100450-84-8Relevant academic research and scientific papers
Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: A comparative study
Liu, Nora,Hoogendoorn, Sascha,Van De Kar, Bas,Kaptein, Allard,Barf, Tjeerd,Driessen, Christoph,Filippov, Dmitri V.,Van Der Marel, Gijsbert A.,Van Der Stelt, Mario,Overkleeft, Herman S.
, p. 5147 - 5157 (2015)
Ibrutinib is a covalent and irreversible inhibitor of Bruton's tyrosine kinase (BTK) and has been approved for the treatment of haematological malignancies, such as chronic lymphocytic leukaemia, mantle cell lymphoma and Waldenstr?m's macroglobulinemia. The covalent and irreversible nature of its molecular mode of action allows identification and monitoring of its target in an activity-based protein profiling (ABPP) setting. Fluorescent and biotinylated ibrutinib derivatives have appeared in the literature in recent years to monitor BTK in vitro and in situ. The work described here complements this existing methodology and pertains a comparative study on the efficacy of direct and two-step bioorthogonal ABPP of BTK.
Synthesis and antimicrobial screening of 4-thiazolidinone and 2-azetidinone derivatives of piperazine
Shingade, Sunil G.,Bari, Sanjaykumar B.
, p. 699 - 706 (2013/04/10)
The Schiff's bases 3a-3h were synthesized by reacting substituted/ unsubstituted aromatic aldehydes 2a-2h with 1-(2-aminoethyl)-piperazine 1. A series of novel aryl-3-(2-piperazin-1-ylethyl)-1,3-thiazolidin-4-one 4a-4h and 3-chloro-1-{2-[4-(chloroacetyl)piperazin-1-yl]ethyl}-4-arylazetidin-2-one 5a-5h were synthesized from the Schiff's bases of 1-(2-aminoethyl)-piperazine 3a-3h. The structures of synthesized compounds were confirmed by analytical (C, H, and N) and spectral (FT-IR, 1H NMR, 13C NMR, and Mass) data. The compounds 4a-4h and 5a-5h were screened for antimicrobial activity. The compounds 4a, 4d, 4f, 4g, 5a, 5d, 5f, and 5g exhibited substantially significant antibacterial as well as antifungal activity.
The design and synthesis of 1,4-substituted piperazine derivatives as triple reuptake inhibitors
Han, Minsoo,Han, Younghue,Song, Chiman,Hahn, Hoh-Gyu
, p. 2597 - 2602 (2012/10/29)
Novel 1,4-substituted piperazine derivatives 5, Series A and B were designed by fragment analysis and molecular modification of 4 selected piperazine-containing compounds which possess antidepressant activity. We synthesized new 39 analogues of Series A and 10 compounds of Series B, respectively. The antidepressant screening against DA, NE, and serotonin neurotransmitter uptake inhibition was carried out using the Neurotransmitter Transporter Uptake Assay Kit. The compounds in Series B showed relatively higher reuptake inhibitory activity for SERT, NET, and DAT than those in Series A. The length of spacer between the central piperazine core and the terminal phenyl ring substituted at the piperazine ring in Series B seems to exert an important role in the activity.
N,N-SUBSTITUTED CYCLIC AMINE DERIVATIVES
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, (2008/06/13)
N,N-substituted cyclic amine derivatives represented by general formula (VIII) or pharmacologically acceptable salts thereof: wherein A represents aryl, etc.; E represents -CO- or -CHOH-; G represents oxygen, etc.; J represents optionally substituted aryl; R1 represents lower alkyl, etc.; Alk represents linear or branched lower alkylene; n, v, w, x and y independently represent each 0 or 1; and p represents 2 or 3. These compounds or salts thereof are efficacious in treating diseases against which calcium antagonism is efficacious. These diseases include cerebrovascular disorder at the acute stage, cerebral stroke, cerebral infarction, head injury, cerebral nerve cell death, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, brain circulatory disturbance, brain function disturbance, pain, convulsion, schizophrenia, hemicrania, epilepsy, circular psychosis, nerve degeneration diseases, brain ischemia, AIDS, complex dementia, edema, anxiety and diabetic nephropathy.
