ChemInform Abstract: Synthesis and Characterization of New Thiourea and Urea Derivatives of 6-Fluoro-3-(piperidin-4-yl)benzo[d] Isoxazole: In vitro Antimicrobial and Antioxidant Activity.

ChemInform ◽  
2016 ◽  
Vol 47 (14) ◽  
Author(s):  
Hasti Sudhamani ◽  
Sk Thaslim Basha ◽  
Nagam Venkateswarlu ◽  
Tartte Vijaya ◽  
Chamarthi Naga Raju
2020 ◽  
Vol 72 (11-12) ◽  
pp. 1900323
Author(s):  
Xiaozhen Zhu ◽  
Xia Zhang ◽  
Xuelu Gao ◽  
Xianyao Meng ◽  
Yuetao Yi

2021 ◽  
Vol 42 (1) ◽  
pp. 29-38
Author(s):  
Hari Sharan Adhikari ◽  
Aditya Garai ◽  
Bishnu Prasad Marasini ◽  
Rameshwar Adhikari ◽  
Paras Nath Yadav

High molecular weight nanocrystalline chitosan (HMWNC)with Mw of 350 kDa and 66.92% DDA was prepared by alkaline N-deacetylation of chitin that was abundantly obtained after demineralization and deproteinization of pulverized crab shells, and commercially available chitosan oligosaccharide (COS) with average Mw< 3000 Da and 87% DDA was encapsulated with HMWNC. The encapsulation of COS as a pharmaceutical ingredient into HMWC was hypothesized to enhance the bioavailability of COS in target cells. The HMWNC encapsulated chitosan oligosaccharide (COS-HMWNC) showed in vitro antioxidant activity on 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals (IC50 = 512.6±14.4 μg/mL) while others showed less than 50% inhibition at 1000 μg/mL. The lower the molecular weight of chitosan, the higher was the antioxidant activity. The study showed that the encapsulation of COS molecules in HMWNCcould be used as a simple and effective way of enhancing the antioxidant activity of COS.


2019 ◽  
Vol 18 (10) ◽  
pp. 1417-1424 ◽  
Author(s):  
Emilia Naydenova ◽  
Diana Wesselinova ◽  
Svetlana Staykova ◽  
Ivan Goshev ◽  
Ljubomir Vezenkov

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
G. Kiran ◽  
T. Maneshwar ◽  
Y. Rajeshwar ◽  
M. Sarangapani

A series of β-Isatin aldehyde-N,N′-thiocarbohydrazone derivatives were synthesized and assayed for theirin vitroantimicrobial and antioxidant activity. The new compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. All the test compounds possessed a broad spectrum of activity having MIC values rangeing from 12.5 to 400 μg/ml against the tested microorganisms. Among the compounds3e,3jand3nshow highest significant antimicrobial activity. The free radical scavenging effects of the test compounds against stable free radical DPPH (α,α-diphenyl-β-picryl hydrazyl) and H2O2were measured spectrophotometrically. Compounds3j,3n,3l, and3e, respectively, had the most effective antioxidant activity against DPPH and H2O2scavenging activity.


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