No abstract

We address the challenging large-scale content-based face image retrieval problem, intended as searching images based on the presence of specific subject, given one face image of him/her. To this end, one natural demand is a supervised binary code learning method. While the learned codes might be discriminating, people often have a further expectation that whether some semantic message (e.g., visual attributes) can be read from the human-incomprehensible codes. For this purpose, we propose a novel binary code learning framework by jointly encoding identity discriminability and a number of facial attributes into unified binary code. In this way, the learned binary codes can be applied to not only fine-grained face image retrieval, but also facial attributes prediction, which is the very innovation of this work, just like killing two birds with one stone. To evaluate the effectiveness of the proposed method, extensive experiments are conducted on a new purified large-scale web celebrity database, named CFW 60K, with abundant manual identity and attributes annotation, and experimental results exhibit the superiority of our method over state-of-theart.

Concise synthesis of (±)-Lingzhiol has been achieved. The key reaction involves one-step construction of a 5/5/6/6 tetra-ring backbone of Lingzhiol via epoxy-arene cyclization.

No abstract

Inhibition of dipeptidyl peptidase IV is an important approach for the treatment of type-2 diabetes. In this study, we reported a multistage virtual screening workflow that integrated 3D pharmacophore models, structural consensus docking, and molecular mechanics/generalized Born surface area binding energy calculation to identify novel dipeptidyl peptidase IV inhibitors. After screening our in-house database, two hit compounds, HWL-405 and HWL-892, having persistent high performance in all stages of virtual screening were identified. These two hit compounds together with several analogs were synthesized and evaluated for in vitro inhibition of dipeptidyl peptidase IV. The experimental data indicated that most designed compounds exhibited significant dipeptidyl peptidase IV inhibitory activity. Among them, compounds 35f displayed the greatest potency against dipeptidyl peptidase IV in vitro with the IC50 value of 78 nm. In an oral glucose tolerance test in normal male Kunming mice, compound 35f reduced blood glucose excursion in a dose-dependent manner.

Enantioselective total synthesis of (+)-Lingzhiol has been achieved. It is the first example of in tandem semipinacol rearrangement reactions, the migrated aryl group further reacting with the carbonyl oxonium electrophile to furnish a polycyclic skeleton. Our synthesis involves 13 steps and proceeds in 6% overall yield.

No abstract

Total synthesis of (±)-cochlearol A was accomplished, which features a cis 6/6 B/D ring synthesis. A TMSOTf-promoted lactonization of tert-butoxy ketoester produced the desired lactone with quaternary carbon. The cis configuration of the B/E ring is essential for regioselective B/D ring formation. Finally, simple deprotections and transformations gave cochlearol A in 16 steps from known ethyl 4-tert-butoxyacetoacetate.