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2-Pyridone is considered as one of the most famous efficient pharmaceutical compounds. Many approaches were discovered to synthesize 2-pyridone. In this present research, chloroacetylation of benzylamine at simple conditions, EtONa/EtCOONa produced N-benzyl-2-chloroacetamide 2. Compound 2 was allowed to react with different reagents. These reagents are acetylacetone, ethyl cyanoacetate, ethyl acetoacetate, and diethyl malonate, creating 2-pyridone derivatives with a good yield. The structures of the prepared compounds were elucidated by spectral data (IR, 1HNMR, and 13CNMR). The synthesized compound was tested for its antimicrobial activity against the Gram-positive (Staphylococcus aureus) and the Gram-negative (Escherichia coli) bacteria. In addition, the antifungal activities of the compounds were tested against two fungi (Candida albicans and Aspergillus flavus). Molecular docking studies were applied using the Autodock vina method. Theoretical methods prove all the experimental results by using molecular docking using Autodock vina and by ADEMT studies. The docking results represent that compound 20 had the best docking free energy, and it is the effective compound toward the selected bacterial and fungal proteins. ADME studies showed that the only compound 18 could cross the blood–brain barrier, and compound 15 was predicted to be soluble.

Some previously reported pyrimidine candidates 1–7 were founded to have potent tumor inhibition activities on diffrrent models of human primary and secondary brain tumors and in the same time these derivatives were founded to have potent anti-angiogenic effects on Ehrlich Ascites Tumor [EAT] cells in-vivo. These pyridine derivatives were founded to be selectively inhibit the p110α isoform. These pyridine derivatives were potent inhibited the histone deactylase. Also, they are inhibited the Sphingosine kinase SK1 activities.

A series of the newly substituted pyrano[1,2,3]triazine derivatives 3–14 were synthesized using compounds 1 and 2 as starting materials. Compound 2 was methylated using methyl iodide to compound 3, which was treated with aromatic aldehydes to give acryloyl derivatives 4a–c. Compounds 4a,b were reacted with ethyl cyano-acetate to give pyran-3-carboxylates 5a,b which were reacted with ethyl glycinate hydrochloride to give 6a,b. Treatment of 6a,b with hydrazine hydrate gives acid hydrazides 7a,b, which were reacted with 5,5-dimethyl-1,3-cyclohexanedione to give acetohydrazides 8a,b. Cyclization of 8b with 2-(4-nitrobenzylidene)malononitrile afforded hexahydroquinoline 9. However, the acridindione 10 was synthesized by heating of 8b with 2-(4-nitrobenzylidene)malononitrile in acetic acid containing few drops of triethylamine. Treatment of 7a,b with phenyl isothiocyanate or 2,5-hexanedione or phthalic anhydride gave compounds 11a,b, 13a,b and 14a,b, respectively. In the present work, all the selected pyrano[1,2,3]trizine derivatives were soluble in DMSO at concentrations high enough to allow cell experiments, and the in vitro biological activity of these compounds was evaluated by their growth inhibitory potency in liver HEPG2 cancer cell lines. The cytotoxic potency of compounds 3–14 was studied in comparison to the known anticancer drugs 5-fluorouracil and doxorubicin.

The structure of the natural dipyranocoumarin dipetalolactone has been confirmed by an unambiguous synthetic route from resorcinol. This sequence was initiated by a pyran ring formation step which introduced the 3-chloro-3-methylbut-1-yne moiety. Then, the expected product undergoes a Fremy’s salt-meditated oxidative addition followed by ring closure to yield dipetalolactone. Dipetalolactone was also found to have immunological activity in a mouse carcinoma S180-bearing mice cell line.

A series of novel coumarin derivatives were synthesized from 6-hydroxy-7-methoxy-4-methyl coumarin which was isolated from the aerial parts of the Egyptian medicinal plant Ammi majus L. (Apiaceae). The key intermediate 3-amino-5-methoxy-1-(4-methoxyphenyl)-10-methyl-8-oxo-1,8-dihydropyrano[3,2-f]chromene-2-carbonitrile (3c) was obtained in one-pot synthesis by treating α-cyanocinnamonitrile (1-c) with the natural compound: 6-hydroxy-7-methoxy-4-methyl coumarin (2). Chemical, elemental and spectroscopic evidences confirmed the structures of the synthesized compounds. Some of the newly synthesized compounds exhibited better anti-inflammatory activities at low concentrations compared with indomethacin as positive control.

A series of newly substituted thieno[3,2-g]chromene derivatives were synthesized from 1-(7-mercapto-2,2-dimethylchroman-6-yl)ethanone (3) as starting material. The compound 3 in turn was synthesized by reacting of 1-(2,4-dihydroxyphenyl)ethanone with isoprene to get compound 2 followed by its reaction with phosphorus pentasulfide. Condensation of 3 with N-phenylchloroacetamide or phenacylbromide gave the corresponding thienochromene derivatives 5 and 6. Also, compound 3 was reacted with maleic anhydride and acrylonitrile to afford the corresponding derivatives 8 and 9, respectively. Alkylation of 3 with diazomethane or ethyl bromoacetate afforded the corresponding S-substituted derivatives 10 and 11. The latter compound 11 was cyclized to ester derivative 12, which was obtained directly from 3 on reaction with ethyl bromoacetate. Treatment of 12 with hydrazine hydrate afforded the corresponding hydrazide 13, which was condensed with aromatic aldehydes or acetyl acetone to yield the corresponding Schiff’s bases 14a–d S-pyrazolo derivative 15, respectively. Finally, compound 13 was treated with 2,5-hexandione or carbon disulfide to give the corresponding compounds 16 and 17, respectively. Some of the newly synthesized compounds exhibited better anti-inflammatory activities than the reference controls with low concentrations. The structures of newly synthesized compounds were confirmed by chemical, elemental, and spectroscopic evidences. The detailed synthesis, spectroscopic data, and pharmacological activities were reported.

We present an efficient and facile synthesis of 4,6-diaryl-2-oxo-1,2-dihydropyridine-3-carbonitriles (5a–j) via a four-component system of aromatic aldehydes (1), acetophenones (2), ethyl cyanoacetate (3), and ammonium acetate (4). The short reaction time coupled with the simplicity of the reaction procedure and clean reaction make this method one of the most efficient methods for synthesis of this class of compounds.

A novel and mild protocol for the synthesis of phosphonotripeptide 16 were achieved from novel formylpyrazolofuran 3 , benzyl carbamate 5 , triphenyl phosphite 6 by Birum-Oleksyszyn reaction using copper (II) trifliate as Lewis acid catalyst in dry dichloromethane at room temperature which synthesis of novel N-benzyloxy-α-aminophosphonate 7 . A mechanism for this condensation reaction is proposed. Cleavage of the N-benzyloxy carbonyl group under acid hydrolysis afford the free α-aminophosphonate 9 in quantitative yield. This in turn, by reaction with N-phthaloylglycine 12 via TUBU to phthalimido group 13 .Cleavage of phthalimido group under hydrazinedihydrochloride afford free peptide 14 .the result phosphonotripeptide 16 obtained by the reaction of free peptide with bioactive cyclic moiety-COCl 15 . The structures of all new compounds were established by IR, 1 HNMR and mass spectral data. Also anti-cancer, anti-inflammatory and biochemical activities of all these compounds were reported.

In continuation to our search for new heterocyclic systems based antiinflammatories, the suggestion and synthesis of some pyrimidines, thienopyrimidines, and their derivatives, were herein realized. The pharmacological screening showed that many of these compounds have good antiinflammatory activity. The structure assignments of the new compounds are based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data, and pharmacological properties are reported.

A series of pyrimidinones, thienopyrimidines, and their derivatives were synthesized using N-methylindolyl acetic acid as a starting material. Sixteen new heterocyclics containing a pyrimidine ring were thus prepared. The pharmacological screening showed that many of these compounds have good analgesic and antiparkinsonian activities comparable to Voltarene® and Benzatropine® as reference drugs. The structure assignments of the new compounds based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data, and pharmacological properties are reported.

A set of 20 disperse dyes (V)/(VIII) is synthesized by reaction of hydrazinopyrazolopyridazine (IV) with arylazoacetylacetone or -malononitrile.

In continuation to our search for new heterocyclic systems based antiinflammatories, the suggestion and synthesis of some pyrimidines, thienopyrimidines, and their derivatives, were herein realized. The pharmacological screening showed that many of these compounds have good antiinflammatory activity. The structure assignments of the new compounds are based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data, and pharmacological properties are reported.

A series of pyrimidinones, thienopyrimidines, and their derivatives were synthesized using N-methylindolyl acetic acid as a starting material. Sixteen new heterocyclics containing a pyrimidine ring were thus prepared. The pharmacological screening showed that many of these compounds have good analgesic and antiparkinsonian activities comparable to Voltarene® and Benzatropine® as reference drugs. The structure assignments of the new compounds based on chemical and spectroscopic evidence. The detailed synthesis, spectroscopic data, and pharmacological properties are reported.

Investigation of the aerial parts of the Egyptian medicinal plant Ammi majus L. led to isolation of new coumarin, 6-hydroxy-7-methoxy-4 methyl coumarin (2) and 6-hydroxy-7-methoxy coumarin (3); this is the first time they have been isolated from this plant. The structures of the compounds (2 &3) were elucidated by spectroscopic data interpretation and showed anti-inflammatory and anti-viral activity. Graphical abstract An efficient, one-new coumarin (2) was isolated from the aerial parts of the A. Majus L. was evaluated for their anti-viral and anti-inflammatory activities.