The reaction between different arylhydrazones and ninhydrin (= indene-1,2-3-trione) in acetonitrile at room temperature is described to produce novel bioactive 1-(3-chlorophenyl)indeno[1,2-c]pyrazol-4(1H)-one analouges. In evaluations of the ability to inhibit the growth of different human cell lines and some pathogenic bacterial strains in vitro, compounds 3c and 3f showed significant potency compared with the reference drugs. Both derivatives interacted well with the active site of the BRAF protein, according to molecular docking studies.

Novel polycyclic compounds, 1-pyrene-based pyridone derivatives, are synthesized by treatment of pyrenyl acetohydtazide with several arylidenemalononitriles and acetylacetone. Intramolecular cyclization furnishes the functionalized substituted pyridine-2-ones with high yields. Structures of the products are elucidated from the spectral data. Tests on antibacterial activity of the products reveal their high antibacterial effect.

A new series of novel substituted 3,4-dihydronaphthalene incorporated to benzo[h]quinoline, benzo[g]indazole, thiazolidin-4-one, pyrazolo[3,4-d]thiazol and thiazolo[4,5-b]pyridine ring systems were synthesized and evaluated for their cytotoxicity against selected human cancer cell lines. Some of the tested compounds exhibited promising carcinoma growth inhibition. The detailed synthesis, spectroscopic data and biological activities of the tested compounds were reported.

Some uracil- and thiouracil-5-sulfonohydrazide derivatives have been synthesized to be evaluated as antischistosomal agents. N-[2-(1,5-Dimethyl-3-oxo-2-phenylpyrazolin-4-yl)-4-oxo-1,3-thiazolidin-3-yl]-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-sulfonamide (3c) was formulated in jojoba oil and used to paint mice tails before infection with Schistosoma mansoni cercariae. Using Boc-Val-Leu-Gly-Arg-PNA, a specific substrate for trypsin-like serine proteinases, compound 3c inhibited cercarial serine protease activity with 50 % inhibition concentration (IC50) of 160 μg. Upon topical application on mice tails before infection with S. mansoni cercariae, it caused a 20 % reduction in worm burden compared with untreated infected mice. Using soluble crude cercarial antigen in enzyme-linked immunosorbent assay (ELISA), no significant changes were observed in the levels of immunoglobulin M (IgM) and IgG in sera from treated infected mice at 2, 4, and 6 weeks postinfection (WPI) compared with the level in sera from infected untreated mice. At 4 WPI, sera from treated infected mice showed significantly low (P < 0.05) IgM reactivity to crude soluble worm antigen compared with infected nontreated ones. IgG levels in sera from treated infected mice at 2 and 4 WPI were significantly lower (P < 0.05) than in sera from infected nontreated mice. At 6 WPI, the IgG response showed no significant differences in sera from both mice groups. Sera from treated infected mice at 2, 4, and 6 WPI had generally lower IgM reactivity to soluble egg antigen when compared with the level in sera from nontreated infected mice. At all time points postinfection, sera collected from treated infected mice showed significantly low IgG reactivity (P < 0.05) compared with infected nontreated mice.

Some N-p-substituted phenyl uracil-5-sulphonamide derivatives have been synthesized to be evaluated as molluscicides against Biomphalaria alexandrina snails, the intermediate host of Schistosoma mansoni. Schistosoma mansoni infected mice were treated with hemolymph obtained from pre-treated Biomphalaria alexandrina snails with the products 4a, 10a, 10b and 4b or obtained from non-treated snails. The selection of the concentration based on the predetermined dose which caused mortality of less than 50% of snails/24 h. LC50 of compounds 4a, 10a, 10b and 4b was 50, 100, 200 and 50 ppm respectively. The result showed that immunostimulatory effect of treated hemolymph with compounds 4a, 10a and 4b was related to significant protective effects (44.4, 34.6 and 50.4% reduction in worm burden respectively). In addition, mean total worm burdens were significantly reduced in non treated hemolymph by 33.8%. The effect of hemolymph obtained from treated or non treated snails on S. mansoni adult worms antigens was studied by indirect immunofluorescence technique using chronic mouse sera (CMS). The results indicated that there was a strong reaction with epitopes in gut epithelium, tubercles, teigument and subtegumental musculature of untreated and treated S.mansoni adult worms antigens. Therefore, treatment of hemolymph obtained from pre-treated snails with compounds 4a, 10a, and 4b can stimulate specific immune response and induce protective effects against S. mansoni infection.