نتایج جستجو برای: cryptolepine isosteres
تعداد نتایج: 248 فیلتر نتایج به سال:
The proteolytic processing of polyproteins by the 3CL protease of severe acute respiratory syndrome coronavirus is essential for the viral propagation. A series of tripeptide a,b-unsaturated esters and ketomethylene isosteres, including AG7088, are synthesized and assayed to target the 3CL protease. Though AG7088 is inactive (IC50 > 100 lM), the ketomethylene isosteres and tripeptide a,b-unsatu...
Quindoline (QUIND, indolo[3,2-b]quinoline) and cryptolepine (CRYPT, 5-methyl-10H-indolo[3,2-b]quinoline) together with their corresponding derivatives have been studied for decades due to their important biological activity against diseases like malaria. The biological activity of drugs is routinely investigated using fluorescence based methods. However, recent reports show that the photophysic...
An efficient method for the construction of the tetrahydrofolate skeleton is described. Starting from pterin analogues and aromatic amines, 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives and the heterocyclic benzoyl isosteres were synthesized via a novel aziridine intermediate. Following this method, the byproducts of carbon-nitrogen bond hydrogenolysis in traditional synthetic strategy can ...
Regioselective N-alkylation of 4-chloro-2-methoxy-7H-pyrrolo[2,3d]pyrimidine (6) with ethyl 3-bromopropionate under liquid-liquid phase-transfer reaction conditions gave the ester 7a. Its saponification yielded the acid 7b. The logP values of a series of N(9)-functionalized purines and purine isosteres were calculated.
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