Evidence map›Paper›PMID 39770408›Full record

ReviewPharmaceuticals (Basel, Switzerland)2024

Synthesis of Diazacyclic and Triazacyclic Small-Molecule Libraries Using Vicinal Chiral Diamines Generated from Modified Short Peptides and Their Application for Drug Discovery.

Mukund P Tantak, Ramanjaneyulu Rayala, Prakash Chaudhari, Chhanda C Danta, Adel Nefzi

Abstract readReview
In one paragraph

Review in Pharmaceuticals (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
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

2 citing papers in PubMed.

  1. Article
  2. Article
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

5 authors.

Mukund P TantakHerbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.ORCID 0000-0001-9230-7533
Ramanjaneyulu RayalaHerbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.ORCID 0000-0002-0198-6903
Prakash ChaudhariHerbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.
Chhanda C DantaHerbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.ORCID 0000-0002-1436-9461
Adel NefziHerbert Wertheim College of Medicine, Center for Translational Science, Florida International University, Port Saint Lucie, FL 34987, USA.ORCID 0000-0003-0155-5887

Funding

Synthesis and in vitro and in vivo screening of fused and tethered heterocyclic peptidomimetics for the discovery of new analgesics with decreased side effectsR33DA044425 · NIDA · TORREY PINES INST FOR MOLECULAR STUDIES · PI MCLAUGHLIN, JAY P., NEFZI, ADEL · 2020 to 2022
$922k
Novel gyrase inhibitors targeting Mycobacterium tuberculosisR21AI178134 · NIAID · FLORIDA INTERNATIONAL UNIVERSITY · PI LENG, FENFEI, NEFZI, ADEL · 2023 to 2024
$422k
NIDA NIH HHS R33 DA044425NIH HHS R21AI178134NIH HHS R33DA044425
6 · The paper itself

Abstract

Small-molecule probes are powerful tools for studying biological systems and can serve as lead compounds for developing new therapeutics. Especially, nitrogen heterocycles are of considerable importance in the pharmaceutical field. These compounds are found in numerous bioactive structures. Their synthesis often requires several steps or the use of functionalized starting materials. This review describes the use of vicinal diamines generated from modified short peptides to access substituted diaza- and triazacyclic compounds. Small-molecule diaza- and triazacyclic compounds with different substitution patterns and embedded in various molecular frameworks constitute important structure classes in the search for bioactivity. The compounds are designed to follow known drug likeness rules, including "Lipinski's Rule of Five". The screening of diazacyclic and traizacyclic libraries has shown the utility of these classes of compounds for the de novo identification of highly active compounds, including antimalarials, antimicrobial compounds, antifibrotic compounds, potent analgesics, and antitumor agents. Examples of the synthesis of diazacyclic and triazacyclic small-molecule libraries from vicinal chiral polyamines generated from modified short peptides and their application for the identification of highly active compounds are described.

Indexed as

combinatorial chemistrydiazacyclic compoundsdiversity-oriented synthesisdrug discoveryheterocyclic compoundsnatural product-like compound librariesnitrogen-containing scaffoldpeptidomimeticspolyaminessmall-molecule librariessolid-phase organic synthesistriazacyclic compoundsvicinal amines

Identifiers

PMID39770408
PMCPMC11678756

What Socratic holds

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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.