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An Overview on Synthetic and Medicinal Perspectives of [1,2,4]Triazolo[1,5-a]pyrimidine Scaffold
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2022-08-10 , DOI: 10.1002/cbdv.202200291 Srinivas Reddy Merugu 1 , Srinivasulu Cherukupalli 1 , Rajshekhar Karpoormath 1
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2022-08-10 , DOI: 10.1002/cbdv.202200291 Srinivas Reddy Merugu 1 , Srinivasulu Cherukupalli 1 , Rajshekhar Karpoormath 1
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[1,2,4]Triazolo[1,5-a]pyrimidine is an important heterocyclic scaffold known to have a wide range of pharmacological activities such as anticancer, antimicrobial, anti-tubercular, CB2 cannabinoid agonists, feticide, and adenosine antagonists. Several clinical trials and marketed drugs such as Trapidil, Essramycin, Pyroxsulam, DSM-265, Flumetsulam, GNF-6702, and Cevipabulin indicate the potential of [1,2,4]triazolo[1,5-a]pyrimidine moiety with various functional groups in medicinal chemistry. Herein, we represent a concise report focusing on the synthetic strategies used for diversely substituted [1,2,4]triazolo[1,5-a]pyrimidine analogs and their pharmacological applications. To the best of our knowledge, since 1980, we are the first to write a review on this emerging scaffold, which reveals the synthetic strategies, and pharmacological activities of differently substituted [1,2,4]triazolo[1,5-a]pyrimidine with special emphasis on structure-activity relationship studies.
中文翻译：
[1,2,4]三唑并[1,5-a]嘧啶支架的合成和药用前景概述
[1,2,4]三唑并[1,5- a ]嘧啶是一种重要的杂环支架，已知具有广泛的药理活性，如抗癌、抗菌、抗结核、CB 2大麻素激动剂、杀胎剂和腺苷拮抗剂. Trapidil、Essramycin、Pyroxsulam、DSM-265、Flumetsulam、GNF-6702 和 Cevipabulin 等多项临床试验和上市药物表明 [1,2,4]三唑并[1,5- a ]嘧啶部分具有各种功能的潜力药物化学组。在此，我们提供一份简明报告，重点介绍用于多种取代的 [1,2,4]三唑并[1,5- a]嘧啶类似物及其药理应用。据我们所知，自 1980 年以来，我们是第一个对这种新兴支架撰写评论的人，该评论揭示了不同取代的 [1,2,4] 三唑并 [1,5- a ]的合成策略和药理活性嘧啶，特别强调构效关系研究。
更新日期：2022-08-10
中文翻译：
[1,2,4]三唑并[1,5-a]嘧啶支架的合成和药用前景概述
[1,2,4]三唑并[1,5- a ]嘧啶是一种重要的杂环支架，已知具有广泛的药理活性，如抗癌、抗菌、抗结核、CB 2大麻素激动剂、杀胎剂和腺苷拮抗剂. Trapidil、Essramycin、Pyroxsulam、DSM-265、Flumetsulam、GNF-6702 和 Cevipabulin 等多项临床试验和上市药物表明 [1,2,4]三唑并[1,5- a ]嘧啶部分具有各种功能的潜力药物化学组。在此，我们提供一份简明报告，重点介绍用于多种取代的 [1,2,4]三唑并[1,5- a]嘧啶类似物及其药理应用。据我们所知，自 1980 年以来，我们是第一个对这种新兴支架撰写评论的人，该评论揭示了不同取代的 [1,2,4] 三唑并 [1,5- a ]的合成策略和药理活性嘧啶，特别强调构效关系研究。
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