Fourteen novel 4-(5-amino-4-cyano-1,3-oxazol-2-yl)benzenesulfonamides have been designed, synthesized, and characterized by spectroscopy and spectrometry methods. They have also been investigated on the NCI-60 cancer cell lines. The most activity compounds, 2, 3, and 9, in concentration 10 µM demonstrated mean GI50 values of 77, 70, and 68%, respectively, against the tumor cells. The best activity compound 2 showed the following GI50 values: non-small cell lung cancer (HOP-92) - 4.56 µM, breast cancer (MDA-MB-468) - 21.0 µM, melanoma (SK-MEL-5) - 30.3 µM. Besides, this compound indicates low toxicity with TGI and LC50 values >100 µM against all cancer cell lines. The COMPARE analysis (NCI) of compound 2 showed a very high correlation (r=0.91) with Tamoxifen as a selective estrogen receptors modulator. Molecular docking studies of ligand 2 demonstrated the complexation with estrogen receptors as a possible antitumor mechanism. The ADMET analysis of compound 2 indicates an optimistic prediction as an antitumor agent.

A series of all novels 4(3-(4-Fluorophenyl)2-methyl-1-(4-(sulfonamidesubtituted)phenyl)-4-oxoazitidin-2-yl)-3-methyl-1-(p-tolyl)-1H-pyrazol-5(4H) One 5a-5r poly functionalized derivatives were containing sulfonamide functionality united with 2-Azitidinone (Azitidin-2-one or β-lactam) group which designed and synthesized with moderate to good yield. The starting with 4-acyl-2-pyrazolin-5-one (APYZ) 1 which condensed with different sulfonamides 2 produced intermediate Schiff bases 4-(arylideneamino)-N-(thiazol-2-yl)benzensulfonamide 3a-r were cyclization with 2-(4-flourophenyl)chloroacetylchloride (F-CAC) 4 which produced targeted compounds 5a-5r of 2-Azitidinone versatile group in good yield. The isolated compounds were recognized by spectral and elemental investigation. The compounds 5f, 5l, 5n, and 5r showed excellent increased antibacterial activity compared to streptomycin standard drug and 5c, 5f, 5l, 5o, and 5r showed moderate to good antioxidant properties with used DPPH radical scavenging assay.

In our work we study the toxic effects of the prepared pyridine and pyradazine derivatives. Five compounds have been synthesized in pure state as reported procedures, and their toxicity as potential insecticidal agents against adult and nymphs of Aphis nerii were screened. The toxicity data in adults, exhibited that compound 6a is more toxic than other synthesized compounds, which LC50 was1.04 ppm while, in nymph compound 4a is more toxic than other synthesized compounds, which LC₅₀ was 0.02 ppm. The other screened compounds showed weak to strong toxicological activity. The structure-activity relationships (SAR) for these compounds were also discussed.

Sulfonamides are a very good antibacterial agent that targets essential bacterial enzymes specifically DNA gyrase. The objective of the present work was to investigate the molecular docking of the (4-(tert-butyl)-N,N-diethylbenzenesulfonamide) with the DNA gyrase of S. aureus. The energy-free topoisomerase activity of the A subunit, which breaks the DNA, is inhibited by 4-quilones such as nalidixic acid and ciprofloxacin. The energy transducing activity of the B subunit is inhibited by novobiocin and other coumarin antibiotics. Single crystal X-ray diffractometer study was carried out to understand the structure, physical and chemical reactive parameters, the title compound is crystallized under monoclinic crystal system with the space group of P21/C. To understand the behaviour of the title compound in living organism, Absorption, Distribution, Metabolism, Excretion analysis was done using Swiss ADME and Osiris data warrior tool. Further, Toxicity of the title compound was predicted by using PKCSM online software.

A series of novel 10-phenylsulfonyl-2-substituted-4,10 dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-one derivatives obtained from N-sulfonation of 2-substituted-pyrimido[1,2-a]benzimidazol-4(10H)-ones and screened for for their in vitro anti-tuberculosis activities against Mycobacterium tuberculosis H37Rv by Microplate Alamar Blue Assay (MABA) method. The structures were established on the basis of their IR, ¹H-NMR, ¹³C-NMR, ESI-MS data and also the compound with 3f were crystallized and analysed by single crystal X-ray diffraction studies.

A series of novel 5-Bromo-3-iodo-1H-pyrazolo[3,4-b]pyridine linked various sulfonamide derivatives 8a-8j poly functionalized were designed and synthesized in moderate to good yield. A starting with iodination of 5-Bromo-1H-pyrazolo[3,4-b]pyridine 5 with iodine produced intermediate 5-Bromo-3-iodo-1H-pyrazolo[3,4-b]pyridine 6 with the reaction of various sulfonamide derivatives 7a-7j via copper catalyzed coupling reaction produced targeted compounds8a-8j. The isolated compounds were accepted by spectral and elemental analysis. The compounds 8a,8c,8d, and 8i were excellent active against Gram-positive and gram-negative bacterial strain compare to streptomycin standard drug. All synthesized compounds showed moderate to good antioxidant properties with used DPPH and Superoxide radical scavenging assay, Compounds 8c, 8g, and 8i exerted significant antioxidant scavenging activity for the DPPH radical.