| Autor: |
Dighe SN; Department of Pharmaceutical Chemistry, Sinhgad College of Pharmacy, Vadgaon (Bk), Pune, Maharashtra 411041, India., Chaskar PK, Jain KS, Phoujdar MS, Srinivasan KV |
| Jazyk: |
angličtina |
| Zdroj: |
ISRN organic chemistry [ISRN Org Chem] 2011 Apr 11; Vol. 2011, pp. 434613. Date of Electronic Publication: 2011 Apr 11 (Print Publication: 2011). |
| DOI: |
10.5402/2011/434613 |
| Abstrakt: |
Remarkably high-speed synthesis of 2-substituted amino-4-aryl thiazoles in polar solvents with a minimum threshold polarity index of 4.8 was found to proceed to completion in just 30-40 sec. affording excellent yields of thiazoles under ambient temperature conditions without the use of any additional catalyst. The purification-free procedure afforded libraries based around a known pharmacophore, namely, substituted arylthiazoles and generated samples of high purity. In terms of combinatorial synthesis in a single solution phase, our protocol is significantly better than those hitherto reported and is amenable for HTS. The in vitro biological tests of some thiazoles showed good activity towards gram-positive bacteria, gram-negative bacteria and fungi comparable with the standard drugs, nitrofurantoin and griseofulvin, for their antibacterial and antifungal activities, respectively. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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