Jarrahpour, Aliasghar published the artcileDiastereoselective synthesis of potent antimalarial cis-β-lactam agents, SDS of cas: 86-51-1, the main research area is lactam preparation diastereoselective antimalarial anticancer activity; 2-Azetidinones; Antimalarial activity; N-(2-aminoethyl) β-lactams; P. falciparum; Staudinger; tert-butyl carbamate.
Fifteen novel β-lactams bearing N-Et tert-Bu carbamate group I (R1 = 4-chlorophenyl, 2-phenylethenyl, 3-methoxyphenyl, etc.; R2 = C6H5O, CH3O) and fifteen N-(2-aminoethyl) βlactams II were synthesized by [2 + 2] ketene-imine cycloaddition reaction (Staudinger). The cycloaddition reaction was found to be totally diastereoselective leading exclusively to the formation of cis-β-lactam derivatives These newly synthesized β-lactams I, II were evaluated for their antimalarial activity against p. falciparum K14 resistant strain and showed good to excellent EC50 values. Among the thirty β-lactams tested, I (R1 = naphthalen-2-yl, R2 = C6H5O), II (R1 = 4-chlorophenyl, R2 = C6H5O; R1 = 2-phenylethenyl, R2 = C6H5O) showed IC50 < 20 μM while I (R1 = 4-nitrophenyl, R2 = C6H5O; R1 = 2-(4-nitrophenyl)ethenyl, R2 = C6H5O; R1 = 3-methoxyphenyl, R2 = C6H5O; R1 = Ph, R2 = C6H5O; R1 = 3-bromophenyl, R2 = C6H5O; R1 = 2,3-dimethoxyphenyl, R2 = C6H5O; R1 = 3-nitrophenyl, R2 = C6H5O), II (R1 = 4-methylphenyl, R2 = C6H5O; R1 = 3-bromophenyl, R2 = C6H5O; R1 = naphthalen-2-yl, R2 = C6H5O) exhibited IC50 <50. Compounds I (R1 = 2-phenylethenyl, R2 = C6H5O; R1 = naphthalen-2-yl, R2 = C6H5O) were examined for their anticancer properties against K562 Leukemia cell line. Compounds R1CH=NCH2CH2NHC(O)OC(CH3)3, I, II, were tested against S. aureus, E. coli, C. albicans and showed no activity below 125 μg/mL. Iranian Journal of Pharmaceutical Research published new progress about Antimalarials. 86-51-1 belongs to class isoquinoline, name is 2,3-Dimethoxybenzaldehyde, and the molecular formula is C9H10O3, SDS of cas: 86-51-1.
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem