Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.

A series of novel indene N-oxide derivatives were prepared by various synthetic methods and evaluated for their ability to activate PPARgamma. The best PPARgamma agonist in this series was 9h, which showed an EC(50) value of 15 nM.

Pyrazolidine derivatives with heteroaryl urea as dipeptidyl peptidase IV inhibitors.

In the continuation of efforts to modify the structure of our novel DP-IV inhibitors, a series of pyrazolidine derivatives with heteroaryl urea was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV).

A safer, simpler, classic intrafascial supracervical hysterectomy technique.

Objectives: Our aim is to introduce the technical aspects and advantages of a new classic intrafascial supracervical hysterectomy (CISH) technique over the conventional technique.

Methods: We performed a retrospective evaluation (Canadian Task Force classification II-2) of 200 women who underwent conventional CISH technique (100 cases), between March 2000 and September 2000, or the new CISH technique (100 cases) between May 2002 and November 2002. The charts of these 200 women were reviewed regarding patient characteristics, indications, uterine weight, estimated blood loss, operating time, and hemoglobin change.

Inhibition of dipeptidyl peptidase IV by novel inhibitors with pyrazolidine scaffold.

Inhibition of dipeptidyl peptidase IV (DPP-IV) activity has been reported to improve nutrient-stimulated insulin secretion through the stabilization of glucagon-like peptide (GLP-1). In the present study, we identified novel DPP-IV inhibitors of pyrazolidine derivatives (Compounds 1 and 2) and characterized their biological effects in vitro and in vivo. Compound 1, an isoleucine pyrazolidide with a phenyl urea group, inhibited rat plasma DPP-IV, porcine kidney DPP-IV, as well as human Caco-2 DPP-IV with IC(50) values of 1.

Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.

A new series of pyrazolidine derivatives was synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 9i was the most active in this series, exhibited IC50 value of 1.56 microM and ED50 value of 80 mg/kg (in vivo DP-IV inhibition; po).