Synthesis, Cytotoxicity Evaluation, DFT Molecular Modeling Studies and Quantitative Structure Activity Relationship of Novel 1,8-Naphthyridines

Fadda, Ahmed A.; Defrawy, Ahmed M. El; El-Hadidy, Sherihan A.

doi:10.5923/j.ajoc.20120204.03

Cited by 26 publications

(20 citation statements)

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“…The synthetic procedures adopted to obtain the target compounds are depicted in Schemes 1-4. In this paper, we report a convenient route to some new naphthyridinyl-1,2,4-triazoles starting from a readily accessible 4-oxo-1,4-dihydro-1,8-naphthyridine-3-carbohydrazide (1) [30]. Therefore, when the acid hydrazide 1 reacted with phenyl isothiocyanate in refluxing ethanol containing a catalytic amount of glacial acetic acid, it afforded 2-(4-oxo-1,4-dihydro-1,8-naphthyridine-3-carbonyl)-Nphenylhydrazinecarbo thioamide (2) in excellent yield.…”

Section: Resultsmentioning

confidence: 99%

New Synthetic Approaches for Cytotoxic Activity of Novel 1,8‐Naphthyridine Derivatives

El-Hadidy¹,

Selim

2017

Journal of Heterocyclic Chem

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A series of substituted 1,8-naphthyridine derivatives was synthesized as cytotoxic agent by using starting material 1,4-dihydro-4-oxo-1,8-naphthyridine-3-carbohydrazide (1). Further reactions on compound 1 were processed with different reagents to afford the corresponding 3-heteraryl-1,8-naphthyridine derivatives 2-22. In vitro cytotoxic activities of new synthesized compounds were assayed against Ehrlich ascites carcinoma, which showed that compounds 3 and 12 had the more potent cytotoxic activity.

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Section: Resultsmentioning

confidence: 99%

New Synthetic Approaches for Cytotoxic Activity of Novel 1,8‐Naphthyridine Derivatives

El-Hadidy¹,

Selim

2017

Journal of Heterocyclic Chem

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“…The cytotoxic activities of the prepared sulfonamides were examined versus HepG2, WI-38, MCF-7, and VERO, carried out according to the previously reported procedure. 16 Boiling 10 with hydrazine hydrate in ethanol/DMF solution (1:1 ratio) afforded the corresponding acid hydrazide 11. The infrared spectrum of 10 displayed bands at ν 3435 and 3360 cm -1 due to NHNH 2 group, besides the presence of amide carbonyl group at ν 1685 cm -1 Reaction of hydrazide 11 with carbon disulphide in refluxing pyridine afforded the thioic acid 12.…”

Section: Cytotoxicity Activitymentioning

confidence: 99%

Some Studies in Sulfadiazine Incorporating Pyridine, Pyrimidine, Oxadiazole, and Azo Moieties Endowed with Pharmaceutical Potency

El-Hadidya

Abu-Melhab

2020

ACSi

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A set of substituted sulfadiazine compounds was prepared as cytotoxic and antitumor agents by using 4-amino-N-(pyrimidin-2-yl)benzenesulfonamide (1) as the starting material. Compound 1 was reacted with different reagents to give the corresponding sulfadiazines 2-18 and hydrozaones 19a-h which were evaluated for their in vitro cytotoxicity versus four cancer cell lines. Compounds 3, 5, 19d and 19h were active against the tested cancer cells.

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“…EMME ( 1 ) and Michael acceptors such as “alkoxyacrylic” derivatives were used in the synthesis of biologically active compounds. “Oxacin” type antibacterials having quinoline and naphyridine structures are good examples . These Michael acceptors reacted with different nucleophiles to give cyclic, fused cyclic structures and related compounds .…”

Section: Introductionmentioning

confidence: 99%

Antimicrobial Properties of Some New Synthesized Benzothiazole Linked Carboxamide, Acetohydrazide, and Sulfonamide Systems

Fadda

Soliman

Bayoumy

2019

Journal of Heterocyclic Chem

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We report herein the interaction of diethylethoxymethylene malonate (1) with 2‐cyanomethylbenzothiazole (7) to give diethyl 2‐(2‐benzothiazole‐2‐(3H)‐ylidiene)‐2‐(cyano ethyl) malonate (8a) in excellent yield. Ethyl 4‐cyano‐1‐oxo‐1H‐benzo[4,5]thiazolo[3,2‐a]pyridine‐2‐carboxylate (9) was synthesized from 8a and subjected to react with hydrazine hydrate to give its corresponding acid hydrazide 10. Condensation of 10 with different acid anhydrides afforded the corresponding benzothiazolo pyridine carboxamide derivatives 11–15. In addition, we report a simple synthesis of N′‐(benzo[d]thiazol‐2‐yl)‐2‐((4‐ayl)amino)acetohydrazide derivative (17), which then reacted with different amines to give the corresponding acetohydrazide derivatives 19a–c. Moreover, compound 17 reacted with some sulfonamide derivatives to give the corresponding sulfonamide derivatives 20 and 22a,b.The newly synthesized compounds were established their structures on the bases of their correct analytical and spectral data and evaluated their antimicrobial activity. It was found that compounds 22a,b displayed the highest antimicrobial activity against the tested organisms.

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Synthesis, Cytotoxicity Evaluation, DFT Molecular Modeling Studies and Quantitative Structure Activity Relationship of Novel 1,8-Naphthyridines

Cited by 26 publications

References 1 publication

New Synthetic Approaches for Cytotoxic Activity of Novel 1,8‐Naphthyridine Derivatives

New Synthetic Approaches for Cytotoxic Activity of Novel 1,8‐Naphthyridine Derivatives

Some Studies in Sulfadiazine Incorporating Pyridine, Pyrimidine, Oxadiazole, and Azo Moieties Endowed with Pharmaceutical Potency

Antimicrobial Properties of Some New Synthesized Benzothiazole Linked Carboxamide, Acetohydrazide, and Sulfonamide Systems

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