Small molecule diversity can be achieved in a single synthetic operation from bifunctional substrates in the absence of additives and under the influence of microwaves with complete control of pathway selectivity. The preliminary Ugi four-component coupling products give rise to three structurally distinct scaffolds that are dependent on solvent effects and sterics. 2,5-Diketopiperazines (Type ...

The second-generation synthesis of 3'-hydroxypacidamycin D (2) has been accomplished via an Ugi-four component reaction at a late stage of the synthesis. This approach provided ready access to a range of analogues including diastereomers of the diaminobutylic acid residue and hybrid-type analogues of mureidomycins. Biological evaluations of these analogues indicated that the stereochemistry at ...

On the basis of our recently resolved first cocrystal structure of Mdm4 in complex with a small molecule inhibitor (PDB ID 3LBJ ), we devised an approach for the generation of potential Mdm4 selective ligands. We performed the Ugi four-component reaction (Ugi-4CR) in 96-well plates with an indole fragment, which is specially designed to mimic Trp23, a key amino acid for the interaction between ...

Isocyanide-based multicomponent reactions (IMCRs) allow the construction of relatively complex molecules through a one-pot synthesis. The combination of IMCRs in a consecutive or sequential fashion further extends the complexity of the molecules obtained. Herein, we report the efficient application of this approach to the synthesis of acylhydrazines bearing 1,5-disubstituted tetrazoles. Our str...

Article history: Received on: 03/02/2013 Revised on: 20/02/2013 Accepted on: 05/03/2013 Available online: 30/03/2013 An efficient and rapid synthesis of novel anti-inflammatory and antimicrobial agents using 4-aminoantipyrine, nicotinic acid, ethylisocyanoacetate and substituted aldehydes via Ugi four component reaction (Ugi-4CR) protocol under microwave irradiation in presence of Fluorite as a...

The perception of linkages between ecosystem services (ES) and the urban green infrastructure (UGI) is evaluated, their impact on human well-being (WB) defined. Using a theoretical approach, UGI’s specific contribution to WB calculated as sum products (a) number perceived ES per group weight factor divided by product (b) respondents (c) factor. Stakeholders demand more than supply from all type...

An Ugi multicomponent reaction based two-step strategy was applied to generate medium-sized rings. In the first linear expansion phase, a series of diamines reacted with cyclic anhydrides to produce different lengths of terminal synthetic amino acids as the starting material for the second phase. The Ugi-4-center 3-component reaction was utilized to construct complex medium-sized rings (8-11) b...

BACKGROUND AND STUDY AIMS Upper gastrointestinal (UGI) cancer in the Western world usually presents at an advanced stage, when opportunities for curative therapy are limited. The failure to detect subtle, early-stage UGI cancer at endoscopy may contribute to a poor prognosis. We undertook a meta-analysis of studies of endoscopic miss rates for UGI cancer to quantify how often opportunities to d...

Libraries of diketopiperazines have been generated in high purity using the small molecule macroarray synthesis platform.