Affiliation:
1. Department of Medicinal Chemistry, College of Pharmacy, Mansoura University, Mansoura 35516, Egypt
Abstract
Antifolates are a class of drugs used as antibacterial, antiparasitic, and anticancer agents.
This review focuses on 2-substituted-mercapto-quinazolin-4(3H)-one analogues as dihydrofolatereductase
(DHFR) inhibitors. Several research work have concluded a structural model for this class
of 2-thio-quinazoline derivatives to get compounds with remarkable biological activity. The pattern
and orientation of the p-system substitutions with regard to the quinazoline nucleus manipulate the
activity. The application of the obtained model criteria produced compounds 18, 20 and 21, which
proved to be 4-8 times more active than the reference drug methotrexate (MTX, 1).
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,Pharmacology,General Medicine
Cited by
8 articles.
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1. Green synthesis of 2‐thioxo‐4‐quinazolinones from 2‐aminobenzamide and isothiocyanates;Vietnam Journal of Chemistry;2024-03-14
2. A Direct Method for Synthesis of Quinoxalines and Quinazolinones Using Epoxides as Alkyl Precursor;Molecules;2023-11-02
3. An Oxidant-Free and Mild Strategy for Quinazolin-4(3H)-One Synthesis via CuAAC/Ring Cleavage Reaction;Molecules;2023-07-28
4. Synthesis, Antifungal Evaluation of 3-[{(1-aminomethyl) -5,7-dimethyl-2-
oxoindolin-3-ylidene} amino]-2-phenylquinazolin-4(3H)-ones and their
NLO, MESP, Global Reactivity Descriptor, and AIM Study through DFT
Approach;Letters in Organic Chemistry;2023-04
5. Application of N,N-Dimethylethanolamine as a One-Carbon Synthon for the Synthesis of Pyrrolo[1,2-a]quinoxalines, Quinazolin-4-ones, and Benzo[4,5]imidazoquinazolines via [5 + 1] Annulation;The Journal of Organic Chemistry;2022-10-18