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Some salicylaldehyde-derived Baylis-Hillman adducts and 3-(chloromethyl)coumarins have been synthesised and evaluated  in vitro  for their antisickling activities. The compounds were screened for inhibitory and reversal activity against mutated haemoglobin (HbSS) in red blood cells at four different concentrations (4 mg/mL, 2 mg/mL, 1 mg/mL and 0.5 mg/mL) as a measure of their antisickling potentials. Among the synthesized compounds, 6-chloro-3-(chloromethyl)coumarin  4d  showed the highest inhibitory activity (83.75±1.90%), followed by 6-chlorocoumarin-3-methylsulfinic acid  5d  (80.90 ±0.91%) and the least was  tert -butyl-3-hydroxy- 3-(2-hydroxyphenyl)-2-methylenepropanoate  3a ( 33.33±1.86%). The results obtained from the reversal antisickling experiment showed that the percentage of sickle cells able to revert to the normal biconcave shape was dose dependent. Compound  5d  had the highest reversal activity (66.49±1.39%) followed by 6-bromo-3- (chloromethyl)coumarin  4c  (59.66±2.95) and  4d  (55.50±1.95%) at 4 mg/mL. Compound  4c  had higher reversal activity than the standard  p -hydroxybenzoic acid at 2 mg/mL, 1 mg/mL and at 0.5 mg/mL. The 3-substituted coumarins  4a-d , and  5d  had higher inhibitory antisickling activities than their Baylis-Hillman precursors  3a-d . Effect of  4a-d  and  5d  on the rate of polymerization of sickle cell heamoglobin was further studied spectrophotomerically using hemolysate of HbSS. The considerable inhibitory and reversal activities of these compounds make them good candidates for further antisickling studies.

Evaluation of Some Salicylaldehyde-derived Baylis-Hillman Adducts and Coumarin Derivatives as Potential Antisickling Compounds