Pyrimidine-Pyrazole Hybrids as Morpholinopyrimidine-Based Pyrazole Carboxamides: Synthesis, Characterisation, Docking, ADMET Study and Biological Evaluation

  title={Pyrimidine-Pyrazole Hybrids as Morpholinopyrimidine-Based Pyrazole Carboxamides: Synthesis, Characterisation, Docking, ADMET Study and Biological Evaluation},
  author={Mayur K. Vekariya and Rajesh H. Vekariya and Kinjal D. Patel and Nirav P. Raval and Prapti U. Shah and Dhanji P. Rajani and Nisha K Shah},
9 Citations
A Retrospective Study of Synthesis, Structure-Activity Relationship and Antimicrobial Activity of 4-Formyl Pyrazole Containing Isoniazid Moiety
4-Formyl pyrazole is nitrogen containing heterocyclic aromatic molecule containing isoniazid moiety. The molecule is formed by fusion of two heterocyclic ring i.e. pyrazole and isoniazid. The current
Pyrazole Bearing Pyrimidine Analogues as the Privileged Scaffolds in Antimicrobial Drug Discovery: A Review
Abstract Historically, heterocyclic compounds including N-heterocycles and their derivatives are valuable source for the identification of therapeutically active agents. Studies in the recent two
Recent advances in development of anthelmintic agents: Synthesis and biological screening
This review is primarily addressed to the description of the recent advances in the synthesis of heterocyclic compounds as anthelmintic agents, which can facilitate the development of more potent and effective anthel mintic agents.
Recent developments in synthetic chemistry and biological activities of pyrazole derivatives
This systematic review covers the published studies from 1990 to date and provides an overview on the recent advances in synthetic approaches for the preparation of pyrazoles, including eco-friendly methodologies, heterogeneous catalytic systems, ligand-free systems, ultrasound and microwave-assisted reactions.
Structure elaboration of isoniazid: synthesis, in silico molecular docking and antimycobacterial activity of isoniazid–pyrimidine conjugates
Investigation of a new series of isoniazid–pyrimidine conjugates synthesized in good yields and evaluated for antitubercular activity against the H37Rv strain of Mycobacterium tuberculosis suggests a rationale for further work on this promising series of antitubercles.


Design, synthesis, and evaluation of new thiadiazole-based direct inhibitors of enoyl acyl carrier protein reductase (InhA) for the treatment of tuberculosis.
From this series, 8d is identified as having the best balance of potency and properties, whereby the resolved 8d S-enatiomer shows encouraging in vivo efficacy.
Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity.
Discovery of 4-{4-[(3R)-3-Methylmorpholin-4-yl]-6-[1-(methylsulfonyl)cyclopropyl]pyrimidin-2-yl}-1H-indole (AZ20): a potent and selective inhibitor of ATR protein kinase with monotherapy in vivo antitumor activity.
The discovery and synthesis of a series of sulfonylmorpholinopyrimidines that show potent and selective ATR inhibition are described that leads to compound 6 (AZ20) which inhibits ATR immunoprecipitated from HeLa nuclear extracts with an IC50 of 5 nM.
Overcoming the Limitations of Fragment Merging: Rescuing a Strained Merged Fragment Series Targeting Mycobacterium tuberculosis CYP121
Freedom to merge: A combination of crystal structure examination and in silico predictions made it possible to overcome the conformational limitations of fragment merging and escape the internal
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.
In vitro and in vivo biomarker studies demonstrated the ability of 3 to shut down the PI3K/Akt pathway and induce apoptosis in cancer cells, validating suppression of PI3k/mTOR signaling as a potential anticancer therapy.