Synthesis, characterization and evaluation of antidiabetic activity of novel indoline derivatives

Manoharan, Dhineshkumar; Kulanthai, Kannan; Gnanavel, S.; Raji, Vijayan; Palvannan, Thayumanavan

doi:10.3329/bjp.v12i2.30872

Cited by 6 publications

(3 citation statements)

References 16 publications

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“…Furthermore, nitro group in compound 15 was reduced following the reported procedure 35 . Compound 16 served as crucial starting material to obtain compounds 17a-j , where it reacted with the respective isocyanate in THF 36 . The urea derivatives 17a-j were obtained in good yield and purity.…”

Section: Resultsmentioning

confidence: 99%

Design, molecular modelling and synthesis of novel benzothiazole derivatives as BCL-2 inhibitors

Ismail,

Khalil,

Taha

et al. 2023

Sci Rep

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Apoptosis plays a crucial role in cancer pathogenesis and drug resistance. BCL-2 family of enzymes is considered as one of the key enzymes which is involved in apoptosis. When there is disruption in the balance between anti-apoptotic and pro-apoptotic members of the BCL-2 family apoptosis is dysregulated in the affected cells. Herein, 33 novel benzothiazole-based molecules 7a-i, 8a-f, 9a-b, 12a-e, 13a-d, 14a,b, and 17a-j were designed, synthesized and tested for their BCL-2 inhibitory activity. Scaffold hopping strategy was applied in designing of the target compounds. Compounds 13c and 13d showed the highest activity with IC50 values equal to 0.471 and 0.363 µM, respectively. Molecular docking studies of the synthesized compounds showed comparable binding interactions with the lead compound. Structure activity relationship study was performed to show the effects of structural modifications on the inhibitory activities on BCL-2.

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Section: Resultsmentioning

confidence: 99%

Design, molecular modelling and synthesis of novel benzothiazole derivatives as BCL-2 inhibitors

Ismail,

Khalil,

Taha

et al. 2023

Sci Rep

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“…[54] In the same way, indoline derivatives are also effective antidiabetic compounds, which have been identified in the sample of R. hastatus. [55] The Momordica charantia (bitter gourd) has been demonstrated with significant antidiabetic activity and it has been reported with high percentage of Nerolidol. [56] The GC (FID-MS) analysis of R. hastatus also reveals the presence of fatty acids, i.e., Myristic acid and palmitic acid and GPR-40 "fatty acid receptors" have been identified on the B-cells of pancrease that are responsible for insulin secretion.…”

Section: Discussionmentioning

confidence: 99%

Nutritional and medicinal aspects of Rumex hastatus D. Don along with in vitro anti-diabetic activity

Ahmad

Ullah

Ayaz

et al. 2019

International Journal of Food Properties

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Rumex hastatus being used for medicinal and nutritional purposes as a functional food in various countries is hereby evaluated by the gas chromatography-mass spectroscopy, proximate analysis, physicochemical (fluorescence) analysis, quantitative analysis of secondary metabolites and sensory evaluations studies. Various samples of R. hastatus were also evaluated for in vitro anti-diabetic potential. The investigational study demonstrated that R. hastatus is a rich source of carbohydrate, i.e., 432.4 mg/g. Moisture content, protein, fiber, ash content and fats were recorded as 22.8%, 133.9 mg/g, 124.4 mg/g, 54.5 mg/g and 25.6 mg/g, respectively. In the same way, the secondary metabolite displayed a relatively greater amount of flavonoids (84.5 mg/g) followed by saponins (65.5 mg/g) and alkaloids (49.5 mg/g). Similarly, the GC (FID-MS) analysis of R. hastatus revealed the detection of 120 compounds. Out of those identified compounds, selected anti-diabetic compounds were sorted out, viz butyl phthalate, phytol, ethylthreonine, dihydrobenzofuran, indoline, guanidine, nerolidol, myristic acid, palmitic acid, caryophyllene, anozol. In physicochemical fluorescence analysis and the sensory evaluation, data were also recorded along with the anti-diabetic with IC 50 value of 42.09 µg/ml. The overall investigational analysis of R. hastatus obviously demonstrated that this plant was a rich source of primary and secondary metabolites. It may be concluded from the GC (FID-MS) analysis that R. hastatus is a potential source of anti-diabetic constituents, which may confer hypoglycemic potential. Based on the recorded data it may also be inferred that R. hastatus is among safe and nutritious herbs, which can be used in lieu of green vegetables and functional food with anti-diabetic potential. ARTICLE HISTORYdifference is that each plant species differs in the amount and concentration of these substances. The plants rich in primary metabolites are usually used for nutritional purposes, while secondary metabolites are preferred for medicinal purposes. [6,11,12] The plants may possess fats, protein, carbohydrates, vitamins and minerals in such quantity that are considered sufficient for our daily requirements. One can use specific species of plant as food that possess required amount of primary metabolites and low amount of secondary metabolites. But the plants that possess high amount of secondary metabolites than the primary metabolites can cause serious health complications. [13,14] So this is necessary to figure out the amount of nutritional and medicinal elements in those plants, which are being used as food by people.The nutritional values of various plants have been reported by different investigators. [15,16] Diabetes mellitus is a metabolic disorder characterized by increase in blood glucose level. It can affect individuals at any stage of life but the frequency of diabetes is considerably high among the obese and aged people. [17] Various therapeutic measures are employed to alleviate the symptoms of this disease. One of t...

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“…[11] Furthermore, the antidiabetic activity of synthesized N-(4-aminophenyl)indoline-1carbothiamides) (281) was examined using standard -amylase inhibition assay method. [117] R (280) (281)…”

Section: Antidiabeticmentioning

confidence: 99%

Indoline-based heterocyclic scaffold: Synthetic methods, chemical reactions and biological prospect

Sharafeldin

2020

Egypt. J. Chem.

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Indolines are significant compounds because of their diversity of applications in synthetic organic chemistry, pharmaceutical, industrial chemistry as well as they are present in several biologically active compounds in both natural and synthetic origins. Recently,there are high expectations that they exhibit interesting applications in selective potentiate the activity of β-lactam antibiotics in MRSA as well as other pharmacological arena, such as anticancer, anti-inflammatory, antioxidant, anticoagulant agents, etc. Furthermore, they are considered as considerable compounds due to their widespread use as building blocks and as chiral support in asymmetric synthesis. As a result, a new trends for the indoline-based nucleus in medicinal chemistry studies require to be reviewed especially many reports have been suggested that the indoline-based compounds have a very high therapeutic value (in MRSA) and needs to be explored for further studies. So, this review deals with the main innovations regarding indoline-based heterocycle scaffold stressing on their synthesis, reactions and their pharmacological activities.

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Synthesis, characterization and evaluation of antidiabetic activity of novel indoline derivatives

Cited by 6 publications

References 16 publications

Design, molecular modelling and synthesis of novel benzothiazole derivatives as BCL-2 inhibitors

Design, molecular modelling and synthesis of novel benzothiazole derivatives as BCL-2 inhibitors

Nutritional and medicinal aspects of Rumex hastatus D. Don along with in vitro anti-diabetic activity

Indoline-based heterocyclic scaffold: Synthetic methods, chemical reactions and biological prospect

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