A Remarkably High-Speed Solution-Phase Combinatorial Synthesis of 2-Substituted-Amino-4-Aryl Thiazoles in Polar Solvents in the Absence of a Catalyst under Ambient Conditions and Study of Their Antimicrobial Activities.
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.
Department of Pharmaceutical Chemistry, Sinhgad College of Pharmacy, Vadgaon (Bk), Pune, Maharashtra 411041, India.
Satish N
SN
Dighe
Pratip K
PK
Chaskar
Kishor S
KS
Jain
Manisha S
MS
Phoujdar
Kumar V
KV
Srinivasan