Antitubercular activity assessment of fluorinated chalcones, 2-aminopyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives: In vitro, molecular docking and in-silico drug likeliness studies.

A series of newer previously synthesized fluorinated chalcones and their 2-amino-pyridine-3-carbonitrile and 2-amino-4H-pyran-3-carbonitrile derivatives were screened for their in vitro antitubercular activity and in silico methods. Compound 40 (MIC~ 8 μM) was the most potent among all 60 compounds, whose potency is comparable with broad spectrum antibiotics like ciprofloxacin and streptomycin and three times more potent than pyrazinamide. Additionally, compound 40 was also less selective and hence non-toxic towards the human live cell lines-LO2 in its MTT assay.

Design, Synthesis, and Antibacterial and Antifungal Activities of Novel Trifluoromethyl and Trifluoromethoxy Substituted Chalcone Derivatives.

Despite the availability of many drugs to treat infectious diseases, the problems like narrow antimicrobial spectrum, drug resistance, hypersensitivities and systemic toxicities are hampering their clinical utility. Based on the above facts, in the present study, we designed, synthesized and evaluated the antibacterial and antifungal activity of novel fluorinated compounds comprising of chalcones bearing trifluoromethyl (-) and trifluoromethoxy (-) substituents. The compounds were characterized by spectroscopic techniques and evaluated for their antimicrobial activity against four pathogenic Gram-positive ( and ) and Gram-negative ( and ) bacterial and fungal ( and ) strains.

Sekikaic acid modulates pancreatic β-cells in streptozotocin-induced type 2 diabetic rats by inhibiting digestive enzymes.

The antioxidant and antidiabetic effects of sekikaic acid were investigated using and study models. possessed good antioxidant activity as assessed through hydroxyl radicals (IC value = 41.5 µg/mL) and ferric ions assay (IC value = 42.

Development and Validation of a Stability Indicating RP-HPLC Method for Simultaneous Estimation of Teneligliptin and Metformin.

Objectives: The main objective of the present work is to develop a simple, precise, specific and stability method indicating reverse phase high performance liquid chromatography method for simultaneous estimation of teneligliptin and metformin in bulk and tablet dosage form.

Materials And Methods: The analysis was performed with a Kromasil C18 column (250×4.6 mm, 5 μm) at 30°C using buffer: acetonitrile: methanol (65:25:10, v/v/v) as mobile phase.

Novel indolizine derivatives lowers blood glucose levels in streptozotocin-induced diabetic rats: A histopathological approach.

Background: Diabetes mellitus is a deadly disorder in human which induce chronic complications. The streptozotocin (STZ)-induced diabetes in rat is the most common animal model of human diabetes. The present study investigated the effects of novel indolizine derivatives (1-16) on plasma blood glucose concentrations in STZ-diabetic rats.

Synthesis, Antimicrobial, and Computational Evaluation of Novel Isobutylchalcones as Antimicrobial Agents.

A series of 25 new chalcones were synthesized by Claisen-Schmidt condensation, well characterized by spectroscopic data, and evaluated for their antibacterial and antifungal activities by serial tube dilution method. Among the compounds tested, and containing 2,4-dichlorophenyl and 2,4-difluorophenyl moiety, respectively, were found to be the most potent in the series against both bacterial and fungal strains with a MIC value of 16 g/mL in each case. Further computational evaluation for antimicrobial activity was performed by atom based 3D-QSAR using PHASE™ software in order to have a correlation between the observed activities and predicted activities.

Molecular docking based screening of G6PS with 1, 5 Benzothiazepine derivates for a potential inhibitor.

Glucosamine-6-phosphate synthase (G6PS) (EC 2.6.1.

Molecular docking based screening of novel designed chalcone series of compounds for their anti-cancer activity targeting EGFR kinase domain.

Epidermal growth factor receptors (EGFR) are critical for the growth of many tumors and expressed at high levels in about one third of epithelial cancers. Hence, blockade of the binding sites for EGFR has been hypothesized as an effective anti-cancer therapy. Chalcone derivative compounds have been shown to be highly effective anti-cancer agents, however there are still so many novel derivatives possible, one of which might get us the best targeted EGFR inhibitor.

3D QSAR analysis of 2-(substituted aryl)-thiazolidine-4-carboxamides as potent antitubercular agents.

Thiazolidine-4-carboxylic acid derivatives were recognized recently for their potent antitubercular activity. A total of sixty four thiazolidine derivatives published in the recent times were collected and 3D QSAR models were developed, using CoMFA and COMSIA with high predictability. Later, we selected three new molecules, recently synthesized in our lab and evaluated them using the developed QSAR models.

A simple, rapid and sensitive liquid chromatography-tandem mass spectrometry method for the determination of dienogest in human plasma and its pharmacokinetic applications under fasting.

A simple, rapid and sensitive analytical method using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS) detection with positive ion electrospray ionization was developed for the determination of dienogest in human K2 EDTA plasma using levonorgestrel d6 as an internal standard (IS). Dienogest and IS were extracted from human plasma using simple liquid-liquid extraction. Chromatographic separation was achieved on a Zorbax XDB-Phenyl column (4.

Synthesis, characterization and in vitro biological evaluation of some novel 1,3,5-triazine-Schiff base conjugates as potential antimycobacterial agents.

A series of some novel 1,3,5-triazine-Schiff base conjugates (1-32) have been synthesized and evaluated for their in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using Alamar Blue assay and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Compounds 4 (4-Methoxy-6-methyl-N-(3,4,5-trimethoxybenzylidene)-1,3,5-triazin-2-amine), 11 (4-Methoxy-6-methyl-N-(2-hydroxy-3-bromo-5-chloro-benzylidene)-1,3,5-triazin-2-amine) and 24 (4-Methoxy-6-methyl-N-(1-(2,5-dihydroxyphenyl)ethylidene)-1,3,5-triazin-2-amine) exhibited a significant activity at 3.125, 6.

Synthesis, characterization and biological evaluation of some novel 2,4-thiazolidinediones as potential cytotoxic, antimicrobial and antihyperglycemic agents.

A series of some novel 2,4-thiazolidinediones (TZDs) (2a-x) have been synthesized and characterized by FTIR, (1)H NMR, (13)C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their cytotoxicity, antimicrobial and in vivo antihyperglycemic activities. Among the tested compounds for cytotoxicity using Brine Shrimp Lethality assay, compound 2t ((Z)-5-(4-((E)-3-oxo-3-(thiophen-2-yl)prop-1-enyl)benzylidene)-1,3-thiazolidine-2,4-dione) exhibited significant inhibitory activity at ED(50) value 4.

A new diterpene from the leaves of Andrographis paniculata Nees.

Phytochemical investigation of the methanolic extract of the leaves of Andrographis paniculata Nees yielded a minor, new diterpene, 21-nor-3,19-isopropylidine-14-deoxy-ent-labda-8(17),13-dien-16,15-olide (1), together with five known labdane type diterpenes, andrographolide 3, 14-deoxyandrographolide 4, 14-deoxy-12-hydroxyandrographolide 5, 14-deoxy-11,12-dihydroandrographolide 6, neoandrographolide 7, and two acids, cinnamic acid 8, and ferulic acid 9. The chemical structures were established by spectroscopic analyses, including 1D- and 2D-NMR spectroscopic experiments, and on the basis of HR-ESI MS analyses. The methanolic extract of the leaves exhibited moderate antibacterial and antifungal activities at a dose of 200 microg/mL in comparison with the reference standards.

Synthesis, characterization and in vitro biological evaluation of some novel diarylsulfonylureas as potential cytotoxic and antimicrobial agents.

A series of novel diarylsulfonylureas (1-28) have been synthesized and characterized by FTIR, (1)H NMR, (13)C NMR and LC mass spectral analysis. All the synthesized compounds were evaluated for their in vitro cytotoxicity and antimicrobial activities. Among the tested compounds for cytotoxicity using Brine Shrimp Lethality assay, compounds 18 and 22 exhibited significant cytotoxicity at ED(50) values 3.

Dissolution studies and quantification of meloxicam in tablet dosage form by spectrophotometry.

Two simple and inexpensive UV spectrophotometric methods were developed for the quantification and dissolution studies of meloxicam in tablet dosage forms. Meloxicam was estimated at 365nm and 360nm in Method I and Method II, respectively. The calibration curve was linear over a concentration range from 2.

A study of anti-inflammatory and analgesic activity of new 2,4,6-trisubstituted pyrimidines.

Chalcone derivatives (3a-m) were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes according to Claisen-Schmidt condensation. These chalcones, on reaction with guanidine hydrochloride under basic alcoholic conditions gave 2,4,6-trisubstituted pyrimidines (5a-m) in quantitative yields. All the newly synthesized pyrimidines were characterized by means of IR, ¹H- and ¹³C-NMR, Electron Ionization (EI)-mass and elemental analyses and screened for anti-inflammatory and analgesic activities by in vivo.

Flavones from the stem of Andrographis paniculata Nees.

Chemical investigation of Andrographis paniculata Nees (Acanthaceae) resulted in the isolation of three flavones identified as 5-hydroxy-7,8,2'-trimethoxyflavone 1, 5-hydroxy-7,8-dimethoxyflavone 2 and 5-hydroxy-7,8,2',5'-tetramethoxyflavone 3 from the hexane, methanol and chloroform extracts of the root and stem.