Design, synthesis, and conformational analysis of a novel spiro-bicyclic system as a type II .beta.-turn peptidomimetic

1992 ◽  
Vol 114 (23) ◽  
pp. 8778-8783 ◽  
Author(s):  
Michael J. Genin ◽  
Rodney L. Johnson
Keyword(s):  
Conformational Analysis ◽  
Type Ii ◽  
Design Synthesis ◽  
Beta Turn ◽  
Bicyclic System

A Bioactive Somatostatin Analog without a Type II? ?-Turn: Synthesis and Conformational Analysis in Solution

2001 ◽  
Vol 7 (10) ◽  
pp. 521-528 ◽  
Author(s):  
Shaokai Jiang ◽  
Sharon Gazal ◽  
Gary Gelerman ◽  
Ofer Ziv ◽  
Olga Karpov ◽  
...  
Keyword(s):  
Conformational Analysis ◽  
Somatostatin Analog ◽  
Type Ii

scholarly journals Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors

2013 ◽  
Vol 7 (1) ◽  
pp. 39-48 ◽  
Author(s):  
Reema Abu Khalaf ◽  
Ghassan Abu Sheikha ◽  
Mahmoud Al-Sha'er ◽  
Mutasem Taha
Keyword(s):  
Acetic Acid ◽  
Type Ii Diabetes Mellitus ◽  
Biological Evaluation ◽  
Diabetic Patients ◽  
Type Ii ◽  
Design Synthesis ◽  
Multifunctional Protein ◽  
Design And Synthesis ◽  
Dpp Iv

As incidence rate of type II diabetes mellitus continues to rise, there is a growing need to identify novel therapeutic agents with improved efficacy and reduced side effects. Dipeptidyl peptidase IV (DPP IV) is a multifunctional protein involved in many physiological processes. It deactivates the natural hypoglycemic incretin hormone effect. Inhibition of this enzyme increases endogenous incretin level, incretin activity and should restore glucose homeostasis in type II diabetic patients making it an attractive target for the development of new antidiabetic drugs. One of the interesting reported anti- DPP IV hits is Gemifloxacin which is used as a lead compound for the development of new DPP IV inhibitors. In the current work, design and synthesis of a series of N4-sulfonamido-succinamic, phthalamic, acrylic and benzoyl acetic acid derivatives was carried out. The synthesized compounds were evaluated for their in vitro anti-DPP IV activity. Some of them have shown reasonable bioactivity, where the most active one 17 was found to have an IC50 of 33.5 μM.

scholarly journals Design, Synthesis, and Conformational Analysis of Oligobenzanilides as Multifacial α-Helix Mimetics

2019 ◽  
Vol 21 (12) ◽  
pp. 4433-4438 ◽  
Author(s):  
Theo Flack ◽  
Charles Romain ◽  
Andrew J. P. White ◽  
Peter R. Haycock ◽  
Anna Barnard
Keyword(s):  
Conformational Analysis ◽  
Design Synthesis ◽  
Helix Mimetics ◽  
Α Helix

Design, Synthesis, Conformational Analysis and Application of Azabicycloalkane Amino Acids as Constrained Dipeptide Mimics

ChemInform ◽  
2004 ◽  
Vol 35 (40) ◽  
Author(s):  
Laura Belvisi ◽  
Lino Colombo ◽  
Leonardo Manzoni ◽  
Donatella Potenza ◽  
Carlo Scolastico
Keyword(s):  
Amino Acids ◽  
Conformational Analysis ◽  
Design Synthesis

Design, Synthesis, and Conformational Analysis of a Proposed Type I β-Turn Mimic

1998 ◽  
Vol 120 (18) ◽  
pp. 4334-4344 ◽  
Author(s):  
Brian E. Fink ◽  
Phil R. Kym ◽  
John A. Katzenellenbogen
Keyword(s):  
Conformational Analysis ◽  
Type I ◽  
Design Synthesis ◽  
Turn Mimic

Rational Design, Synthesis, and Evaluation of Nanomolar Type II Dehydroquinase Inhibitors

ChemMedChem ◽  
2007 ◽  
Vol 2 (7) ◽  
pp. 1015-1029 ◽  
Author(s):  
Richard J. Payne ◽  
Fabienne Peyrot ◽  
Olivier Kerbarh ◽  
Andrew D. Abell ◽  
Chris Abell
Keyword(s):  
Rational Design ◽  
Type Ii ◽  
Design Synthesis ◽  
Type Ii Dehydroquinase
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