16264-05-4Relevant articles and documents
Fe-MIL-101 modified by isatin-Schiff-base-Co: a heterogeneous catalyst for C-C, C-O, C-N, and C-P cross coupling reactions
Farrokhi, Alireza,Rouzifar, Majid,Sansano, José Miguel,Sobhani, Sara
, p. 19963 - 19976 (2021/11/12)
A metal-organic framework functionalized with a cobalt-complex is preparedviapost-synthetic modification of Fe-MIL-101-NH2. Initially, Fe-MIL-101-NH2reacted with isatin to produce Fe-MIL-101-isatin-Schiff-base, which can anchor the cobalt by the addition of cobalt acetate. The resulting MOF-Co catalyst is characterized by employing multiple techniques. This new modified MOF acts as a heterogeneous and recyclable catalyst for efficient Ullmann, Buchwald-Hartwig, Hirao, Hiyama and Mizoroki-Heck cross-coupling reactions of several aryl halides/phenylboronic acid/phenyltosylate with phenols, anilines/heterocyclic amines, triethyl phosphite, triethoxyphenylsilane and alkenes and generates the expected coupling products in good to high yields.
1,4-Diarylpiperazines and analogs as anti-tubercular agents: Synthesis and biological evaluation
Forge,Cappoen,Laurent,Stanicki,Mayence,Huang,Verschaeve,Huygen,Vanden Eynde
scheme or table, p. 95 - 101 (2012/04/10)
Despite progress in modern chemotherapy to combat tuberculosis, the causative pathogen Mycobacterium tuberculosis (M.tb.) is far from eradicated. Bacillary resistance to anti-mycobacterial agents, bacillary persistence and human immunodeficiency virus (HIV) co-infection hamper current drug treatment to completely cure the infection, generating a constant demand for novel drug candidates to tackle these problems. A small library of novel heterocyclic compounds was screened in a rapid luminometric in vitro assay against the laboratory M.tb. strain H37Rv. A group of amidines was found to have the highest potency and was further evaluated for acute toxicity against C3A hepatocytes. Next, the most promising compounds were evaluated for activity against a multi-drug resistant clinical isolate. The group of amidines was also tested for their ability to kill intracellular M.tb. residing in mouse J774A.1 macrophages. Finally, we report on a correlation between the structural differences of the compounds and their anti-mycobacterial activity.
Synthesis, antituberculosis activity, and DNA binding affinity of a highly diverse library of 1,4-diarylpiperazines
Vanden Eynde, Jean Jacques,Mayence, Annie,Lecour Jr., Louis,Huang, Tien L.
, p. 401 - 414 (2007/10/03)
A library of eighteen 1,4-diarylpiperazines has been synthesized and evaluated for antituberculosis activity and DNA binding affinity. Among them, 4,4′-(1,4-piperazinediyl)bis(N-alkylbenzenecarboximidamides) emerged as attractive leads for further drug development.