Download (8Mb) - Etheses - Saurashtra University
Download (8Mb) - Etheses - Saurashtra University
Download (8Mb) - Etheses - Saurashtra University
Create successful ePaper yourself
Turn your PDF publications into a flip-book with our unique Google optimized e-Paper software.
No.<br />
H 2N<br />
Compound<br />
Code<br />
N<br />
N<br />
C8H17 R1<br />
R 1<br />
Yield %<br />
1 BS-199 4-OCH3 56<br />
2 BS-200 4-F 71<br />
3 BS-201 3,4-di Cl 64<br />
4 BS-202 3-Br 68<br />
5 BS-203 Naphthalen-1-yl 59<br />
6 BS-204 4-NO2 66<br />
7 BS-205 4-(4-NO2-Ph) 52<br />
8 BS-206 4-SO2Me 61<br />
9 BS-207 4-SMe 40<br />
10 BS-208 4-(4-biphenyl)_ 31<br />
Yields are isolated yields over 2 steps.<br />
Table -2: 2-aminoimidazole with octyl substitution at N-1 position<br />
3.5 Biofilm Activity<br />
The preliminary results from our lab the basic compound (A) with a non-substituted<br />
phenyl group at the C(5) position of the imidazole ring shows a moderate biofilm<br />
inhibitory activity (IC50 = 130 µM). Interestingly, substitution of the para- position of<br />
the phenyl ring with a chlorine (B) atom enhances the biofilm inhibitory activity<br />
about ten times (IC50 = 16 µM).<br />
H 2N<br />
N<br />
N<br />
H<br />
N<br />
H2N N<br />
H<br />
A B<br />
In an attempt to improve their biofilm inhibitory activity, we substituted the N1position<br />
of some of the para-substituted 4(5)-phenyl-2-aminoimidazoles with n-alkyl<br />
and cyclo-alkyl groups by using our previously established chemistry.<br />
Cl