scholarly journals Synthesis, Characterization and Evaluation of Antidiabetic Activity of Novel Pyrazoline Fused Indole Derivatives

2021 ◽  
pp. 276-292
Author(s):  
Nagesh Vaddiraju ◽  
M. Ajitha ◽  
K. Rajnarayana
Keyword(s):  
Research Work ◽  
Biological Evaluation ◽  
Antidiabetic Activity ◽  
Dimethyl Formamide ◽  
Indole Derivatives ◽  
Standard Drug ◽  
Chemical Structures ◽  
Frame Work

The primary purpose of this research work is to synthesize, characterize and biological evaluation of novel pyrazoline fused indole derivatives lead to creating a new molecular frame work. Methodology: In the present study, the new series of novel pyrazoline fused indole derivatives were synthesized from from indole and substituted acetophenone by the 4 step process. In the first step indole and dimethyl formamide were coupled by using phosphorous oxychloride and NaOH to prepare the compound 1 Indole-3-aldehyde. In the second step compound 1 was condensed with substituted aetophenone to synthesis the compound 2 chalcones (a-h). In the third step chalcones 2(a-h) were coupled with semicarbazide or thiosemicarbazide to synthesis the compound 3(a-p). In the final step compound 3(a-p) were coupled with indole-3-aldehyde to prepare the final product of R-substitutedN-((1H-indol-3-yl)methylene)-5-(1H-indol-3-yl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carboxamide and R-substitutedN-((1H-indol-3-yl)methylene)-5-(1H-indol-3-yl)-3-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide 4(a-p). Results: The chemical structures of the synthesized compounds were characterized by means of IR, Mass and NMR spectroscopy. The compounds were screened for anti-diabetic activity by In-vitro and In-vivo methods. In In-vivo method 4a, 4m have exhibited moderate anti-diabetic activity as that of standard drug, glibenclamide. In In-vitro method 4a, 4e & 4m have shows moderate anti-diabetic activity as that of reference standard, acarbose. Conclusion: The synthesized novel pyrazoline fused indole derivatives have moderate antidiabetic activity as that of standard drug by In-vitro and In-vivo methods. These compounds can be further exploited to get the potent lead compound.

Novel Phytochemical Constituents and their Potential to Manage Diabetes

2020 ◽  
Vol 26 ◽  
Author(s):  
Shaik Ibrahim Khalivulla ◽  
Arifullah Mohammed ◽  
Kokkanti Mallikarjuna
Keyword(s):  
Natural Products ◽  
Large Population ◽  
World Health ◽  
In Vivo Studies ◽  
Antidiabetic Activity ◽  
Therapeutic Drug ◽  
Pharmacological Activities ◽  
Chemical Structures

Background: Diabetes is a chronic disease affecting a large population worldwide and stands as one of the major global health challenges to be tackled. According to World Health Organization, about 400 million are having diabetes worldwide and it is the seventh leading cause of deaths in 2016. Plant based natural products had been in use from ancient time as ethnomedicine for the treatment of several diseases including diabetes. As a result of that, there are several reports on plant based natural products displaying antidiabetic activity. In the current review, such antidiabetic potential compounds reported from all plant sources along with their chemical structures are collected, presented and discussed. This kind of reports are essential to pool the available information to one source followed by statistical analysis and screening to check the efficacy of all known compounds in a comparative sense. This kind of analysis can give rise to few numbers of potential compounds from hundreds, whom can further be screened through in vitro and in vivo studies, and human trails leading to the drug development. Methods: Phytochemicals along with their potential antidiabetic property were classified according to their basic chemical skeleton. The chemical structures of all the compounds with antidiabetic activities were elucidated in the present review. In addition to this, the distribution and their other remarkable pharmacological activities of each species is also included. Results: The scrutiny of literature led to identification of 44 plants with antidiabetic compounds (70) and other pharmacological activities. For the sake of information, the distribution of each species in the world is given. Many plant derivatives may exert antidiabetic properties by improving or mimicking the insulin production or action. Different classes of compounds including sulfur compounds (1-4), alkaloids (5-11), phenolic compounds (12-17), tannins (18-23), phenylpropanoids (24-27), xanthanoids (28-31), amino acid (32), stilbenoid (33), benzofuran (34), coumarin (35), flavonoids (36-49) and terpenoids (50-70) were found to be active potential compounds for antidiabetic activity. Of the 70 listed compounds, majorly 17 compounds are from triterpenoids, 13 flavonoids and 7 are from alkaloids. Among all the 44 plant species, maximum number (7) of compounds are reported from Lagerstroemia speciosa followed by Momordica charantia (6) and S. oblonga with 5 compounds. Conclusion: This is the first paper to summarize the established chemical structures of phytochemicals that have been successfully screened for antidiabetic potential and their mechanisms of inhibition. The reported compounds could be considered as potential lead molecules for the treatment of type-2 diabetes. Further, molecular and clinical trials are required to select and establish the therapeutic drug candidates.

scholarly journals Synthesis and biological evaluation of some novel pyrazolopyrimidines incorporating a benzothiazole ring system

2013 ◽  
Vol 63 (1) ◽  
pp. 19-30 ◽  
Author(s):  
Mohammed Afzal Azam ◽  
Loganathan Dharanya ◽  
Charu Chandrakant Mehta ◽  
Sumit Sachdeva
Keyword(s):  
Antimicrobial Activity ◽  
Diclofenac Sodium ◽  
Biological Evaluation ◽  
Ring System ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Pyrimidine Moiety ◽  
Synthesis And Biological Evaluation

In the present study, a series of benzothiazol derivatives 3a-l containing pyrazolo[3,4-d]pyrimidine moiety at the second position were synthesized and characterized by analytical and spectral data. The compounds were tested for their in vitro antimicrobial activity. Compounds 1-(1,3-benzothiazol-2- yl)-3-methyl-4-phenyl-1H-pyrazolo[3,4-d]pyrimidine (3a), 1- (1,3-benzothiazol-2-yl)-4-(4-chlorophenyl)-3-methyl-1H-pyrazolo[ 3,4-d]pyrimidine (3d) and 1-(1,3-benzothiazol-2-yl)- 3-methyl-4-substituted phenyl-1H-pyrazolo[3,4-d]pyrimidines (3h-j) showed significant inhibitory activity against P. aeruginosa whereas compounds 1-(1,3-benzothiazol-2-yl)-4- (2-chlorophenyl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3b), 2-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin- 4-yl]phenol (3e), 1-(1,3-benzothiazol-2-yl)-4-(3,4-dimethoxyphenyl)- 3-methyl-1H-pyrazolo[3,4-d]pyrimidine (3h), 4-[1-(1,3-benzothiazol-2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyri midin-4-yl]-N,N-dimethylaniline (3j) and 1-(1,3-benzothiazol- 2-yl)-3-methyl-4-[2-phenylvinyl]-1H-pyrazolo[3,4-d]pyrimidine (3k) were found to be active against C. albicans. Some of these synthesized compounds were evaluated for their in vivo acute toxicity, analgesic, anti-inflammatory, and ulcerogenic actions. The tested compound 4-[1-(1,3-benzothiazol- 2-yl)-3-methyl-1H-pyrazolo[3,4-d]pyrimidin-4-yl]-N, N-dimethylaniline (3j) exhibited maximum analgesic and anti-inflammatory activities. Compounds 1-(1,3-benzothiazol- -2-yl)-3-methyl-4-(3-nitrophenyl)-1H-pyrazolo[3,4-d]pyrimidine (3i) and 3j showed a significant gastrointestinal protection compared to the standard drug diclofenac sodium.

Synthesis and studies of thiazolidinedione–isatin hybrids as α-glucosidase inhibitors for management of diabetes

2021 ◽  
Vol 13 (5) ◽  
pp. 457-485
Author(s):  
Ramandeep Kaur ◽  
Rajnish Kumar ◽  
Nilambra Dogra ◽  
Ashok Kumar ◽  
Ashok Kumar Yadav ◽  
...  
Keyword(s):  
In Silico ◽  
Binding Free Energy ◽  
Biological Evaluation ◽  
Free Energy Calculations ◽  
Standard Drug ◽  
Glucosidase Inhibitors ◽  
Cytotoxicity Studies ◽  
Cytotoxicity Assessment

Aim: Keeping in view the side effects associated with clinically used α-glucosidase inhibitors, novel thiazolidinedione–isatin hybrids were synthesized and evaluated by in vitro, in vivo and in silico procedures. Materials & methods: Biological evaluation, cytotoxicity assessment, molecular docking, binding free energy calculations and molecular dynamics studies were performed for hybrids. Results: The most potent inhibitor A-10 (IC50 = 24.73 ± 0.93 μM) was competitive in manner and observed as non-cytotoxic. A-10 possessed higher efficacy than the standard drug (acarbose) during in vivo biological testing. Conclusion: The enzyme inhibitory potential and safety profile of synthetic molecules was recognized after in vitro, in vivo, in silico and cytotoxicity studies. Further structural optimization of A-10 can offer potential hit molecules suitable for future investigations.

Formulation, Optimization, in Vitro and in Vivo Investigation of Ketoprofen - Fumaric Acid Co-crystal for the Solubility Enhancement of Ketoprofen

2021 ◽  
Author(s):  
Meenakshi Bhatia ◽  
Ashwani Kumar ◽  
Vikas Verma ◽  
Snehlata Yadav ◽  
SUNITA DEVI
Keyword(s):  
Fumaric Acid ◽  
Protein Denaturation ◽  
Research Work ◽  
Molar Ratio ◽  
Scanning Calorimetry ◽  
Standard Drug ◽  
Anti Inflammatory ◽  
Analgesic Activities

Abstract The present piece of research work is framed as improving the solubility of ketoprofen by forming co-crystal using fumaric acid as a coformer. Co-crystal of ketoprofen and fumaric acid were prepared by simple solvent assisted grinding. The independent variables i.e. drug and coformer were mixed in 1:1 molar ratio and dependent variables were assumed to be solubility and % drug release. Differential scanning calorimetry, fourier transform infrared spectroscopy, X-ray diffraction, nuclear magnetic resonance and scanning electron microscopy techniques were used to characterize the preparation of optimized batch of co-crystal and further, evaluated for in-vitro and in-vivo anti-inflammatory and analgesic activities. Based on results of solubility and dissolution rate studies the drug showed 4-5 fold improvement in both the properties on co-crystallisation. The values of Gibbs free energy are negative at all levels of carrier demonstrating spontaneity of drug solubilization process. The IC50 value of optimized batch of co-crystal formulation and pure drug was observed as 327.33 µg/ml and 556.11 µg/ml, respectively, demonstrating that co-crystal formulation possesses more percentage protection against protein denaturation than the drug ketoprofen. In-vivo (anti-inflammatory and analgesic) activities revealed that optimized batch of co-crystal formulation delivered a rapid pharmacological response in wistar rats and albino mice when compared with standard drug.

Construction of C-glycosides of heterocycles containing the pyrimidin-2-amine or the 1H-pyrazolo[3,4-b]pyridine moiety and their biological evaluation for anticancer activities

2019 ◽  
Vol 43 (3-4) ◽  
pp. 152-157
Author(s):  
Wu-Wu Li ◽  
Min-Yan Zheng ◽  
Ying Guo ◽  
Zun-Ting Zhang ◽  
Ji-Chang Han ◽  
...  
Keyword(s):  
High Resolution Mass Spectrometry ◽  
Positive Control ◽  
Biological Evaluation ◽  
Human Leukemia ◽  
Anticancer Activities ◽  
Standard Drug ◽  
Chemical Structures ◽  
Pyridine Moiety ◽  
Heterocyclic Derivatives

A series of novel C-glycosides of heterocyclic derivatives containing a pyrimidin-2-amine or a 1 H-pyrazolo[3,4- b]pyridine moiety were synthesized using condensation reactions of the substituted puerarin with guanidine or 3-amino-5-hydroxypyrazole in methyl alcohol. Their chemical structures were characterized by Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and high-resolution mass spectrometry. In addition, their biological activity has been demonstrated by in vitro evaluation against the human leukemia cells K562 and human prostate cancer cells PC-3 by MTT-based assays, using the commercially available standard drug of cis-platin as a positive control. The results also demonstrated that most of the compounds showed considerable cytotoxicity to these two cell lines of K562 and PC-3, and indicated that novel C-glycosides of heterocyclic derivatives may be potential leads for further biological screenings and may generate drug-like molecules.

scholarly journals Design and Synthesis of 2-Mercapto Benzoxazole coupled Benzyl Triazoles as Anti-inflammatory Agents Targeting COX-2 Enzyme

2020 ◽  
Vol 32 (12) ◽  
pp. 3209-3218
Author(s):  
K. Praveen Kumar ◽  
Y. Prashanthi ◽  
G. Rambabu ◽  
Md. Ataur Rahman ◽  
J.S. Yadav
Keyword(s):  
Chemical Space ◽  
Biological Evaluation ◽  
Inflammatory Activity ◽  
Design Synthesis ◽  
Standard Drug ◽  
Design And Synthesis ◽  
Cox 2 ◽  
Anti Inflammatory

In this study, we report the design, synthesis and the biological evaluation of 19 analogues of 2-mercapto benzoxazole coupled benzyl triazoles (BOTs) based on analysis of the binding site and literature of chemical space. These BOTs were evaluated both in vitro and in vivo for their anti-inflammatory activity. Eleven compounds showed less than 10 μM in vitro COX-2 enzyme activities. The most potent analogue among the BOT analogues were BOT15, BOT3 and BOT19 with IC50 3.40 μM, 4.50 μM and 4.57 μM respectively against COX-2. The in vivo anti-inflammatory activity of two BOTs has significantly higher than that of standard drug, ibuprofen. 2-Mercapto benzoxazole coupled benzyl triazoles (BOTs) were also tested for their antioxidant capacity and proved to be an as active scavenger, better than ascorbic acid.

A Review on Phytochemistry, Pharmacological Action, Ethanobotanical Uses and Nutritional Potential of Kedrostis foetidissima (Jacq.) Cogn.,

2020 ◽  
Vol 18 (1) ◽  
pp. 5-20 ◽  
Author(s):  
Kalaiseziyen Pavithra ◽  
Ganapathy Saravanan
Keyword(s):  
Biological Activities ◽  
Research Work ◽  
Pharmacological Action ◽  
Biologically Active ◽  
In Vivo Studies ◽  
Traditional Medicines ◽  
Chemical Structures ◽  
Medicinal Properties

Nature is an amazing source for food, shelter, clothing and medicine. An impressive number of modern drugs are isolated from many sources like plants, animals and microbes. The development of natural products from traditional medicines is of great importance to society. Modern concepts and methodologies with abundant clinical studies, unique diversity of chemical structures and biological activities aid the modern drug discovery process. Kedrostis foetidissima (Jacq.) Cogn., a traditional medicinal plant of the Cucurbitaceae family, is found in India, Sri Lanka, Ethiopia and Western Malaysia. Almost all parts of the plant are used in traditional systems of medicines and reported having medicinal properties in both in vitro and in vivo studies. In the last few years, extensive research work had been carried out using extracts and isolated phytoconstituents from Kedrostis foetidissima to confirm its pharmacology and biological activities. Many scientific reports show that crude extracts and extensive numbers of phytochemical constituents isolated from Kedrostis foetidissima have activities like antimicrobial, antioxidant, anticancer, gastroprotective, anti-inflammatory and various other important medicinal properties. The therapeutic properties of the plants are mainly attributed to the existence of phytoconstituents like phenols, alkaloids, flavonoids, tannins, terpenoids and steroids. This comprehensive review in various aspects gave a brief overview of phytoconstituents, nutritional values and medicinal property of the plant and might attract the researchers to explore its medicinal activity by discovering novel biologically active compounds that can serve as a lead compound in pharmaceutical and food industry.

Synthesis and Biological Evaluation of 6-Substituted Mangiferin Derivatives as Antioxidant and Anticancer agents

2021 ◽  
Vol 18 ◽  
Author(s):  
Mohan H. Patil ◽  
Uma D. Kabra ◽  
Krishna R. Gupta ◽  
Milind J. Umekar
Keyword(s):  
Antioxidant Activity ◽  
Anticancer Agents ◽  
Biological Evaluation ◽  
Anticancer Activities ◽  
Standard Drug ◽  
Chemical Structures ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of ◽  
Better Than

: Esterified and alkyl amine derivatives of mangiferin were synthesized and evaluated for in vitro antioxidant and anticancer activities. The chemical structures of the derivatives were confirmed using elemental analysis and spectral data.The antioxidant activity was assessed using 2,2-diphenyl-1-picrylhydrazy (DPHH) assay and some derivatives displayed antioxidant activity better than mangiferin and standard drug ascorbic acid. Among the synthesized derivatives, few exhibited enhanced anticancer activity against human breast (MDA-MB-231) cancer cell lines, then the parent mangiferin.

scholarly journals Pharmacological Modeling and Study for Antidiabetic Activity of Praecitrullus fistulosus Leaves Extracts

2020 ◽  
Vol 10 (4-s) ◽  
pp. 13-16
Author(s):  
Ashutosh Tiwari ◽  
C.K Tyagi ◽  
Harish Pandey ◽  
Sunil Kumar Shah
Keyword(s):  
Research Work ◽  
Ethanol Extract ◽  
Extraction Methods ◽  
Water Soluble ◽  
Antidiabetic Activity ◽  
In Vivo Models ◽  
Successive Extraction ◽  
Praecitrullus Fistulosus

Phytochemical and pharmacological investigations of leaves of Praecitrullus fistulosus for the antidiabetic activity have been done in our research work encompassed in depth and systematic screening of plant leaves and further extraction, characterization and bioevaluation. The research was envisaged for antidiabetic activity of different extracts procured by successive extraction methods and to find out or isolate the most possible active compounds from the active extracts showing the best activity. The antidiabetic activity of all extracts has been evaluated by STZ induced diabetes. The isolated compounds have been evaluated by in-vitro and in-vivo models. The alcohol soluble extractives values were found to be higher than water soluble extractive value. Alcohol being a moderately non polar solvent, able to extract polar and non-polar components yields higher extractive value. The ethanol extract shows significant enhancement in glucose tolerance in glucose fed hyperglycemic normal rats and produced a marked decrease in blood glucose levels at 200 mg/kg and 400 mg/kg body weight in streptozotocin-diabetic rats after 21 days treatment. Keywords: Praecitrullus fistulosus, Streptozotocin and Glibenclamide, diabetes, Pharmacological Evaluation

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