A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonis...A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin H, induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9a, 9g and 9j exhibited potent antagonistic activity of AT1 receptor.展开更多
A series of natural product 23-hydroxybetulinic acid derivatives were prepared. In the preparation of mono-O-benzoyl ester derivative, it was observed that benzoyl group migrated from 3-0- to 23-O-position during the ...A series of natural product 23-hydroxybetulinic acid derivatives were prepared. In the preparation of mono-O-benzoyl ester derivative, it was observed that benzoyl group migrated from 3-0- to 23-O-position during the detritylation.展开更多
Dihydrotetrabenazine(DTBZ) is the major pharmacologically active form of tetrabenazine(TBZ),which was approved by FDA for the treatment of chorea associated with Huntington’s disease(HD).An unexpected Hoffmann elimin...Dihydrotetrabenazine(DTBZ) is the major pharmacologically active form of tetrabenazine(TBZ),which was approved by FDA for the treatment of chorea associated with Huntington’s disease(HD).An unexpected Hoffmann elimination was observed during the treatment of DTBZ with sodium hydrogen and alkyl halides,leading to the formation of both eliminated products(major) and hydroxyl-alkylated products(minor).展开更多
基金We are thankful to the National Natural Science Foundation of China(No.30371688)Key Fund of Ministry of Education of China(No.03089)for financial support.
文摘A series of 2-alkylbenzimidazole derivatives 9a-n have been designed and synthesized as a novel class of non-peptide angiotensin H AT1 receptor antagonists. The synthesized compounds were evaluated for their antagonism of angiotensin H, induced contraction in the rabbit thoracic aortic ring and the results showed that compounds 9a, 9g and 9j exhibited potent antagonistic activity of AT1 receptor.
基金supported by the National Natural Science Foundation of the People's Republic of China(No.30472083).
文摘A series of natural product 23-hydroxybetulinic acid derivatives were prepared. In the preparation of mono-O-benzoyl ester derivative, it was observed that benzoyl group migrated from 3-0- to 23-O-position during the detritylation.
基金supported by the "111 Project" from the Ministry of Education of China and the State Administration of Foreign Expert Affairs of China(No.111-2-07)
文摘Dihydrotetrabenazine(DTBZ) is the major pharmacologically active form of tetrabenazine(TBZ),which was approved by FDA for the treatment of chorea associated with Huntington’s disease(HD).An unexpected Hoffmann elimination was observed during the treatment of DTBZ with sodium hydrogen and alkyl halides,leading to the formation of both eliminated products(major) and hydroxyl-alkylated products(minor).
