Boggu, Pulla Reddy published the artcileDiscovery of benzimidazole analogs as a novel interleukin-5 inhibitors, COA of Formula: C4H11NO, the publication is European Journal of Medicinal Chemistry (2019), 111574pp., database is CAplus and MEDLINE.
A series of novel ((hydroxyalkyl)aminomethyl)benzimidazole analogs I [n = 1, 2, 3, 4; R = H, tert-Bu, Ph, etc.; R1 = H, cyclohexyl, 4-pyridinylmethyl, etc.] and II [R2 = Ph, 4-methoxyphenyl, benzyl, 4-methoxybenzyl] were synthesized and evaluated for their IL-5 inhibitory activity using pro-B Y16 cell line. Among them, compound I [n = 1, R = Et, R1 = H] (94.3% inhibition at 30 μM, IC50 = 3.5 μM, cLogP = 4.132) and compound I [n = 1, R = cyclohexylemthyl, R1 = H] (94.7% inhibition at 30 μM, IC50 = 5.0 μM, cLogP = 6.253) showed the most potent inhibitory activity. The essential feature of SAR indicated that the chromenone ring can be replaced by a benzimidazole ring to maintain the inhibitory activity. In addition, the hydroxyethylaminomethyl group was suitable for the IL-5 inhibitory activity. Moreover, the hydrophobic substituents on carbon played an important role in the IL-5 inhibitory activity of these analogs. However, N-substituted analogs did not improve inhibitory activity. In addition, MTT assay of compounds I [n = 1; R = Et, cyclohexylmethyl; R1 = H] with normal B lymphoblasts revealed that they had no significant effects on cell viability.
European Journal of Medicinal Chemistry published new progress about 96-20-8. 96-20-8 belongs to alcohols-buliding-blocks, auxiliary class Amine,Aliphatic hydrocarbon chain,Alcohol, name is 2-Aminobutan-1-ol, and the molecular formula is C4H11NO, COA of Formula: C4H11NO.
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