Sheng, Tao published the artcileDiscovery and preliminary mechanism of 1-carbamoyl β-carbolines as new antifungal candidates, Application In Synthesis of 123-39-7, the main research area is carbamoyl carboline preparation antifungal activity docking study SAR; Action mechanism; Antifungal activities; Gaeumannomyces graminis; Histone acetylation; β-Carboline.
Various 1-substituted β-carbolines I (R1 = CH3, C6H5, 4-BrC6H4, etc.), II (R2 = C6H5, CONH2, CONHC6H5, etc.), III (R3 = Me, Ph, OH, etc.) and IV (R4 = Me, Ph, 2-pyridyl, etc.) were synthesized from com. inexpensive tryptophan and demonstrated significant in vitro antifungal activity against G. graminis. Significantly, compound II (R2 = CONH2) (EC50 = 0.45μM) with carboxamide at 1-position displayed the best efficacy and nearly 20 folds enhancement in antifungal potential compared to Silthiopham (EC50 = 8.95μM). Moreover, compounds 4,9-dihydro-3H-pyrido[3,4-b]indole-1-carboxamide, 9H-pyrido [3,4-b]indole-1-carboxamide, and II (R2 = CO2Me) exhibited excellent in vitro antifungal activities and in vivo protective and curative activities against B. cinerea and F. graminearum. Preliminary mechanism studies revealed that compound II (R2 = CONH2) caused reactive oxygen species accumulation, cell membrane destruction, and deregulation of histone acetylation. These findings indicated that 1-carbamoyl β-carbolines I, II, III and IV can be selected as a promising model for the discovery of novel and broad-spectrum fungicide candidates.
European Journal of Medicinal Chemistry published new progress about Agrochemical fungicides. 123-39-7 belongs to class amides-buliding-blocks, name is N-Methylformamide, and the molecular formula is C2H5NO, Application In Synthesis of 123-39-7.
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics