Skip to main content
. Author manuscript; available in PMC: 2018 Jul 1.
Published in final edited form as: Expert Opin Drug Discov. 2017 Jun 2;12(7):711–731. doi: 10.1080/17460441.2017.1331216

Table 4. SAR of optimized mannosides containing fused heteroaryl B-rings.

graphic file with name nihms899021u2.jpg
Cmpd R1 R2 R3 HAI EC>90 [nM] Biofilm IC50 [nM] DSF Temp [ °C]
21 H H -- 100 -- --
22 -- -- H 250 -- --
23 CH3 H -- 31 130 75.5
24 -- -- CH3 62 140 75.0
26 CH3 CH2C(O)NH(3-pyridyl) -- 1 18 --
27 CH3 C(O)NH(3-pyridyl) -- 62 -- --
graphic file with name nihms899021t1.jpg
R1 R2 X-X Binding IC50 [nM] Aggregation IC50 [μM]
28 Cl H CH=CH 14.9 8.3
29 H NO2 CH2-CH2 20 26.9
30 Cl NO2 CH2-CH2 2.4 3.4