145162-36-3Relevant academic research and scientific papers
INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS
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Page/Page column 386, (2021/01/29)
The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.
Synthesis and fluorescence properties of aminocyanopyrrole and aminocyanothiophene esthers for biomedical and bioimaging applications
Agrebi, Asma,Allouche, Fatma,Alves, Sérgio,Baleiz?o, Carlos,Cherif, Oussama,Farinha, José Paulo
, (2020/03/11)
We prepared a series of substituted aminocyanopyrroles and another of aminocynaothiophenes. We describe an efficient new one-step synthetic strategy via the condensation of an alkyl sarcosinate and ethoxymethylenemalononitrile, through a Gewald-like reaction. The UV–visible absorption and steady-state and time resolved fluorescence properties of some representative compounds, as well as their acid-base behavior, is also presented. The compounds might be useful for medicinal applications and as bioimaging probes.
Pyrrolopyrimidine derivatives and purine analogs as novel activators of Multidrug Resistance-associated Protein 1 (MRP1, ABCC1)
Schmitt, Sven Marcel,Stefan, Katja,Wiese, Michael
, p. 69 - 79 (2016/12/07)
Multidrug resistance (MDR) is the main cause of diminished success in cancer chemotherapy. ABC transport proteins are considered to be one important factor of MDR. Besides P-glycoprotein (P-gp, ABCB1) and Breast Cancer Resistance Protein (BCRP, ABCG2), Mu
Pyrrolopyrimidine Derivatives as Novel Inhibitors of Multidrug Resistance-Associated Protein 1 (MRP1, ABCC1)
Schmitt, Sven Marcel,Stefan, Katja,Wiese, Michael
, p. 3018 - 3033 (2016/05/19)
Five series of pyrrolo[3,2-d]pyrimidines were synthesized and evaluated with respect to potency and selectivity toward multidrug resistance-associated protein 1 (MRP1, ABCC1). This transport protein is a major target to overcome multidrug resistance in cancer patients. We investigated differently substituted pyrrolopyrimidines using the doxorubicin selected and MRP1 overexpressing small cell lung cancer cell line H69 AR in a calcein AM and daunorubicin cell accumulation assay. New compounds with high potency and selectivity were identified. Piperazine residues at position 4 bearing large phenylalkyl side chains proved to be beneficial for MRP1 inhibition. Its replacement by an amino group led to decreased activity. Aliphatic and aliphatic-aromatic variations at position 5 and 6 revealed compounds with IC50 values in high nanomolar range. All investigated compounds had low affinity toward P-glycoprotein (P-gp, ABCB1). Pyrrolopyrimidines with small substituents showed moderate inhibition against breast cancer resistance protein (BCRP, ABCG2).
PYRROLE AND PYRAZOLE DERIVATIVES AS POTENTIATORS OF GLUTAMATE RECEPTORS
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Page/Page column 75, (2008/06/13)
The present invention relates to pyrrole and pyrazole compounds of formula (I) and their pharmaceutically acceptable salts, and further relates to their use in treating schizophrenia, cognitive deficits associated with schizophrenia, Alzheimer's disease, dementia of the Alzheimer's type, mild cognitive impairment, or depression. The compounds act as potentiators on glutamate receptors, in particular AMPA and the GluR family.
On the Synthesis of 3-amino-pyrroles by Thorpe-Ziegler-Cyclization
Gewald, K.,Schaefer, H.,Bellmann, P.,Hain, U.
, p. 491 - 496 (2007/10/02)
N-Aryl and alkylaminomethylene cyanacetic acid derivatives 1 react with α-halogencarbonyl compounds 2 in the presence of potassium carbonate/sodium ethoxide to yield the substituted 3-amino-pyrroles 6.Using the same principle of cyclization pyrrole deriva
