Activity Of Standard Drugs Research Articles

Synthesizing, Studying Molecular Docking, Characterizing, and Preliminary Evaluating Anti-Bacterial Effects of Derivatives of Serotonin Contain Imidazolidine Ring

This study included synthesis of new serotonin derivatives in which imidazolidine rings are present in their structures. The final imidazolidine derivatives compounds were synthesized by reaction of synthesized
 
 Schiff bases derivatives of serotonin with the glycine (NH2-CH2COOH) in presence of tetrahydrofuran (THF) as a solvent. The imidazolidine derivatives were identified by physical characteristics, FT-IR spectroscopy and 1H- NMR spectroscopy. Biological activities against two Gram negative (Klebsiella and E. coli) and two Gram positive (Streptococcus pyogenes and Staphylococcus aureus) bacteria were also distinguished. All the synthesized compounds III(a-d) exhibit moderate activities on four types of bacteria comparing with the activity of standard drug (Trimethoprim) but the highest activities of these compounds occur on Streptococcus pyogenes and their least activities occur on E. coli. The synthesized compounds were studied for the molecular docking to know the interaction and affinity of binding between them and bacteria

In-vitro antidiabetic activity of methanolic extract of leaves and fruits of Pouteria campechiana (Kunth) Baehni

Introduction and Aim: Herbal medicine have been used to treat several ailments since decades. Pouteria campechiana (Kunth) Baehni belongs to the family Sapotaceae which is widely found around the world. In folk medicine, various parts of P. campechiana is used to treat various illness. Inhibition of alpha-amylase and alpha-glucosidase enzymes can be an important strategy in management of postprandial blood glucose level in non-insulin dependent diabetic patient. Hence, present study focused to evaluate the in vitro antidiabetic activity of leaf and fruit methanolic extract of Pouteria campechiana (Kunth) Baehni. Materials and Methods: Methanolic extract of P. campechiana leaf (PCL) and fruit (PCF) was screened by biochemical assay such as ?-amylase inhibition activity by CNPG3 method (2-chloro-p-nitrophenyl-?-D-maltotrioside) and ?- glucosidase inhibition activity and in vitro cellular assay such as glucose uptake assay in 3T3-L1 cell line. Results: Methanolic extract of P. campechiana leaf and fruit showed inhibition of ??Amylase and ??Glucosidase enzymes. The methanolic extract of P. campechiana leaf and fruit at varying concentrations (?g/ml), did not exhibit cytotoxicity against 3T3-L1 cell line after 24 hours of incubation. The test compounds PCL and PCF induced the uptake of 2?(N?(7?Nitrobenz?2?oxa?1,3?diazol?4?yl) Amino) ? 2?Deoxyglucose (2-NBDG) in 3T3L1 cells. PCF and PCL both showed almost similar activity of standard drug, Metformin at higher concentrations. Conclusion: Based on the results, it can be concluded that methanolic leaf and fruit extract of P. campechiana possess antidiabetic activity.

Extracts of Ficusgibboseblame and its potentiating effect for type II diabetes in rats

HydroalcoholicextractofGreeneriesandstalkbarkofFicusgibbosaBlume is evaluated for their potentiating action in Streptozotocin – Nicotinamide encouraged type 2 diabetes in Sprague Dawley rats. The excerpts are managed at the amount of 100, 250 and 500 mg/kg body weight along with sub operative dose (2.5 mg/kg body weight) of the standard antidiabetic drug (Glibenclamide) for a period of 5 weeks. The test extracts potentiated the antidiabetic activity of standard drug by significantly dropping the raised blood glucose levels and the effect was almost comparable with solitary efficacy of therapeutic dose (5 mg/kg body weight) of typical drug Glibenclamide during 5th week of the study. Its abandons have deviated, on the other hand, orchestrated and more gibbose in those end. The juice of the bark furthermore abandons from claiming color fig alternately bumped fig plant is utilized to grinding those pills furthermore settling on A decoction in toxicology. Plant appeases diminished Kapha, pitta, skin diseases, ulcers, hepatopathy, diabetes, ulcerative stomatitis, leucorrhoea and gynaecological issues. Male Sprague Dawley Rats abstainedinstantare vaccinated intraperitoneally with result about Nicotinamide at a dosage of 195 mg /kg body weight. 15 minutes after same animals are vaccinated for the newly readied result from claiming Streptozotocin (STZ) In measurement about (65 mg/kg physique weight) intraperitoneally. The animals are permitted to drink 1% glucose result instant will succeed the pill prompted hypoglycaemia.

Design, Synthesis, and Biological Evaluation of New 8‐Trifluoromethylquinoline Containing Pyrazole‐3‐carboxamide Derivatives

The article describes the design, synthesis, and characterization of a new series of 8‐trifluoromethylquinoline substituted pyrazole‐3‐carboxamides (9a, 9b, 9c, 9d, 9e, 9f, 9g, 9h, 9i, 9j, 9k, 9l, 9m, 9n, 9o, 9p, 9q, 9r, 9s, 9t) derived from different primary and secondary amines. The intermediate and target compounds were characterized using spectroscopic methods. The structures of intermediate 7 and target molecule 9d were evidenced by the single crystal X‐ray study. All the synthesized target compounds (9a, 9b, 9c, 9d, 9e, 9f, 9g, 9h, 9i, 9j, 9k, 9l, 9m, 9n, 9o, 9p, 9q, 9r, 9s, 9t) and three intermediates (6, 7, 8) were screened for their in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv strain. Two compounds, 9k and 9t, showed significant inhibition activity with MIC of 3.13 µg/mL, which is comparable with the activity of standard drug, ethambutol. The carboxamides derived from benzylamine derivatives were more active than their aniline analogs. In general, the hybrid amides with a N‐methylene linkage (‐CONHCH2‐) exhibited enhanced antitubercular activity. In the antibacterial screening, intermediate 3‐hydrazinyl‐2‐methyl‐8‐(trifluoromethyl)quinoline (6) displayed remarkable activity against the tested bacterial strains. Further, the active anti‐TB derivatives were non‐toxic to benign NIH 3T3 cells, which demonstrate the lack of general cellular toxicity and hence signifies their suitability for further lead development.

Synthetic aspects, spectral, thermal studies and antimicrobial screening on bis(N,N-dimethyldithiocarbamato-S,S′)antimony(III) complexes with oxo or thio donor ligands

The bis(N,N-dimethyldithiocarbamato-S,S′)antimony(III) complexes have been obtained by the reaction of chloro bis(N,N-dimethyldithiocarbamato-S,S′)antimony(III) with corresponding oxo or thio donor ligands such as sodium benzoate 1, sodium thioglycolate 2, phenol 3, sodium 1-propanethiolate 4, potassium thioacetate 5, sodium salicylate 6, ethane-1,2-dithiolate 7 and disodium oxalate 8. These complexes have been characterized by the physicochemical [melting point, molecular weight determination and elemental analysis (C, H, N, S and Sb)], spectral [UV–Visible, FT-IR, far IR, NMR (1H and 13C)], thermogravimetric (TG & DTA) analysis, ESI-Mass and powder X-ray diffraction studies. Thermogravimetric analysis of the complexes confirmed the final decomposition product as highly pure antimony sulfide (Sb2S3) and powder X-ray diffraction studies show that the complexes are in lower symmetry with monoclinic crystal lattice and nano-ranged particle size (11.51–20.82nm). The complexes have also been screened against some bacterial and fungal strains for their antibacterial and antifungal activities and compared with standard drugs. These show that the complexes have greater activities against some human pathogenic bacteria and fungi than the activities of standard drugs.

Synthesis, characterization, DNA binding, oxidative damage of DNA strand scission, and antimicrobial activities of β-diketone condensed Schiff-base transition metal complexes

Co(II), Ni(II), Cu(II), Zn(II), and VO(IV) complexes containing a versatile β-diketone Schiff-base ligand (obtained by the condensation of 3-furan-2-ylmethylene-2,4-dione and 2-aminophenol) have been synthesized and characterized. Microanalytical, magnetic, and spectroscopic data reveal that the central metal is coordinated to two oxygens of phenolate and two nitrogens of imine of the ligand. Binding of synthesized complexes with calf thymus DNA has been investigated by spectroscopic and electrochemical methods and viscosity measurements. The complexes are able to form adducts with DNA and to distort the double helix by changing the base stacking. Electrostatic binding of vanadyl complex is observed from the weak hypochromism in electronic absorption spectra and no change in the viscosity with DNA. Oxidative DNA cleavage activities of the complexes are studied with supercoiled pUC19 DNA using gel electrophoresis. The hydroxyl radical (OH•) is likely to be the species responsible for the cleavage of pUC19 DNA by the synthesized complexes. Under our experimental conditions, the vanadyl complex has no significant cleavage of DNA. The compounds have been screened for activity against several bacterial and fungal strains and the results are compared with the activity of standard drugs.