Synthesis of new coumarin derivatives and assessment of their antimicrobial efficacy.

Aim: Developing new antimicrobial agents in response to the urgent challenge of antimicrobial resistance.

Methods: Synthesis of the targeted coumarins, elucidation of their structures using spectroscopic tools, and investigation of their antimicrobial activity.

Results: Coumarin-pyrazole with CF in the 3-position of the pyrazole ring displayed the lowest minimum inhibitory concentrations (MICs) and the minimum bactericidal concentrations (MBCs) with values of 1.

Preparation of thiourea derivative incorporated AgPO core shell for enhancement of photocatalytic degradation performance of organic dye under visible radiation light.

Photocatalysis is a promising technique to reduce hazardous organic pollutants using semiconductors under visible light. However, previous studies have been concerned with the behavior of silver phosphate (AgPO) as n-type semiconductors, and the problem of their instability is still under investigation. Herein, 4,4'-(((oxalylbis(azanediyl)) bis(carbonothioyl)) bis(azanediyl)) dibenzoic acid is synthesized by green method and used to enhance the photocatalytic behavior for AgPO.

2-Thioxo-3,4-dihydropyrimidine and thiourea endowed with sulfonamide moieties as dual EGFR and VEGFR-2 inhibitors: Design, synthesis, docking, and anticancer evaluations.

The effectiveness of a new series of thiopyrimidine and thiourea containing sulfonamides moieties was tested on HCT-116, MCF-7, HepG2, and A549. HepG2 cell line was the one that all the new derivatives affected the most. The greatest potent compounds against the four HepG2, HCT116, MCF-7, and A549 cell lines were 8f and 8g with IC  = 4.

Synthesis of Novel Nano-Sulfonamide Metal-Based Corrosion Inhibitor Surfactants.

The synthesis of novel corrosion inhibitors and biocide metal complex nanoparticle surfactants was achieved through the reaction of sulfonamide with selenious acid to produce a quaternary ammonium salt. Platinum and cobalt surfactants were then formed by complexing the first products with platinum (II) or cobalt (II) ions. The surface properties of these surfactants were then investigated, and the free energy of form micelles (ΔG) and adsorption (ΔG) was determined.

Design, synthesis, anticancer, and docking of some S- and/or N-heterocyclic derivatives as VEGFR-2 inhibitors.

Novel heterocyclic derivatives (4-22) were designed, synthesized, and evaluated against hepatocellular carcinoma type (HepG2) and breast cancer (MCF-7) cells, targeting the VEGFR-2 enzyme. Compounds 18, 10, 13, 11, and 14 were found to be the most potent derivatives against both the HepG2 and MCF-7 cancer cell lines, with GI  = 2.11, 2.

Pyridine-derived VEGFR-2 inhibitors: Rational design, synthesis, anticancer evaluations, in silico ADMET profile, and molecular docking.

Novel pyridine-derived compounds (5-19) were designed and synthesized, and their anticancer activities were evaluated against HepG2 and MCF-7 cells, targeting the VEGFR-2 enzyme. Compounds 10, 9, 8, and 15 were found to be the most potent derivatives against the two cancer cell lines, HepG2 and MCF-7, respectively, with IC  = 4.25 and 6.

Design, synthesis, molecular docking, in silico ADMET profile and anticancer evaluations of sulfonamide endowed with hydrazone-coupled derivatives as VEGFR-2 inhibitors.

A new series of sulfonamide endowed with hydrazone coupled to dimethyl and/or diethyl malonates were prepared. Various sulfa drugs were diazotized and followed by coupling with active methylene of dimethyl and/or diethyl malonate to afford the new intermediates hydrazones 3 and 4. The reactivity of hydrazone derivatives towards hydrazines was investigated.

Design, green synthesis, molecular docking and anticancer evaluations of diazepam bearing sulfonamide moieties as VEGFR-2 inhibitors.

Novel series of diazepam bearing sulfonamide moieties 5 and 7 were designed, synthesized and evaluated for anticancer activity against HepG2, HCT-116 and MCF-7 cell lines. MCF-7 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 5 was found to be the most potent derivative overall the tested compounds against the three HepG2, HCT116 and MCF-7 cancer cell lines with IC = 8.

Novel Anticancer Fused Pyrazole Derivatives as EGFR and VEGFR-2 Dual TK Inhibitors.

EGFR and VEGFR-2 represent promising targets for cancer treatment as they are very important in tumor development as well as in angiogenesis and metastasis. In this work, 6-amino-4-(2-bromophenyl)-3-methyl-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile and (E)-4-(2-Bromobenzylidene)-5-methyl-2,4-dihydro-3H-pyrazol-3-one were selected as starting materials to synthesize different fused pyrazole derivatives; dihydropyrano[2,3-c]pyrazole , , -, and , pyrazolo[4',3':5,6]pyrano[2,3-d]pyrimidine , pyrazolo[3,4-d]pyrimidine and , and pyrazolo[3,4-c]pyrazole derivatives were synthesized to evaluate their anticancer activity against HEPG2 human cancer cell lines compared to erlotinib and sorafenib as reference drugs. Seven compounds , , , , , , and showed nearly 10 fold higher activity than erlotinib (10.

Design and synthesis of some new thiophene, thienopyrimidine and thienothiadiazine derivatives of antipyrine as potential antimicrobial agents.

4-acetamide Pyrazolone 2 was synthesized by acetylation of 4-amino antipyrine 1 in excellent yield. 4-acetamide pyrazolone 2 was exploited as a starting material for the syntheses of hitherto unknown different types of new heterocyclic compounds incorporating the antipyrine moiety which expect highly biological activity against various microorganisms. Thus, Claisen condensation of 4-acetamide pyrazolone 2 with diethyl oxalate have been utility to afford new 4-oxaloacetyl antipyrine 3, which upon hydrazinolysis of the ester function to obtain the acetohydrazide derivative 18 which used as starting material to synthesize 1,2,4-triazol 19 and hydrazone 20 derivatives.