Protein tyrosine phosphatase (PTP) 1B is a potential target for the treatment of diabetes and obesity. Phosphotyrosine (pTyr) is the substrate for PTP1B dephosphorylation. Malonic acid moiety was used herein as a mimic of the phosphate group in pTyr, and novel malonic acid derivatives 1-7 were designed, synthesized and evaluated as PTP1B inhibitors. Results from enzymatic assays indicated that compounds 3 and 4 exhibited potent inhibition against human recombinant PTP1B with IC50 values of 7.66 and 1.88 micromol x L(-1), respectively.

The COVID-19 pandemic has significantly disrupted medical education, particularly affecting clinical-year students. Educational institutions often had to halt, shorten or impose significant restrictions on their hospital rotations due to strict infection control and social-distancing guidelines implemented in tertiary healthcare institutions, as well as manpower and logistical constraints amid the pandemic. Thus, distance-based learning platforms such as online lectures and case-based teaching were increasingly adopted in place of bedside and face-to-face tutorials. While interactive virtual case-based discussions are generally useful in imparting clinical reasoning skills to medical students, they are unfortunately not able to fully replicate the experience of clerking, examining and managing real patients in the wards, which is a quintessential process towards building clinical acumen and attaining core clinical competencies. Therefore, for final year medical students who are preparing for their Bachelor of Medicine and Bachelor of Surgery (MBBS) examinations, many are naturally concerned by how learning in this "new normal" may affect their ability to make the transition to become competent junior doctors. As such, we seek to share our learning experiences as the first batch of medical students to have completed our entire final year of clinical education amid the COVID-19 pandemic, and offer 4 practical suggestions to future batches of students on how to adapt and optimise clinical learning under these circumstances: actively engaging in virtual learning, making the most of every clinical encounter, learning how to construct peer teaching/practice sessions, and maintaining physical and psychological well-being.
COVID-19 ; Humans ; Pandemics ; SARS-CoV-2 ; Singapore/epidemiology* ; Students, Medical