Literature DB >> 27894044

An insight on synthetic and medicinal aspects of pyrazolo[1,5-a]pyrimidine scaffold.

Srinivasulu Cherukupalli1, Rajshekhar Karpoormath2, Balakumar Chandrasekaran1, Girish A Hampannavar1, Neeta Thapliyal1, Venkata Narayana Palakollu1.   

Abstract

Pyrazolo[1,5-a]pyrimidine scaffold is one of the privileged hetrocycles in drug discovery. Its application as a buliding block for developing drug-like candidates has displayed broad range of medicinal properties such as anticancer, CNS agents, anti-infectious, anti-inflammatory, CRF1 antagonists and radio diagnostics. The structure-activity relationship (SAR) studies have acquired greater attention amid medicinal chemists, and many of the lead compounds were derived for various disease targets. However, there is plenty of room for the medicinal chemists to further exploit this privileged scaffold in developing potential drug candidates. The present review briefly outlines relevant synthetic strategies employed for pyrazolo[1,5-a]pyrimidine derivatives. It also extensively reveals significant biological properties along with SAR studies. To the best of our understanding current review is the first attempt made towards the compilation of significant advances made on pyrazolo[1,5-a]pyrimidines reported since 1980s.
Copyright © 2016 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Anti-cancer agents; Anti-infectious agents; Anti-inflammatory agents; CNS agents; Pyrazolo[1,5-a]pyrimidine; Radiopharmaceuticals

Mesh:

Substances:

Year:  2016        PMID: 27894044     DOI: 10.1016/j.ejmech.2016.11.019

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  14 in total

1.  Annulation of Hydrazones and Alkynes via Rhodium(III)-Catalyzed Dual C-H Activation: Synthesis of Pyrrolopyridazines and Azolopyridazines.

Authors:  Andrew D Streit; Adam J Zoll; Gia L Hoang; Jonathan A Ellman
Journal:  Org Lett       Date:  2020-01-24       Impact factor: 6.005

2.  Synthesis and biological evaluation of chalcone-linked pyrazolo[1,5-a]pyrimidines as potential anticancer agents.

Authors:  Chandrakant Bagul; Garikapati Koteswara Rao; Venkata Krishna Kanth Makani; Jaki R Tamboli; Manika Pal-Bhadra; Ahmed Kamal
Journal:  Medchemcomm       Date:  2017-07-13       Impact factor: 3.597

Review 3.  Research progress in the biological activities of 3,4,5-trimethoxycinnamic acid (TMCA) derivatives.

Authors:  Zefeng Zhao; Huanhuan Song; Jing Xie; Tian Liu; Xue Zhao; Xufei Chen; Xirui He; Shaoping Wu; Yongmin Zhang; Xiaohui Zheng
Journal:  Eur J Med Chem       Date:  2019-04-06       Impact factor: 6.514

Review 4.  Revisiting the Structure and Chemistry of 3(5)-Substituted Pyrazoles.

Authors:  Alina Secrieru; Paul Michael O'Neill; Maria Lurdes Santos Cristiano
Journal:  Molecules       Date:  2019-12-20       Impact factor: 4.411

5.  Synthesis and Antimicrobial Evaluation of Novel Pyrazolopyrimidines Incorporated with Mono- and Diphenylsulfonyl Groups.

Authors:  Amani M R Alsaedi; Thoraya A Farghaly; Mohamed R Shaaban
Journal:  Molecules       Date:  2019-11-05       Impact factor: 4.411

6.  Exploration of Pyrazolo[1,5-a]pyrimidines as Membrane-Bound Pyrophosphatase Inhibitors.

Authors:  Niklas G Johansson; Loïc Dreano; Keni Vidilaseris; Ayman Khattab; Jianing Liu; Arthur Lasbleiz; Orquidea Ribeiro; Alexandros Kiriazis; Gustav Boije Af Gennäs; Seppo Meri; Adrian Goldman; Jari Yli-Kauhaluoma; Henri Xhaard
Journal:  ChemMedChem       Date:  2021-10-12       Impact factor: 3.466

7.  Facile approach to benzo[d]imidazole-pyrrolo[1,2-a]pyrazine hybrid structures through double cyclodehydration and aromatization and their unique optical properties with blue emission.

Authors:  Gi Hun Bae; Suzi Kim; Na Keum Lee; Anuradha Dagar; Jeong Hwa Lee; Jeeyeon Lee; Ikyon Kim
Journal:  RSC Adv       Date:  2020-02-18       Impact factor: 3.361

Review 8.  Functional Pyrazolo[1,5-a]pyrimidines: Current Approaches in Synthetic Transformations and Uses As an Antitumor Scaffold.

Authors:  Andres Arias-Gómez; Andrés Godoy; Jaime Portilla
Journal:  Molecules       Date:  2021-05-05       Impact factor: 4.411

9.  Temperature-modulated selective C(sp3)-H or C(sp2)-H arylation through palladium catalysis.

Authors:  Thirupathi Gogula; Jinquan Zhang; Madhava Reddy Lonka; Shuaizhong Zhang; Hongbin Zou
Journal:  Chem Sci       Date:  2020-09-24       Impact factor: 9.825

10.  A New Method for the Synthesis of 3-Thiocyanatopyrazolo[1,5-a]pyrimidines.

Authors:  Vladimir A Kokorekin; Sergey V Neverov; Vera N Kuzina; Vladimir A Petrosyan
Journal:  Molecules       Date:  2020-09-11       Impact factor: 4.411

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