31061-79-7Relevant academic research and scientific papers
Oxadiazole based Os(IV) compounds as potential DNA intercalator and cytotoxic agents
Bhatt, Bhupesh S.,Patel, Mohan N.,Pathak, Chandramani,Pursuwani, Bharat H.,Vaidya, Foram U.
, (2020/07/10)
Os(IV) compounds and ligands have been synthesized and well characterized. DNA cleavage tendency of compounds has been evaluated using gel electrophoresis and binding behavior has been evaluated by viscosity measurements, absorption titration, fluorescenc
An efficient one-pot synthesis of 2,5-disubstituted-1,3,4-thiadiazoles from aldehydes and hydrazides using Lawesson’s reagent
Ko, Inseok,Park, Soojin,Lee, Goeun,Kim, Hakwon
, p. 67 - 78 (2019/03/07)
Five-membered heterocyclic-ring systems, such as thiadiazoles, remain an important and prevalent scaffold in the development of novel leads in medicinal chemistry for a variety of therapeutic targets. A two-step, one-pot synthesis of 2,5-disubstituted-1,3,4-thiadiazole derivatives from aryl hydrazides and aryl aldehydes using Lawesson’s reagent is described, yielding 2,5-disubstituted-1,3,4-thiadiazoles in moderate-to-high yields. Based on preliminary biological experiments, some of the newly synthesized thiadiazoles show antioxidant activity.
Synthesis and Fluorescence Properties of Eu3+, Tb3+ Complexes with Schiff Base Derivatives
Liu, Yanhong,Kong, Weihua,Yang, Zehui,Dai, Ming,Shi, Ling,Guo, Dongcai
, p. 567 - 576 (2016/03/12)
Novel Schiff base ligands derived from N′-benzylidene-benzohydrazide (substituted by-H,-CH3,-OCH3,-Cl) and 2-chloro-N-phenylacetamide were synthesized. The solid complexes of rare earth (Eu, Tb) nitrate with these Schiff base ligands
2,5-Diaryloxadiazoles and their precursors as novel inhibitors of cathepsins B, H and L
Garg, Shweta,Raghav, Neera
, p. 64 - 74 (2016/07/06)
High levels of cathepsins indicated in various pathological conditions like arthritis, cancer progressions, and atherosclerosis explains the need to explore potential inhibitors of these proteases which can be of great therapeutic significance. We, in the present work, report the synthesis of some 2,5-diaryloxadiazoles from N-subsitutedbenzylidenebenzohydrazides. The synthesized compounds were screened for their inhibitory potential on cathepsins B, H and L. Structure Activity Relationship studies show that 2,5-diaryloxadiazoles were less inhibitory than their precursors. 1i and 2k have been found to be most inhibitory to cathepsins B and L. Their Ki values have been calculated as 11.38 × 10-8 M and 66.4 × 10-8 M for cathepsin B and 4.2 × 10-9 M and 47.31 × 10-9 M for cathepsin L, respectively. However, cathepsin H activity was maximally inhibited by compounds, 1e and 2c with Ki values of 4.4 × 10-7 M and 5.6 × 10-7 M, respectively. Enzyme kinetic studies suggest that these compounds are competitive inhibitors to the enzymes. The results have been compared with docking results obtained using iGemDock.
Training a Constitutional Dynamic Network for Effector Recognition: Storage, Recall, and Erasing of Information
Holub, Jan,Vantomme, Ghislaine,Lehn, Jean-Marie
supporting information, p. 11783 - 11791 (2016/10/07)
Constitutional dynamic libraries (CDLs) of hydrazones, acylhydrazones, and imines undergo reorganization and adaptation in response to chemical effectors (herein metal cations) via component exchange and selection. Such CDLs can be subjected to training by exposition to given effectors and keep memory of the information stored by interaction with a specific metal ion. The long-term storage of the acquired information into the set of constituents of the system allows for fast recognition on subsequent contacts with the same effector(s). Dynamic networks of constituents were designed to adapt orthogonally to different metal cations by up- and down-regulation of specific constituents in the final distribution. The memory may be erased by component exchange between the constituents so as to regenerate the initial (statistical) distribution. The libraries described represent constitutional dynamic systems capable of acting as information storage molecular devices, in which the presence of components linked by reversible covalent bonds in slow exchange and bearing adequate coordination sites allows for the adaptation to different metal ions by constitutional variation. The system thus performs information storage, recall, and erase processes.
Tin Powder-Promoted One-Pot Construction of α-Methylene-γ-lactams and Spirolactams from Aldehydes or Ketones, Acylhydrazines, and 2-(Bromomethyl)acrylate
Xu, Yanli,Huang, Danfeng,Wang, Ke-Hu,Ma, Junyan,Su, Yingpeng,Fu, Ying,Hu, Yulai
, p. 12224 - 12233 (2016/01/09)
A concise and efficient method for the synthesis of α-methylene-γ-lactams is developed from multicomponent one-pot reactions of aldehydes or ketones, hydrazides, and ethyl 2-(bromomethyl)acrylate promoted by tin powder. The reaction proceeds smoothly under mild reaction conditions without using any catalyst to give the corresponding products in high yields. α-Methylene-γ-spirolactams can also be prepared from cyclic ketones.
Efficient oxidative cyclization of N -acylhydrazones for the synthesis of 2,5-disubstituted 1,3,4-oxadiazoles using t-BuOI under neutral conditions
Gao, Peng,Wei, Yunyang
, p. 113 - 119 (2013/05/23)
An efficient procedure for the oxidative cyclization of N -acylhydrazones was developed utilizing tert-butyl hypoiodite (t-BuOI), which is generated in situ from t -BuOCl and NaI. A variety of 2,5-disubstituted 1,3,4-oxadiazoles were synthesized in high yields within short reaction time. The method is also suitable for cyclization of N -acylhydrazones derived from heterocyclic aldehydes and aliphatic aldehydes. Mild reaction conditions and simple workup operations make the procedure a good alternative for the synthesis of 2,5-disubstituted 1,3,4-oxadiazoles.
One-pot, three component synthesis of 2,5-disubstituted 1,3,4-oxadiazoles catalyzed by heteropolyacid
Heravi, Majid M.,Zadsirjan, Vahideh,Bakhtiari, Khadijeh,Bamoharram, Fatemeh F.
, p. 259 - 263 (2013/03/29)
H6[PMo9V3O40] was used as an efficient catalyst for the preparation of 1-aroyl-2-arylidene hydrazines. 2,5-Disubstituted 1,3,4-oxadiazoles have been synthesized by oxidation of 1-aroyl-2-arylidene hydrazines with CrO3 in excellent yields.
Synthesis, characterization and biological studies of mononuclear copper(II) complexes with ciprofloxacin and N, O donor ligands
Patel, Mohan N.,Patel, Chintan R.,Joshi, Hardik N.
, p. 51 - 55 (2013/03/13)
The mixed ligand Cu(II) complexes of ciprofloxacin and N, O donor Schiff bases have been prepared and characterized by physicochemical techniques. In these complexes, ciprofloxacin acts as bidentate deprotonated ligand bound to the metal through the pyrid
Electrosynthesis and screening of novel 1,3,4-oxadiazoles as potent and selective antifungal agents
Singh, Sushma,Sharma, Laxmi Kant,Saraswat, Apoorv,Siddiqui, Ibadur R.,Kehri, Harbans K.,Singh, Rana K. Pal
, p. 4237 - 4245 (2013/05/08)
The electrochemical oxidation of aldehyde-N-aroylhydrazone has been studied in the presence of NaClO4 as supporting electrolyte in MeOH solution using cyclic voltammetry and controlled potential electrolysis. The results indicate that intramolecular cyclization of aldehyde-N-aroylhydrazone has been successfully performed at a platinum electrode in an undivided cell with good yields of the corresponding 1,3,4-oxadiazoles at ambient conditions. The reaction products were characterized by spectroscopic methods and a mechanism was deduced from voltammetry studies. The antifungal activity of the synthesized compounds was evaluated on Fusarium oxysporum, Alternaria solani, Candida albicans and Aspergillus niger. The results revealed that all the synthesized compounds have significant antifungal activity against the tested fungi. Among the synthesized derivatives 7b, 7d, 7g, 7h, 7i, 7j and 7r were found to be the most effective antifungal compounds. The Royal Society of Chemistry 2013.
