Synthesis, Molecular Docking and Pharmacological Investigation of Heterocyclic Amine Derivatives as Potential Anticancer Agents

Cancer is life threatening disease that causes great damage to health worldwide. Studies shown that hypoxia is the major contributor to tumor and cancer development due to overexpression of carbonic anhydrase. To encounter such cells abnormalities, demanding new drugs or novel analogs of currently in use. Therefore, the search for new pharmacoactive moieties with considerable effective activity against such tumors and cancers is needed. The implication of heterocyclic amine and acetamide derivatives well known as chemotherapeutic agents. Heterocyclic amine morpholine was taken as principal products and its new derivatives were synthesized after being designed computationally via molecular docking. A series of some of its new synthetic analogs i.e heterocyclic amine derivatives 1(a-o) were successfully synthesized and screened for their anticancer and carbonic anhydrase inhibitory potential. Most of the compounds showed good results possessing reasonable carbonic anhydrase inhibitory activity particularly compounds 1c, 1d, 1h and 1i showed very reasonable carbonic anhydrase inhibitory activity whereas compound 1h showed maximum inhibition comparable to acetazolamide. Similarly, four of the synthesized compounds showed good anticancer activity particularly compound 1b, 1c, 1h, and 1i showed reasonable, whereas compound 1h have better IC50 value comparable to cisplatin when evaluated via in vitro MTT assay.

Antioxidant activity of heterocyclic amino containing derivatives of naphthoquinone and their compositions with surface-active rhamnolipids

Composite preparations based on heterocyclic amine-containing naphthoquinone derivatives and surfactant rhamnolipids were obtained. The intensity of the processes of lipid peroxidation (LPO), oxidative modification of proteins (OMB) and radical-absorbing activity against 1,1-diphenyl-2-picrylhydrazyl (DFPG) was studied. Compounds exhibiting high antioxidant activity against LPO and OMB processes were identified, namely: 2-[(6-(4-fluorophenyl-5-oxo-2,5-dihydro-1,2,4-triazin-3-yl) phenyl)amino]naphthalene-1,4-dione 1d and its composite preparation with rhamnolipid 1d + RL. It was found that all synthesized compounds show antioxidant activity in LPO processes.

Heterocyclic Amine-Induced Feeding Deterrence and Antennal Response of Honey Bees

The productivity and survival of managed honey bee colonies is negatively impacted by a diverse array of interacting factors, including exposure to agrochemicals, such as pesticides. This study investigated the use of volatile heterocyclic amine (HCA) compounds as potential short-term repellents that could be employed as feeding deterrents to reduce the exposure of bees to pesticide-treated plants. Parent and substituted HCAs were screened for efficacy relative to the repellent N,N-diethyl-meta-toluamide (DEET) in laboratory and field experiments. Additionally, electroantennogram (EAG) recordings were conducted to determine the level of antennal response in bees. In video-tracking recordings, bees were observed to spend significantly less time with an HCA-treated food source than an untreated source. In a high-tunnel experiment, the HCA piperidine was incorporated in a feeding station and found to significantly reduce bee visitations relative to an untreated feeder. In field experiments, bee visitations were significantly reduced on melon flowers (Cucumis melo L.) and flowering knapweed (Centaurea stoebe L.) that were sprayed with a piperidine solution, relative to untreated plants. In EAG recordings, the HCAs elicited antennal responses that were significantly different from control or vehicle responses. Overall, this study provides evidence that HCAs can deter individual bees from food sources and suggests that this deterrence is the result of antennal olfactory detection. These findings warrant further study into structure–activity relationships that could lead to the development of short-term repellent compounds that are effective deterrents to reduce the contact of bees to pesticide-treated plants.

Using Adinandra nitida leaf extract to prevent heterocyclic amine formation in fried chicken patties

Adinandra nitida leaf extract, rich in polyphenols and flavonoids, can effectively prevent the formation of heterocyclic amines in fried chicken patties.