Application of 7524-52-9. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: H-Trp-OMe.HCl, is researched, Molecular C12H15ClN2O2, CAS is 7524-52-9, about Discovery and preliminary mechanism of 1-carbamoyl β-carbolines as new antifungal candidates. Author is Sheng, Tao; Kong, Mengmeng; Wang, Yujie; Wu, HuiJun; Gu, Qin; Chuang, Anita Shyying; Li, Shengkun; Gao, Xuewen.
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.
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Reference:
1,3-Benzodioxole – Wikipedia,
Dioxole | C3H4O2 – PubChem