366-81-4Relevant academic research and scientific papers
Design, synthesis and insecticidal activity of novel semicarbazones and thiosemicarbazones derived from chalcone
Cheng, Wei,Xiao, Tingting,Qian, Weifeng,Lu, Tong,Zhang, Tingting,Tang, Xiaorong
, p. 3801 - 3809 (2020/03/23)
Thirty semicarbazone and thiosemicarbazone derivatives (2a–w and 4a–g) from chalcones containing furan and thiophene ring were designed and synthesized. They were characterized by IR, 1H NMR, 13C NMR and HRMS. The crystal structure o
2,4,6-trisubstituted pyridine compound and application thereof in pesticide
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Paragraph 0082; 0084, (2021/06/13)
The invention relates to a 2,4,6-trisubstituted pyridine compound and application thereof in pesticides, and belongs to the technical field of pesticides. The structural formula of the 2,4,6-trisubstituted pyridine compound is as shown in formula (I), in
Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides
Mete, Ebru,Comez, Birnur,Inci Gul, Halise,Gulcin, Ilhami,Supuran, Claudiu T.
, p. 1 - 5 (2016/12/14)
A series of new thienyl-substituted pyrazoline benzenesulfonamides were synthesized and their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were tested on the human (h) isoforms hCA I and hCA II. The inhibition constant (Ki) of thes
Thiophene chalcone semicarbazone Schiff base compounds, and preparation method and applications thereof
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Paragraph 0029; 0033; 0034, (2016/10/10)
The invention provides thiophene chalcone semicarbazone Schiff base compounds, and a preparation method and applications thereof. Structure general formula of the thiophene chalcone semicarbazone Schiff base compounds is represented by a formula I in the invention, wherein R is used for representing single substitution or double substitution, and is used for representing fluorine atoms, chlorine atoms, bromine atoms, iodine atoms, methyl, methoxyl, or phenyl. The thiophene chalcone semicarbazone Schiff base compounds are simple and novel in structure, are convenient to be synthesized, and possess excellent control effects on plant pathogenic fungi. The thiophene chalcone semicarbazone Schiff base compounds are taken as plant pathogenic fungi inhibitors for the first time.
Thiophene allyl alcohol compound as well as preparation method and application thereof
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Paragraph 0034; 0035, (2016/10/17)
The invention provides a thiophene allyl alcohol compound. A general structural formula of the thiophene allyl alcohol compound is shown in the specification, wherein in the general formula (I), R1 is a hydrogen atom, a chlorine atom, a bromine atom, meth
Synthesis and biological evaluation of novel 1,3,5-trisubstituted pyrazolines
Revanasiddappa,Jisha,Varghese, Saira Susan,Kalsi, Jasmine,Jose, Neethu
, p. 51 - 54 (2019/01/21)
A new series of chalcones (1a-j) was prepared by reacting 2-thiophene carbaldehyde and substituted ketones in alcohol medium in presence of NaOH. The chalcones undergoes selective cyclization with 4-hydroxybenzohydrazide (2) in gl acetic acid medium to yield the title compounds 1,3,5-trisubstituted pyrazolines (3a-j). All the newly synthesized compounds were evaluated for their in-vitro antibacterial and antifungal activities. The structures of the new compounds were assigned on the basis of elemental analysis, 1H NMR, IR and Mass spectral data.
Synthesis and selective inhibitory activity against human COX-1 of novel 1-(4-substituted-thiazol-2-yl)-3,5-di(hetero)aryl-pyrazoline derivatives
Carradori, Simone,Secci, Daniela,Bolasco, Adriana,De Monte, Celeste,Yá?ez, Matilde
, p. 973 - 979 (2013/02/23)
Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2-pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1-thiocarbamoyl-2- pyrazolines with the ethyl ester of α-bromo-pyruvic acid. The synthesized compounds were confirmed by spectroscopic data and assayed to evaluate their in vitro ability to inhibit both isoforms of human cyclooxygenase (hCOX). Some derivatives (compounds 5, 6, 13, 16, and 17) displayed promising selectivity against hCOX-1 in the micromolar range and were shown to have a selectivity index similar or better than the reference drugs (indometacin, diclofenac). The introduction of a phenyl or a 4-F-phenyl ring on the C5 associated with a 4-substituted phenyl or a heteroaryl group on the C3 of (4-substituted-thiazol- 2-yl)pyrazoline derivatives improved the activity against hCOX-1. Thanks to these preliminary results it could be possible to extend our knowledge of the pharmacophoric requirements for the discovery of new pyrazoline-based hCOX-1 inhibitors. Novel 1-(4-ethyl carboxylate-thiazol-2-yl)-3,5-di(hetero)aryl-2- pyrazoline derivatives were obtained by reacting 3,5-di(hetero)aryl-1- thiocarbamoyl-2-pyrazolines with the ethyl ester of α-bromo-pyruvic acid. Some derivatives displayed promising selectivity against human cyclooxygenase 1 (hCOX-1) in the micromolar range, with a selectivity index similar or better than the reference drugs, indometacin and diclofenac. Copyright
