Akbar Idhayadhulla

Synthesis of new morpholine-connected pyrazolidine derivatives and their antimicrobial, antioxidant, and cytotoxic activities.

A simple and convenient one-pot four-component synthesis of morpholine-connected pyrazolidine derivatives 2a-f and 4a-f was developed using direct metal-free catalysis, with the identities of the synthesized compounds confirmed by IR, NMR (1H and 13C), mass spectrometry, and elemental analysis. The prepared compounds were inspected for antimicrobial, antioxidant, and cytotoxic activities. Antimicrobial and antifungal activities against five bacterial and four fungal pathogens, respectively, were investigated using the disc diffusion technique. In antibacterial activity, compounds 2d and 2f (MIC=2μg/mL) exhibited significantly higher activity than the standard ciprofloxacin. The results of antifungal assay showed that the activity of compound 4a (MIC=0.5μg/mL) was significantly higher than the standard clotrimazole. Antioxidant activity was screened based on ABTS+ radical scavenging and linoleic acid peroxidation performance. Compound 4a showed substantial antioxidant (91.3%) activities, as compared with the Trolox standard. Cytotoxicity was evaluated using HepG2 (liver), HeLa (cervical), and MCF-7 (breast) cancer cell lines, with high toxicities observed for 2b (GI50=12.2μm) and 4a (GI50=07.8μm).

Evaluation of antioxidant and anticancer activities of chemical constituents of the Saururus chinensis root extracts

Evaluation of antioxidant and anticancer activities were screened by various Saururus chinensis root extracts. Four solvents (ethyl acetate, methanol, ethanol, and water) extracts were investigated for their total flavonoids, phenol contents and their antioxidant activity of DPPH (2,2-diphenyl-1-picrylhydrazyl), NO (nitric oxide), H2O2 (hydrogen peroxide), ABTS 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonicacid)diammonium assays, FRAP (ferric reducing ability of plasma) assays and anticancer activity. The total phenolic and flavonoid content of extracts were determined by using FC (Folin–Ciocalteu) and AlCl3 colorimetric assay method. Total flavonoid content in these plants ranged from 24.7 to 72.1 mg g−1 and amount of free phenolic compounds was between 11.2 and 67.1 mg g−1 extract. The all extracts have significant levels of phenolics and flavonoids content. Anticancer activity was screened for MCF-7 breast cancer cell line. Ethanol extract shows significant of antioxidant activity and water extract shows significant of anticancer activity compared with standard (BHT) butylated hydroxy toluene. These ethanol and water extracts could be considered as a natural source for using antioxidant, and anticancer agents compared to commercial available synthetic drugs.

Synthesis of Some 2-Thioxo-imidazolidin-4-one Derivatives and its Antimicrobial Activity

Series of newly prepared 3-{[2,6-bis(4-substituted phenyl)-1- methylpiperidin-4- ylidene] amino}- 2-thioxo-imidazolidin-4-one derivatives (3a-3f) have been synthesized by the cyclization of compound (2a-2f), ethyl chloro acetate and fused sodium acetate. The chemical structures were confirmed by IR, 1H NMR and elemental analysis. The synthesized compounds were screened for their antimicrobial activity against four antibacterial and four antifungal organisms.

Effective synthesis of some novel pyrazolidine-3,5-dione derivatives via Mg(II) catalyzed in water medium and their anticancer and antimicrobial activities

Novel pyrazolidine-3,5-dione derivatives (2a–g, 4a–g, and 6a–g) were synthesized by an easy-to-perform Mg(II) acetylacetonate-catalyzed reaction with high yields using water as the reaction medium. Synthesized compounds were screened for anticancer and antimicrobial activities. The compound 6c (LD50 19.1xa0µg/mL) showed anticancer activity higher than that of all other compounds against MCF-7 breast cancer cell line. Results of antimicrobial activities revealed that the compound 4d (MIC 0.5xa0μg/mL) had higher activity than ciprofloxacin against Staphylococcus aureus, whereas the compound 2b (MIC 0.5xa0μg/mL) had higher activity than clotrimazole against Candida albicans. Overall results of this study envisaged that the compounds 2b, 4d, and 6c have the potential to be developed as anticancer and antimicrobial agents.Graphical abstractNovel pyrazolidine-3,5-dione derivatives (2a–g, 4a–g, and 6a–g) were synthesized via an easy-to perform Mg(II) catalysis in water medium. The synthesized compounds were screened for anticancer and antimicrobial activities.

Cytotoxic, larvicidal, nematicidal, and antifeedant activities of piperidin-connected 2-thioxoimidazolidin-4-one derivatives

The objective of this study was to investigate brine shrimp cytotoxicity, larvicidal, nematicidal, and antifeedant activities of novel piperidin-connected 2-thioxo-imidazolidin-4-one derivatives. The activities of target compounds were compared with some naturally occurring (−)-pinidinol, hydantocidin, and positive controls. Target compounds were synthesized via cyclocondensation method. The compounds were synthesized and then characterized by infrared spectroscopy, 1H NMR, 13C NMR, mass spectral, and elemental analyses. Brine shrimp cytotoxicity assay was investigated using freshly hatched, free-swimming nauplii of Artemiasalina. Larvicidal screening was performed against urban mosquito larvae (Culex quinquefasciatus). Nematicidal activity was evaluated using juvenile nematodes of Meloidogyne javanica. Regarding antifeedant activity, marine-acclimated Oreochromis mossambicus fingerlings were used. Compounds 3a-c (piperidin-connected 2-thioxoimidazolidin-4-one) were found to be lethal to the second instar larvae of mosquito, which produced LD50 values of 1.37, 6.66, 6.51u202fμg/mL, compared to compounds (−) pinidinol and hyantocidin LD50 values of 18.28 and 22.11u202fμg/mL respectively. Compound 3a-c was found to kill 100% of fish fingerlings within 6u202fh at 20u202fµg/mL, with LD50 values of 1.54, 1.79, 1.52u202fµg/mL, compared to compounds (−) pinidinol and hyantocidin with LD50 values of 10.21 and 21.05u202fμg/mL respectively. Compound 3c with LD50 value of 1.57u202fμg/mL demonstrated high nematicidal activity compared to compound 3a, 3b, (−) Pinidinol and Hyantocidin LD50 values of 6.45, 2.42, 14.25, 26.30u202fμg/mL respectively. Therefore, the 2-thioxoimidazolidin-4-one with piperidin ring showed high potential cytotoxic, larvicidal, nematicidal, and antifeedent activities.

Environmental biotoxicity screening of some pyrrole and 1,4- dihydropyridine heterocyclic derivatives

The nematicide and larvicidal use is slate for reduction due to environmental problems, human and animal health concerns. For example, effective nematicides such as dibromochloropropane (DBCP) and ethylenedibromide (EDB) have been withdrawn from the market due to their deleterious effects on humans and the environment. According to World Health Organization (WHO), the one of strategies is to destroy their vectors or intermediate hosts. The best method is control of mosquito larvae using insecticides (Sun