Literature DB >> 15357972

Synthesis and DP-IV inhibition of cyano-pyrazoline derivatives as potent anti-diabetic agents.

Jin Hee Ahn1, Hye-Min Kim, Sun Ho Jung, Seung Kyu Kang, Kwang Rok Kim, Sang Dal Rhee, Sung-Don Yang, Hyae Gyeong Cheon, Sung Soo Kim.   

Abstract

A new series of cyano-pyrazoline derivatives with secondary amine at P-2 site was synthesized through achiral and chiral synthetic methods and evaluated for their ability to inhibit dipeptidyl peptidase IV (DP-IV). Compound 5i revealed good in vivo efficacy (ED50: 4.1 mg/kg; in vivo DP-IV inhibition). Also chiral derivative (11b) having (S)-configuration of compound 5i was found to be more potent.

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Year:  2004        PMID： 15357972     DOI： 10.1016/j.bmcl.2004.06.046

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Regioselective synthesis and biological studies of novel 1-aryl-3, 5-bis (het) aryl pyrazole derivatives as potential antiproliferative agents.

Authors:  Hanumappa Ananda; Kothanahally S Sharath Kumar; Mayilaadumveettil Nishana; Mahesh Hegde; Mrinal Srivastava; Raghava Byregowda; Bibha Choudhary; Sathees C Raghavan; Kanchugarakoppal S Rangappa
Journal:  Mol Cell Biochem       Date:  2016-11-24       Impact factor: 3.396

2.  3,5-Bis[1-acetyl-5-(4-chloro-phen-yl)-4,5-dihydro-1H-pyrazol-3-yl]-2,6-dimethyl-pyridine.

Authors:  Qun Qian; Jun Zhang; Min Zhang; Xiang He; Yi-Ben Xia
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2008-08-06

3.  Reaction of 7α-bromo-6-nitrocholest-5-enes with hydrazine: Formation of steroidal pyrazolines and molecular docking against SARS-CoV-2 omicron protease.

Authors:  Avadhesh Kumar; Mehtab Parveen; Mahboob Alam
Journal:  Steroids       Date:  2022-10-05       Impact factor: 2.760

4.  1-[5-(2H-1,3-Benzodioxol-5-yl)-3-(4-methyl-phen-yl)-2-pyrazolin-1-yl]ethanone.

Authors:  Wan-Sin Loh; Ibrahim Abdul Razak; M Abdul Rahiman; G N Ravikumar
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-04-13
  4 in total

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