New Heterocyclic Compounds Derived from 4,6‐Diamino‐3‐cyano‐2‐methylthiopyridine and their Biological Activity

Ghattas, Abd El-Badih A. G.; Khodairy, A.; Moustafa, H. M.; Hussein, Bahgat R. M.

doi:10.1002/jhet.2649

Cited by 11 publications

(4 citation statements)

References 22 publications

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“…In view of these findings and in continuation of our previous work [20][21][22][23][24][25], we reported herein a simple, rapid, and high-yielding multicomponent reaction protocol for the synthesis of 2-tosyloxyphenylpyridine derivatives 5 and 8-17.…”

Section: Introductionmentioning

confidence: 58%

Multicomponent Reaction for Synthesis of Novel 2‐Tosyloxyphenylpyridines

Hussein

Ali

2019

Journal of Heterocyclic Chem

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2‐Tosyloxybenzaldehyde 1 was reacted with some active methylene compounds as 1:1 or 1:2 molar ratio under different basic conditions to afford the corresponding 2‐tosyloxyarylidenes 2–4 and/or 2‐tosyloxyphenylpyridine 5, respectively. Multicomponent reaction of 2‐tosyloxyarylidene 2 and AcONH4 with active methylene compounds namely: malononitrile, ethyl acetoacetate, ethyl benzoylacetate, 1,3‐benzothiazol‐2‐ylacetonitrile, acetophenones or 3‐acetylheterocycle derivatives in methanol gave 2‐tosyloxyphenylpyridine derivatives 8–17, respectively. The structures of new compounds were elucidated by elemental and spectral analysis.

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Section: Introductionmentioning

confidence: 58%

Multicomponent Reaction for Synthesis of Novel 2‐Tosyloxyphenylpyridines

Hussein

Ali

2019

Journal of Heterocyclic Chem

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“…The 160-163 were tested as anti-inflammatory agents. [85] During in vivo studies (using carrageenan paw oedema) in rats these compounds were found efficient oedema inhibitors. Available standards indomethacin and celecoxib both showed 31 % inhibition in 1 h and it increased to more than 60 % after 3 h. The initial results of tested compounds after 1 h were very close to the standard and these compounds exhibited inhibition in the range 30-37 %, while after 3 h the said inhibition was observed in the range 43-64 %.…”

Section: Antiinflamatory and Analgesics Activitiesmentioning

confidence: 99%

Pyridine Derivatives as Biologically Active Precursors; Organics and Selected Coordination Complexes

Khan

2021

ChemistrySelect

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Pyridine (py) is an important heterocyclic compound and is an integral part of various natural products. There are various medicines containing py ring system being available in the market to combat different human ailments. Observing the medicine market, Omeprazole, a widely used py-based drug in medicinal market since 1998. Netupitant (an antiemitic drug, since 2014) is used in combination with another drug to prevent acute and delayed vomiting and nausea associated with cancer chemotherapy led the run towards development of anticancer drugs. Several drugs have been approved by FDA for the treatment of cancer in recent years such as, Abemaciclib (2015), Lorlatinib (2018), Apalutamide (2018) and Ivosidenib (2019). Research on py on the bases of these advancements is an evergreen field and associated with greater hopes to address several disease related issues. Several compounds are in the process of clinical trials and are expected to serve various purposes in days to come. This review article deals with recent findings in py chemistry and its coordination complexes. The medicinal efficiency has been argued for organic and inorganic derivatives. Selected biological applications are hereby discussed as follow up study of our report in 2015. Suitable literature prior to 2015 has also been incorporated in appropriate places in order to cover the scope in broader sense.

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“…Recently, quinazoline compounds and the other heterocyclic compounds attracted many scientists due to their various uses and bioactivities such as antiviral activities, anticancer, antitumor, antidiabetic, antiplasmodium, antiparasite, antioxidant, antimicrobial, anti-inflammatory, and antitubercular. − Notable examples of quinazoline-based drugs include gefitinib and erlotinib, which are tyrosine kinase inhibitors used in the treatment of nonsmall cell lung cancer. These drugs have demonstrated significant efficacy and have revolutionized targeted cancer therapy.…”

Section: Introductionmentioning

confidence: 99%

Preparation, Agricultural Bioactivity Evaluation, Structure–Activity Relationships Estimation, and Molecular Docking of Some Quinazoline Compounds

Hussein,

Moustafa,

Abdou

et al. 2024

J. Agric. Food Chem.

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Quinazoline compounds have gained significant attention in the fields of agriculture and chemistry due to their diverse activities. In this study, we focused on a series of quinazoline derivatives (4a−l). The objectives involved multiple aspects, including preparation, evaluation of their agricultural bioactivity against the maize aphid (Rhopalosiphum maidis), estimation of the structure−activity relationships (SAR), and conducting molecular docking analysis. The results of the agricultural bioactivities revealed that compound (4b) possesses the highest insecticidal activity, and the other compounds have good potential as insecticidal agents. We conducted the SARs and also molecular docking investigation to elucidate the binding modes and interactions of these compounds with target proteins relevant to the agricultural bioactivity. The docking results provided valuable information on the binding affinities and molecular interactions, aiding in the rationalization of the observed bioactivity trends. The enzyme, acetylcholinesterase (AChE), was docked with the 12 synthetic compounds (4a−l). Among these compounds, (4b), (4i), and (4e)exhibited the highest binding affinity, with docking scores (S) of −7.96, −7.83, and −7.73 kcal/mol, respectively. They were followed by compounds (4d) (S = −7.57 kcal/mol), (4c) (S = −7.53 kcal/mol), (4g) (S = −7.34 kcal/mol), (4f) (S = −7.23 kcal/ mol), (4h) (S = −7.14 kcal/mol), (4k) (S = −6.61 kcal/mol), (4j) (S = −6.57 kcal/mol), (4a) (S = −6.28 kcal/mol), and finally (4l) (S = −6.01 kcal/mol). These compounds were shown to have a variety of binding interactions within the 2ACE active site, as evidenced by protein−ligand docking configurations. This study gives evidence that those compounds have AChE-inhibitory capabilities and, hence, may be used for AChE-targeting development. Also, the findings in this study highlight the potential of these compounds as agricultural agents and provide valuable insights for the design and development of some quinazoline derivatives with enhanced bioactivity for crop protection.

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New Heterocyclic Compounds Derived from 4,6‐Diamino‐3‐cyano‐2‐methylthiopyridine and their Biological Activity

Cited by 11 publications

References 22 publications

Multicomponent Reaction for Synthesis of Novel 2‐Tosyloxyphenylpyridines

Multicomponent Reaction for Synthesis of Novel 2‐Tosyloxyphenylpyridines

Pyridine Derivatives as Biologically Active Precursors; Organics and Selected Coordination Complexes

Preparation, Agricultural Bioactivity Evaluation, Structure–Activity Relationships Estimation, and Molecular Docking of Some Quinazoline Compounds

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