Evidence map›Paper›PMID 29215263›Full record

ReviewACS combinatorial science2018

Library-to-Library Synthesis of Highly Substituted α-Aminomethyl Tetrazoles via Ugi Reaction.

Pravin Patil, Bhupendra Mishra, Gitanjali Sheombarsing, Katarzyna Kurpiewska, Justyna Kalinowska-Tłuścik, Alexander Dömling

Abstract readReview
In one paragraph

Review in ACS combinatorial science, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

6 citing papers in PubMed.

  1. Article
  2. Article
  3. Review
  4. Review
  5. Review
  6. 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

6 authors.

Pravin PatilUniversity of Groningen , Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.ORCID 0000-0002-0903-8174
Bhupendra MishraUniversity of Groningen , Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Gitanjali SheombarsingUniversity of Groningen , Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Katarzyna KurpiewskaJagiellonian University , Faculty of Chemistry, Department of Crystal Chemistry and Crystal Physics, Biocrystallography Group, Ingardena 3, 30-060 Kraków, Poland.
Justyna Kalinowska-TłuścikJagiellonian University , Faculty of Chemistry, Department of Crystal Chemistry and Crystal Physics, Biocrystallography Group, Ingardena 3, 30-060 Kraków, Poland.ORCID 0000-0001-7714-1651
Alexander DömlingUniversity of Groningen , Department of Drug Design, A. Deusinglaan 1, 9713 AV Groningen, The Netherlands.ORCID 0000-0002-9923-8873

Funding

Real-time discovery of inhibitors among billion compounds for preview and downloadR01GM097082 · NIGMS · UNIVERSITY OF PITTSBURGH AT PITTSBURGH · PI CAMACHO, CARLOS J. · 2011 to 2020
$2.5M
NIGMS NIH HHS R01 GM097082
6 · The paper itself

Abstract

α-Aminomethyl tetrazoles, recently made accessible by an Ugi multicomponent reaction (MCR), were shown to be excellent starting materials for a further Ugi MCR, yielding substituted N-methyl-2-(((1-methyl-1H-tetrazol-5-yl)methyl)amino)acetamides having four points of diversity in a library-to-library approach. The scope and limitations of the two-step sequence was explored by conducting more than 50 reactions. Irrespective of electron-rich and electron-deficient oxo-components and the nature of the isocyanide component, the reactions give excellent yields. Sterically less hindered α-aminomethyl tetrazoles give better yields of in further Ugi MCR. The target scaffold has four points of diversity and is finding applications to fill screening decks for high-throughput screening (HTS) in the European Lead Factory and in structure-based drug design.

Indexed as

AcetamidesCombinatorial Chemistry TechniquesCyanidesHigh-Throughput Screening AssaysModels, MolecularMolecular StructureSmall Molecule LibrariesStructure-Activity RelationshipTetrazolesAcetamidesCyanidesSmall Molecule LibrariesTetrazolesEuropean Lead factoryhigh-throughput screeninglibrary-to-library approachstructure-based drug designUgi reaction

Identifiers

PMID29215263
PMCPMC5813278

What OpenQuestion 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 OpenQuestion graph.