Biochemical analysis of secondary metabolites of marine old-woman octopus Cistopus indicus (family Octopodidae) led to the identification of two sixteen-membered spiro-linked macrocyclic bislactones, named as cistobislactone A and cistobislactone B with unprecedented feature of henicos framework, based on extensive spectroscopic analyses. Cistobislactone B exhibited potential inhibition property against

Curcumin and cinnamaldehyde are natural products whose antineoplastic activity has been well explored in biological evaluations. However, their poor chemical stability under physiological conditions has been an obstacle to their use as therapeutic agents. Herein, we designed and synthesized two series of curcumin-cinnamaldehyde hybrids by removing reactive functionalities, including β-diketone and

The α-amylase is the main product of pancreas and is necessarily involved in the hydrolysis of carbohydrates into glucose so that it has been known to be a pioneer target for type 2 Diabetes mellitus (DM). Type 2 DM has no certain cure and the global increase in the cases of DM requires effective and extensive number of drug candidates. Drug discovery studies using organic biochemistry approaches are

Despite much research and undeniable advances, cancer treatment and prevention has remained a major challenge for scientists. Both genetic and epigenetic changes are involved in the growth and development of cancer complex and multifactorial disease. Among the possible treatment options, multidrug epigenetic therapy such as the use of dual epigenetic inhibitors, has been a popular option in recent

Phosphoryl prodrugs are key compounds in drug development. Biologically active phosphoryl compounds often have negative charges on the phosphoryl group, and as a result, frequently have poor pharmacokinetic (PK) profiles. The use of lipophilic moieties bonded to the phosphorus (or attached oxygen atoms) masks the negative charge of the phosphoryl group, and cleavage of the lipophilic moieties releases

Ovarian cancer is one of the main causes of women’s mortality worldwide. A variety of biological mechanisms are involved in ovarian cancer pathogenesis, including epigenetic alterations, mutations (especially in tumor suppressor genes), upregulated oncogenes, decreased apoptotic pathways, and dysregulation of other signaling pathways. Surgery and chemotherapy are two common approaches for treating

Chemical investigation of Phaeophytan marine macroalga Turbinaria ornata (family Sargassaceae) resulted in the characterization of three 2-furanone analogues, which were characterized as 6, 7-dihydroxy-8-methyl-3-(5′-methyloct-4′-en-1′-yl)-hexahydrocyclooct-1-en-[1, 2-c]furan-11-one (turbinafuranone A), 4-hydroxy-3-isopropyl-7, 8-dimethyl-6-(pentan-2′-acetate)-hexahydrocycloocta-1-en-[1, 2-c]furan-11-one

Neurolysin, a member of the metallopeptidase M3 family, plays an important role in many biological processes by regulating bioactive oligopeptides in the central nervous system and periphery. Small molecule modulators of neurolysin have therapeutic potential in the treatment of schizophrenia, addiction, epilepsy, Huntington, Parkinson’s, and Alzheimer’s diseases, and tumors. In this article, the structure

Increased bacterial resistance to antibiotics is a major threat to human health, and it is particularly important to develop novel antibiotic drugs. Here, we designed a series of Schiff base thiosemicarbazone derivatives containing an adamantane moiety, and carried out the structural characterization of the compounds and in vitro antibacterial activity tests. Compound 7e was as effective as the commonly

8-Nitro-1,3-benzothiazin-4-ones (BTZs), with BTZ043 and PBTZ169 as the most advanced compounds, represent a new class of potent antitubercular agents, which irreversibly inhibit decaprenylphosphoryl-β-d-ribose-2′-epimerase (DprE1), an enzyme crucial for cell wall synthesis in the pathogen Mycobacterium tuberculosis. Synthesis, structural characterization and in vitro testing against Mycobacterium aurum

We have previously reported a series of thiouracil analogs as bacterial SecA inhibitors. In this study, one potent thiouracil analog, SCA-15, was further evaluated for its inhibitory effects on SecA proteins and against strains of methicillin-resistant Staphylococcus aureus (MRSA) and Bacillus anthracis Sterne. SCA-15 inhibited the ion-channel activities of SecA1 with IC50 of 2.0–2.8 μM and the ATPase

Albumin is an abundant protein in nature with several biological functions. In the human body, both in health and in illness, its transport function is highlighted by the binding to medicinal drugs and consequent distribution in the bloodstream to the site of action. This is particularly relevant for anticancer treatments, since this protein accumulates in the tumor microenvironment to supply the energetic

Biochemical investigation of bioactive compounds from the marine demospongiae Clathria (Thalysias) vulpina (Lamarck, 1814) (family Microcionidae) resulted in the isolation of two previously undescribed 22-membered macrocyclic lactone derivatives clathrolide A and B from its organic extract. Structural elucidation of the compounds were carried out using spectroscopic analysis. Clathrolide A exhibited

Familial Alzheimer’s disease (FAD) is a rare early-onset genetic form of common dementia of old age. Striking in middle age, FAD is caused by missense mutations in three genes: APP (encoding the amyloid precursor protein) and PSEN1 and PSEN2 (encoding presenilin-1 and presenilin-2). APP is proteolytically processed successively by β-secretase and γ-secretase to produce the amyloid β-peptide (Aβ). Presenilin

In this study, 19 3H-benzo[f]chromen chalcone derivatives (2a–2s) were obtained from 2-hydroxy-1-naphthaldehyde as the starting material, and their structures were confirmed by IR, 1H NMR, 13C NMR, and ESI-MS analyses. The antidepressant activities of the compounds were evaluated in mice after one 30 mg/kg dose by means of forced swimming tests, and 18 of the compounds (2a–2l, 2n–2s) showed antidepressant

Increased infection spread is partly facilitated by reduced new drug development. Because of their antimicrobial properties, ferrocenyl chalcone derivatives were assessed in a previous study. However, dilutions of stock ferrocenyl chalcone solution with Mueller–Hinton broth (MHB) resulted in particle formation, and a colour change from deep red to dark-brown. Results of the current study confirmed

Two series of novel NLRP3 inflammasome inhibitors are designed, synthesized, and evaluated in an effort to develop diversified analogs based on the N-(phenylcarbamoyl)benzenesulfonamide scaffold. SAR studies reveal that the sulfonylurea linker can tolerate chemical modifications with either simply changing over the position of carbonyl and sulfonyl group or structurally flexibly inserting a cyclopropyl

α-Glucosidase is responsible for glucose release of oligosaccharides and disaccharides in the intestine and increase postprandial hyperglycemia. Inhibition of this enzyme is a beneficial therapeutic method for glycemic control in diabetes. This study deals with the design and synthesis of 4,5-diphenylimidazole-N-phenylacetamide derivatives 7a–l and the screen of these compounds for their potential

The natural product Ginkgolide B was used as a raw material and modified by esterification on C10-OH or C1-OH to obtain 11 derivatives (1–11), which were structurally characterized with nuclear magnetic resonance spectroscopy. An MTT assay-based in vitro tumor proliferation inhibitory activity test showed that compounds 2, 3, 6, 7, 10, and 11 exhibited strong inhibitory activity against the human ovarian