This research include developing new heterocyclic derivatives of 1,8-naphthalimides bearing 1,3-oxazole, 1,3-thiazole and 1,3,4-triazole moieties as the following:Direct imidation of 1,8-naphthalic anhydride with ethylglycinate in dimethylsulfoxide as solvent under reflux at high temperature for sixteen hours to obtain the N-ester-1,8-naphthalimide(1). Then conversion of this ester into (urea, thiourea, semicarbazide, phenylsemicarbazide, thiosemicarbazide and phenylthiosemicarbazide) derivatives through its reaction with (urea, thiourea, semicarbazide, phenylsemicarbazide, thiosemicarbazide and phenylthiosemicarbazide) respectively to give compounds (2,6,10,12,14 and16). Then cyclization of these compounds by using different reagents. The first cyclization of compounds (2 and 6) by using p-substituted phenacylbromide to give oxazole derivatives (3-5) and thiazole derivatives (7-9) respectively. Furthermore triazole derivatives were prepared through the second cyclization of compounds (10,12,14 and16) in alkaline media(4N. NaOH) to give compounds (11,13,15 and 17) respectively.The structure of the newly synthesized compounds was identified by their FTIR, and some of them by 1 H-NMR, 13 C-NMR spectral data and some physical properties and some specific reactions.Also new compounds were screened in three concentration for their in vitro antimicrobial activity against both Gram (+ve) such as Staphylococcus aureus, Bacillus and Gram (-ve) Escherichia Coli, pseudomonas aeuroginosa bacteria and against Candida albicans fungal and they were found to exhibit good to moderate antimicrobial activities.

This research involves preparation of many bisheterocycles attached to pyrrole rings have been synthesized by the stepwise procedure such asbis(1,2-dihydropyridazine-3,6-dione) (3),bis(2,3dihydrophthalazine-1,4-dione) (4) and bis(tetrahydropyridazine-3,6-dione) (5) derivatives of pyrrole. Further the bis(3,5-dimethyl-1H-pyrazol-1-yl)methanone (6), bis(3-methyl-1H-pyrazol5(4H)-one) (7) and bis(4H-1,3,4-oxadiazin-6(5H)-one) (8) pyrrole derivatives also prepared in good yields. Furthermore, series of bis-benzothiazine (10a-c), bis-benzoxathiazepine (11a-c)and bis-quinazoline compounds (12a-c) attached to pyrrole moieties also have been synthesized successfully.Structures of the newly synthesized compounds were established by physicochemical, elemental analysis CHNS, FTIR, H-NMR and C-NMR spectroscopic methods. The new synthesized agents were evaluated for their in vitro inhibitory effectagainst several candida isolates. Some of the evaluated compounds possessed good activities compared to a fluconazole, nystatin and clotrimazole standard antifungal drugs.

In the present research, a series of some azo compounds (5-9) and 1,2,3-triazoles (11,12) derived from 2-methyl quinazolin-4(3H)-one (3) have been synthesized successfully by stepwise routes includes the following: 3-amino-2-methylquinazolin-4(3H)-one (3) prepared firstly by conversion of 2-aminobenzoic acid into methyl 2-aminobenzoate (1) followed by reaction with acetic anhydride to form methyl -2-acetamidobenzoate (2). The amide then allowed reacting with hydrazine hydrate to give compound (3). Diazotization reaction with sodium nitrite in the presence of hydrochloric acid yield the 3-(chlorodiazenyl)-2-methylquinazolin-4(3H)-one (4). Diazonium salt (4) then enter two different routes. The first route was its conversion into azo compounds (5-9) by reaction with coupling components.The second route included formation of 1,2,3triazole derivatives by interconversion of compound (4) into azido compound (10) followed by treatment with ethyl acetoacetate, acetyl acetone to give 5-methyl-1-(2-methyl-4-oxoquinazolin-3(4H)-yl)-1H-1,2,3-triazole-4-carboxylic acid (11) and3-(4-acetyl-5-methyl-1H-1,2,3-triazol-1-yl)-2-methylquinazolin-4(3H)-one (12) in good yield. Newly synthesized derivatives were characterized spectroscopically by FTIR, 13 C-NMR and 1 H-NMR spectral technique and by determination of their physical properties. The reactions monitored by thin layer chromatography. The antibacterial potential of synthesized compounds have been tested against the growth of four gram positive and gram negative pathogenic bacterial strains using agar well diffusion method. Ampicillin trihydrate used as reference drug. The results of the antibacterial study showed that compounds (7-9)appeared good activity

Cancer is a significant worldwide public health issue. The adverse effects of anticancer chemotherapies still compromise the quality of life of patients. To identify new potential targeted anticancer agents, a series of pyrazoline derivatives were synthesized and evaluated for anticancer effects on A549 (human lung adenocarcenoma cell line). In silico evaluation methods were done before synthesis through molecular docking via genetic optimization for ligand docking (GOLD) Suite software with EGFR tyrosine kinase and exhibited significant tyrosine kinase inhibition activities compared with Erlotinb as a reference drug due to their hydrogen bonding and short contact interaction with key amino acids and these results are compatible with the experimental findings. The new derivatives were synthesized by incorporating pyrazoline pharmacophore into nabumetone moiety as a starting molecule and the chalcone derivatives as intermediate products. The compounds structure were confirmed by 1 H-NMR, some physicochemical properties and infrared spectroscopy. An in vitro assay demonstrated that the final compounds (P1, P2, P3 and P4) exerted potent to moderate cytotoxic activity in the micromolar range with an IC50 values (15.409µM, 7.24µM, 27.05µM, 22.45µM) respectively when compared with Erlotinib (IC50 =25.23µM) while (P5&P6) show weak activity. Pharmacokinetic and physicochemical properties of the final compounds predicted by using ADME evaluations. The results showed all the synthesized compounds have high oral bioavailability and good GI absorption.

Infections caused by bacteria have a significant impact on public health. Chemical synthesis of new derivatives of cephalexin inked to amino acid (tryptophan or histidine) through an amide bond at the acyl side chain is achieved. This is a new approach of incorporating, tryptophan and histidine into the the primary amino group of cephalexin, in order to provide a bulky group very close to the β-lactam ring. This chemical addition act as isosteric group to the alkoximino that protect beta lactam ring from bacterial beta lactamase enzyme. The new derivatives may show resistance to β-lactamases, improve activity and pharmacokinetic properties and may give new life for old drugs that are susceptible to hydrolysis by most β-lactamases. The chemical structures of these derivatives were confirmed by: FTIR, 1H-NMR spectroscopy, elemental micro analysis and some physical properties. Molecular docking on serine beta lactamase and prediction of ADME parameters were recorded using GOLD suite and Swiss ADME software respectively. Docking scores of the new derivatives of Cephalexin on β-lactamases were higher than those of Cephalexin, which may indicate better activity