611-22-3Relevant articles and documents
Kinetics and mechanism of the mineral acid catalysed reactions of hydroxamic acids
Ghosh, Kallol K.,Vaidya, Jyoti,Sinha, Daliya
, p. 563 - 573 (2004)
There is currently a great deal of interest in the chemistry of hydroxamic acids. In recent years we have been studying the synthesis, structure and nucleophilicities of hydroxamic acids. This paper reports a kinetic study of reactivity of some hydroxamic acids RC(O)·N(OH)R′; R = C 6H5·CH=CH, R′ = 4-CH3· C6H4 [p-tolylcinnamo hydroxamic acid]; R = C 6H5, R′ 4-CH3·C6H 4 [p-tolylbenzo hydroxamic acid]; R = C6H5, R′ = 2-CH3·C6H4 [o-tolylbenzo hydroxamic acid] in aqueous mineral acids (HCl, HClO4 and H 2SO4). The rate data of hydrolysis reaction revealed that the reactivity/stability sequence of the compounds is generally p-TBHA > o-TBHA > p-TCHA. An excess acidity analysis reveals that the reaction proceeds by nucleophilic attack of water molecule on the protonated substrate.
Bactericidal composition containing isotianil and osthole
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Paragraph 0019; 0029; 0034, (2021/08/11)
The invention discloses a bactericidal composition containing isotianil and osthole, and belongs to the technical field of pesticide preparation. The bactericidal composition comprises, by weight, 1-50% of isotianil, 0.1-10% of osthole, 5-10% of a bacteri
Synthesis of sulpha drug based hydroxytriazene derivatives: Anti-diabetic, antioxidant, anti-inflammatory activity and their molecular docking studies
Baroliya, Prabhat K.,Chauhan, R. S.,Dayma, Varsha,Dwivedi, Aparna,Goswami, A. K.,Sharma, Poonam,Tripathi, I. P.,Vanangamudi, Murugesan
, (2020/02/15)
Herein, we report synthesis, characterization, anti-diabetic, anti-inflammatory and anti-oxidant activities of hydroxytriazenes derived from sulpha drugs, namely sulphanilamide, sulphadiazine, sulphapyridine and sulphamethazine. Before biological screening of the compounds, theoretical prediction using PASS was done which indicates probable activities ranging from Pa (probable activity) values 65–98% for anti-inflammatory activity. As per the predication, experimental validation of some of the predicted activities particularly anti-diabetic, anti-inflammatory and anti-oxidant was done. Anti-diabetic activities have been screened using two methods namely α-amylase and α-glucosidase inhibition method and IC50 values were ranging from 66 to 260 and 148 to 401 μg/mL, while for standard drug acarbose the values were 12 μg/mL and 70 μg/mL, respectively. Docking studies have also been done for antidiabetic target pancreatic alpha amylase. The molecular docking studies in α-amylase enzyme reveal that the middle phenyl ring of all the compounds mainly occupies in the small hydrophobic pocket formed by the Ala198, Trp58, Leu162, Leu165 and Ile235 residues and sulphonamide moiety establish H-bond interaction by two water molecules. Further, anti-inflammatory activity has been evaluated using carrageenan induced paw-edema method and results indicate excellent anti-inflammatory activity by hydroxytriazenes (71 to 97%) and standard drug diclofenac 94% after 4 h of treatment. Moreover, antioxidant effect of the compounds was tested using DPPH and ABTS methods. All the compounds displayed good results (24–488 μg/mL) against ABTS radical and many compounds are more active than ascorbic acid (69 μg/mL) while all other compounds showed moderate activity against DPPH radical (292–774 μg/mL) and ascorbic acid (29 μg/mL). Thus, the studies reveal potential of sulfa drug based hydroxytriazenes as candidates for antidiabetic, anti-inflammatory and antioxidant activities which have been experimentally validated.
A general and scalable synthesis of polysubstituted indoles
Diana-Rivero, Raquel,García-Tellado, Fernando,Tejedor, David
, (2021/06/14)
A consecutive 2-step synthesis of N-unprotected polysubstituted indoles bearing an electron-withdrawing group at the C-3 position from readily available nitroarenes is reported. The protocol is based on the [3,3]-sigmatropic rearrangement of N-oxyenamines generated by the DABCO-catalyzed reaction of N-arylhydroxylamines and conjugated terminal alkynes, and delivers indoles endowed with a wide array of substitution patterns and topologies.
