2003. Synthesis of novel quinazoline derivatives as antimicrobial agents. (csic.es)
Synthesis of some new 4,5-substituted-4H-1,2,4-trizole-3-thiol derivatives. (csic.es)
Synthesis of unusual indole and azaindole derivatives. (cqab.eu)
Barus, Synthesis and evaluation of antimicrobial activities of new functional derivatives of 3-[5-(4-nitrophenyl)-2-furyl]-4-pyrazole-carbaldehydes, Biointerface Res. (dntb.gov.ua)
Sun, Synthesis and antifungal activity of the derivatives of novel pyrazole carboxamide and isoxazolol pyrazole carboxylate, Molecules, № 20, с. (dntb.gov.ua)
Ouyang, Synthesis and antiviral activities of pyrazole derivatives containing an oxime moiety, J. Agric. (dntb.gov.ua)
Burlov, Synthesis, structure, photo- and electroluminescent properties of zinc (II) complexes with aminomethylene derivatives of 1-phenyl-3-methyl-4-formylpyrazol-5-one and 3- and 6-aminoquinolines, Synth. (dntb.gov.ua)
Inhibitors5
This review mainly focuses the recent and current progresses in quinazoline derivatives as an acetylcholinesterase (AChE) and monoamine oxidase (MAO)-B inhibitors. (amrita.edu)
Here we report a novel class of GCase quinazoline inhibitors, obtained in a high throughput screening, with moderate potency against wild-type GCase. (northwestern.edu)
designed and synthesized a series of phosphoramide mustard functionality, which was incorporated into the quinazoline scaffold, and their potential as EGFR inhibitors for the treatment of lung cancer was investigated. (japsonline.com)
HQSAR Study and Molecular Design of Benzimidazole Derivatives as Corrosion Inhibitors [J]. Acta Phys. (pku.edu.cn)
Cherrak, Performance evaluation of newly synthetized bi-pyrazole derivatives as corrosion inhibitors for mild steel in acid environment, J. Mol. (dntb.gov.ua)
Inhibitor3
Structure-activity relationships for inhibition of erbB1, erbB2, and erbB4 were determined for a series of quinazoline- and pyrido[3,4-d]pyrimidine-based analogues of the irreversible pan-erbB inhibitor, canertinib. (auckland.ac.nz)
The IC50 value of the best quinazoline inhibitor was 64 nM. (cas.cz)
To develop novel and more potent quinazoline-phosphoramidate mustard conjugates as epidermal growth factor receptor (EGFR) inhibitor, three-dimensional quantitative structure-activity relationship [comparative molecular field analysis (CoMFA) and comparative molecular similarity indices analysis (CoMSIA)] combined with molecular docking were performed. (japsonline.com)
Inhibitory activity3
Thus, three series of quinazoline derivatives were prepared and tested for their potential inhibitory activity toward COX-1 and COX-2. (cas.cz)
The contour maps that were produced by the CoMFA and CoMSIA models revealed that steric, electrostatic, and hydrophobic fields were crucial in the inhibitory activity of quinazoline-phosphoramidate derivatives. (japsonline.com)
Then, the possible CA inhibition against the human CA isoforms I, II, and IX was investigated, together with the EGFR inhibitory activity, with the most powerful derivatives. (bvsalud.org)
Heterocyclic compounds3
Abstract Among the N-containing heterocyclic compounds, quinazoline-4-(3H)-one derivatives have been the center of attraction of medicinal and synthetic chemists due to their excellent versatility in biological activities that are witnessed by many approved drugs available in the market which contains quinazoline as main pharmacophore unit. (amrita.edu)
These polymaleimide derivatives can be active catalysts for the selective oxidation of heterocyclic compounds to quinoline and indole via the recycling of -C=O and -C-OH groups, which was confirmed by tracing the reaction with GC-MS using maleimide as the catalyst and by FT-IR analysis with polymaleimide as the catalyst. (nature.com)
Catalytic performance exploration showed that these polymaleimide (PMI) derivatives can be active catalysts for the selective oxidation of heterocyclic compounds to quinoline and indole via the recycling of -C=O and -C-OH groups. (nature.com)
Abstract1
[email protected] ABSTRACT Quinazoline is a bicyclic compound earlier known as benzo- 1, 3-diazine. (pharmaresearchlibrary.com)
Compounds1
Rational design and a SAR study of this class of compounds led to a new series of quinazoline derivatives with single-digit nanomolar potency. (northwestern.edu)
Pyrazole1
Bekhit, Investigation of the anti-inflammatory and analgesic activities of promising pyrazole derivative, Eur. (dntb.gov.ua)
Pyrido1
Quinazoline 54 and pyrido[3,4-d]pyrimidine 71 were identified as clearly superior to canertinib. (auckland.ac.nz)
Potent1
In addition, animal studies indicate that it is significantly more potent than its derivatives and has a very long, dose-independent, half-life. (midas-pharma.com)
Toxicity1
We have synthesized a new quinoline (4,7-dichloroquinoline) derivative which showed significant larvicidal and pupicidal properties against a malarial and a dengue vector and a lethal toxicity ranging from 4.408 µM/mL (first instar larvae) to 7.958 µM/mL (pupal populations) for Anopheles stephensi and 5.016 µM/mL (larva 1) to 10.669 µM/mL (pupae) for Aedes aegypti . (nature.com)
Molecular3
The review has leanings towards the molecular determinants and structure-activity relationships (SAR) of quinazoline derivatives on AChE and MAO inhibitory potencies. (amrita.edu)
The focus of the present work was to develop the 3D-QSAR-based k-nearestneighbour molecular field analysis (kNN-MF) studies on benzylamine derivatives. (ijpsonline.com)
Computer-assisted superimposition of SGB-1534 and 20b showed little structural correspondence between the quinazolinone and 2,3-dihydroimidazo[1,2-c]quinazoline nucleus, and specific interactions of these molecular fragments with the receptor protein appear unlikely. (zhihuiya.com)
Linagliptin1
Linagliptin is a caffeine and quinazoline derivative that inhibits dipeptidyl peptidase 4 (DPP-4). (midas-pharma.com)
Anti-inflammatory1
A number of substituted quinazoline are known for their pharmacological importance, Literature indicate that derivatives consist of variety of pharmacological activity activities like anti-inflammatory, analgesic, anti-microbial, CNS depressant and anti-tubercular, anti-hypertensive anti-tumor activities have reported also. (ajpsonline.com)
Pyrrole1
Inspired by these results, in this work, a molecularly defined single-site heterogeneous catalyst has been designed and prepared via the oxidative polymerization of pyrrole derivatives. (nature.com)
Activity1
Activity of Quinazoline Derivatives: A Review. (ajpsonline.com)
Prediction1
Prediction of Antitumor Activities of Indolo[1,2-b]Quinazoline Derivatives Using Electrotopological State Indices for AtomTypes [J]. Acta Phys. (pku.edu.cn)
Series1
In the present work, we developed a novel series of substituted benzyl‐1,2,3‐triazole derivatives linked to hydrazinecarbothiamide via methoxyphenyl linker and assessed them for their tyrosinase inhibitory effects in t. (researchgate.net)
Activities2
In this article, different s-substituted benzimidazole-thioquinoline derivatives were designed, synthesized, and evaluated for their possible α-glucosidase inhibitory activities. (researchgate.net)
The tyrosinase inhibitory activities of all synthesized derivatives 5a-m were determined against mushroo. (researchgate.net)
Here, we report that a molecularly defined, single-active site heterogeneous catalyst has been designed and prepared via the oxidative polymerization of maleimide derivatives. (nature.com)
Class1
Prazosin hydrochloride, USP a quinazoline derivative, is the first of a new chemical class of antihypertensives. (nih.gov)
Potential2
Benzylamine derivatives have recently been demonstrated interesting potential as the treatment for chronic obstructive pulmonary disease via interaction with the PDE4 enzymes. (ijpsonline.com)
The effects of the 5-cyanopyridine derivatives 6e and 6l on cell-cycle disruption and the apoptotic potential were then investigated. (bvsalud.org)
Study1
In the current study, twenty-five indole-carbohydrazide derivatives linked to different aryl substitutions were rationally designed and synthesized. (researchgate.net)
Properties1
Quinazolinones and several of their derivatives have been found to be of greater interest in view of their varied biological and pharmacological properties. (pharmaresearchlibrary.com)