Obesity contributes to the genesis of many metabolic disorders including dyslipidemia, coronary heart disease (CHD), nonalcoholic fatty liver, type 2 diabetes, etc. Pancreatic lipase plays a vital role in food fat digestion and absorption. Therefore, to control obesity, inhibition of pancreatic lipase is the active therapy. Thus, novel natural product derived labdane appended triazoles with pancreatic lipase inhibition potential were designed and synthesized. Among these hybrids, and exhibited excellent inhibitory activity (IC 0.75 ± 0.02 μM and 0.77 ± 0.01 μM), slightly better than that of the positive control Orlistat (IC 0.8 ± 0.03 μM). Compounds ,, and - inhibited the PL comparable to that of positive control. Interestingly none of the compounds showed cytotoxicity (Hep G2) in the concentration range from 0.5 to 100 μM. Overall results reveal the potential of labdane appended triazoles as antiobesity agents.
A simple and efficient one-pot annulation of arylidenones, alkynes, and nitriles in the presence of BF·OEt is described. A highly functionalized variety of N-substituted pyridine-fused chromeno and pyrano derivatives were obtained with satisfactory yields under mild reaction conditions. The method was proven to be valid for the synthesis of a diverse library of chromeno[3,4-c]pyridines, thiochromeno[3,4-c]pyridines, pyrano[3,4-c]pyridines, and thiopyrano[3,4-c]pyridine derivatives from readily accessible substrates. This experimentally simple protocol provides structurally complex, biologically relevant heterocycles in a one-pot operation.
Heterocyclic compounds are an inevitable part of our life. These important classes of molecules have a wide range of applications starting from life-sustaining drugs to agrochemicals. Numerous methods, including metal...
Fully substituted pyrimidine synthesis accomplished from alkynes and nitriles via BF 3 . Et 2 O mediated [2 + 2 + 2] cycloaddition. The substrate scope of the reaction was broad to include terminal alkynes to internal alkynes and aromatic nitriles to aliphatic nitriles furnished good to acceptable chemical yields. The marine alkaloid, meridianin analogs were synthesized successfully by utilizing this protocol. The pyrimidine analogues were also screened for their broad spectrum of antibacterial property against ten bacteria. Among the derivatives, 2,4-dimethyl-6-p-tolylpyrimidine (3b) has shown excellent inhibition potential against most of the tested organisms with a range of 9 to 21 mm zone of inhibition.
The marine ecosystem is the less explored, biologically diverse, and vastest resource to discover novel antimicrobial agents. In recent decades' antimicrobial drugs are losing their effectiveness due to the growing resistance among pathogens, which causes diseases to have considerable death rates across the globe. Therefore, there is a need for the discovery of new antibacterials that can reach the market. There is a gradual growth of compounds from marine sources which are entering the clinical trials. Thus, the prominence of marine natural products in the field of drug design and discovery across the academia and pharmaceutical industry is gaining attention. Herein, the present review covers nearly 200 marine based antimicrobial agents of 11 structural classes discovered from the year 2010 to 2022. All the discussed compounds have exhibited medium to high antimicrobial activity in inhibiting various microorganisms.
A simple and efficient one-pot synthesis of N-substituted-1,2-dihydropyridines, indenopyridines and 5,6-dihydroisoquinolines by a BF·EtO mediated novel methodology, from easily available α,β-unsaturated ketones/arylidene ketones, phenyl acetylenes and substituted nitriles, has been described. This novel annulation provides quick access to complex polycyclic frameworks with an excellent substrate scope.
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