH2 ⋅ H2O, EtOH, reflux, 14 h; (d) Tolyl isothiocyanatobenzene, DMF, RT, 2 h; (e) (if X = O) EDC⋅ HCl, TEA, DMF, RT, 14 h; (f) (if X = S) Conc. H2O4, RT, 14h. |
| Doi | 10.1007/s11030-015-9640-0 |
| Pmid | 26498121 |
| Wosid | WOS:000373857100003 |
| Url | http://link.springer.com/10.1007/s11030-015-9640-0 |
| Is Certified Translation | No |
| Dupe Override | No |
| Is Public | Yes |
| Language Text | English |
| Keyword | Microbiology Abstracts B: Bacteriology; Antifungal activity; Ethanol; Minimum inhibitory concentration; Antimicrobial agents; Tetraethylammonium; Hydrazine; J 02340:Antibiotics & Antimicrobials |