Evidence map›Paper›PMID 35702778›Full record

ArticleCurrent medicinal chemistry2024

Synthesis of β-Amino Carbonyl 6-(Aminomethyl)- and 6-(Hydroxymethyl)pyrazolopyrimidines for DPP-4 Inhibition Study.

Cheng-Yen Chung, Ching-Chun Tseng, Sin-Min Li, Wei-Zheng Zeng, Yu-Ching Lin, Yu-Pei Hu, Wen-Ping Jiang, Guan-Jhong Huang, Henry J Tsai, Fung Fuh Wong

Abstract read
PubMed Publisher
In one paragraph

Article in Current medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
–field-weighted citation impact, top 89% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

0 citing papers in PubMed, 0 citations in OpenAlex.

No citing paper in PubMed yet.

4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

10 authors at 3 institutions in 1 country.

Cheng-Yen ChungDepartment of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, No. 91, Hsueh-Shih Rd., Taichung, 40402, Taiwan.
Ching-Chun TsengPhd Program for Biotech Pharmaceutical Industry, China Medical University, No. 91, Hsueh-Shih Rd., Taichung, 40402, Taiwan.
Sin-Min LiInstitute of New Drug Development, China Medical University, No. 91 Hsueh-Shih Rd., Taichung 40402, Taiwan.
Wei-Zheng ZengMaster Program for Pharmaceutical Manufacture, China Medical University, No. 91, Hsueh-Shih Rd., Taichung, 40402, Taiwan.
Yu-Ching LinDepartment of Biological Science and Technology, China Medical University, Taichung Taiwan.
Yu-Pei HuDepartment of Biological Science and Technology, China Medical University, Taichung Taiwan.
Wen-Ping JiangDepartment of Pharmacy, Chia Nan University of Pharmacy and Science, Tainan, Taiwan.
Guan-Jhong HuangDepartment of Chinese Pharmaceutical Sciences and Chinese Medicine Resources, China Medical University, No. 91, Hsueh-Shih Rd., Taichung, 40402, Taiwan.
Henry J TsaiDepartment of Health and Nutrition Biotechnology, Asia University, Taichung 413, Taiwan.
Fung Fuh WongPhd Program for Biotech Pharmaceutical Industry, China Medical University, No. 91, Hsueh-Shih Rd., Taichung, 40402, Taiwan.
China Medical University · TWAsia University · TWChia Nan University of Pharmacy and Science · TW

Funding

China Medical University CMU110-MF-99Ministry of Science and Technology of Taiwan MOST 110-2113-M-039-008, MOST-110-2731-M
6 · The paper itself

Abstract

backgroundType-2 diabetes is a chronic progressive metabolic disease resulting in severe vascular complications and mortality risk. Recently, DPP-4 inhibitors had been conceived as a favorable class of agents for the treatment of type 2 diabetes due to the minimal side effects.

methodsSitagliptin is the first medicine approved for the DPP-4 inhibitor. Its structure involved three fragments: 2,4,5-triflorophenyl fragment pharmacophore, enantiomerically β-amino carbonyl linker, and tetrahydrotriazolopyridine. Herein, we are drawn to the possibility of substituting tetrahydrotriazolopyridine motif present in Sitagliptin with a series of new fused pyrazolopyrimidine bicyclic fragment to investigate potency and safety.

resultsTwo series of fused 6-(aminomethyl)pyrazolopyrimidine and 6-(hydroxymethyl) pyrazolopyrimidine derivatives containing β-amino ester or amide as linkers were successfully designed for the new DPP-4 inhibitors. Most fused 6-methylpyrazolopyrimidines were evaluated against DPP-4 inhibition and selectivity capacity. Based on research study, β-amino carbonyl fused 6-(hydroxymethyl)pyrazolopyrimidine possesses the significant DPP-4 inhibition (IC

conclusionβ-Amino esters and amides fused 6-(hydroxymethyl)pyrazolopyrimidine were developed as the new DPP-4 inhibitors. Those compounds with a methyl group or hydrogen in

Indexed as

Dipeptidyl Peptidase 4Dipeptidyl-Peptidase IV InhibitorsPyrimidinesDiabetes Mellitus, Type 2HumansMolecular Docking SimulationMolecular StructurePyrazolesStructure-Activity RelationshipDipeptidyl Peptidase 4Dipeptidyl-Peptidase IV InhibitorsDPP4 protein, humanPyrazolesPyrimidines6-(aminomethyl)pyrazolopyrimidine6-(hydroxymethyl)pyrazolopyrimidineDPP- 4 inhibitorspyrazolopyrimidinesitagliptin.β-amino amideβ-amino ester

Identifiers

PMID35702778
OpenAlexW4282968680

What Socratic holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the Socratic graph.