2<i>H</i>-Thiazolo[4,5-<i>d</i>][1,2,3]triazole: synthesis, functionalization, and application in scaffold-hopping-Reference-Cited by-同舟云学术

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2H-Thiazolo[4,5-d][1,2,3]triazole: synthesis, functionalization, and application in scaffold-hopping

Published:2024 Issue: Volume: Page:
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Miyazaki Ryuya¹^ORCID,Takada Fumito¹,Kikuchi Takunari¹,Oguro Yuya²,Kamata Makoto²,Yukawa Takafumi²,Kato Kenta¹,Muto Kei³^ORCID,Yamaguchi Junichiro¹^ORCID

Affiliation:

1. Department of Applied Chemistry, Waseda University, 513 Wasedatsurumakicho, Shinjuku, Tokyo 162-0041, Japan

2. Takeda Pharmaceutical Company Limited, 2-26-1 Muraoka-Higashi, Fujisawa, Kanagawa 251-8555, Japan

3. Institute of Transformative Bio-molecules, Nagoya University, Furo-cho, Chikusa, Nagoya 464-8601, Japan

Abstract

We have developed 2H-thiazolo[4,5-d][1,2,3]triazole (ThTz), an unprecedented [5-5]-fused heteroaromatic system for medicinal chemistry. C5-sulfonylated ThTz has been commercialized through Tokyo Chemical Industry Ltd (TCI: catalogue number M3881).

Funder

Waseda University

Japan Society for the Promotion of Science

Japan Science and Technology Agency

Publisher

Royal Society of Chemistry (RSC)

Link

http://pubs.rsc.org/en/content/articlepdf/2024/SC/D4SC03874F

Reference30 articles.

1. Heteroaromatic Rings of the Future

2. A decade of fragment-based drug design: strategic advances and lessons learned

3. The rise of fragment-based drug discovery

4. Novel thienopyrrole glycogen phosphorylase inhibitors: Synthesis, in vitro SAR and crystallographic studies

5. Sensitivity of glycogen phosphorylase isoforms to indole site inhibitors is markedly dependent on the activation state of the enzyme

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