Microwave-assisted diastereoselective two-step three-component synthesis for rapid access to drug-like libraries of substituted 3-amino-β-lactams
作者:Guido V. Janssen、Joyce A.C. van den Heuvel、Rik P. Megens、Jorg C.J. Benningshof、Huib Ovaa
DOI:10.1016/j.bmc.2017.11.014
日期:2018.1
a robust microwave-assisted synthesis for the diastereoselective generation of 3-saccharinyl-trans-β-lactams is reported. The method is optimised for combinatorial library synthesis in which decoration of the scaffold is varied on both the β-lactam and the saccharine moiety. Within the European Lead Factory (ELF) consortium, a library of 263 compounds was efficiently produced using the developed methodology
Anti-Inflammatory, Antiproteolytic and Analgesic Activities of Some New Thiadiazolyl Indoles
作者:Manju Tandon、Jayanti P. Barthwal、Triloki N. Bhalla、Pushpa Tandon、Krishna P. Bhargava
DOI:10.1002/ardp.19833160604
日期:——
the 3‐[(2‐aminomethyl)‐5‐(2‐hydroxy‐3‐arylaminopropyl‐mercapto)1,3,4‐thiadiazolyl]indoles 3a‐‐3l. All compounds 3a‐‐3l were studied for their anti‐inflammatory activity against carrageenin induced rat paw oedema. Their antiproteolyticproperties were also evaluated. An attempt has been made to establish structure‐activity relationships.
First synthesis of 2-aminopyrrole and simple 1-substituted-2-aminopyrroles. Observation of fast proton exchange at C-5.
作者:Michael De Rosa、Roy P. Issac、Gregory Houghton
DOI:10.1016/0040-4039(95)02019-l
日期:1995.12
N-(1-substituent-111-pyrrol-2-yl)phlhalimides can be used to prepare the previously unknown 2-aminopyrrole and 1-substituted 2-aminopyrroles which undergo fast proton exchange at C-5 in acetic acid at 25 °C.