27161-64-4Relevant academic research and scientific papers
Discovery, Synthesis, and invitro Evaluation of West Nile Virus Protease Inhibitors Based on the 9,10-Dihydro-3H,4aH-1,3,9,10a-tetraazaphenanthren-4-one Scaffold
Samanta, Sanjay,Cui, Taian,Lam, Yulin
experimental part, p. 1210 - 1216 (2012/08/08)
West Nile virus (WNV), a member of the Flaviviridae family, is a mosquito-borne pathogen that causes a great number of human infections each year. Neither vaccines nor antiviral therapies are currently available for human use. In this study, a WNV NS2B-NS3 protease inhibitor with a 9,10-dihydro-3H,4aH-1,3,9,10a-tetraazaphenanthren-4-one scaffold was identified by screening a small library of non-peptidic compounds. This initial hit was optimized by solution-phase synthesis and screening of a focused library of compounds bearing this scaffold. This led to the identification of a novel, uncompetitive inhibitor (1a40, IC50=5.41±0.45μM) of WNV NS2B-NS3 protease. Molecular docking of this chiral compound onto the WNV protease indicates that the Senantiomer of 1a40 appears to interfere with the productive interactions between the NS2B cofactor and the NS3 protease domain; (S)-1a40 is a preferred isomer for inhibition of WNV NS3 protease.
Aqua mediated one pot facile synthesis of novel thioxo-1,2,4-triazin-5(2H)- one and [1,2,4] triazino[5,6-b]indole derivatives and their biological activities
Sachdeva, Harshita,Dwivedi, Diksha,Singh, Har Lal,Sharma, Kanti Prakash
, p. 1348 - 1354 (2013/06/27)
Rapid and highly efficient one pot green chemical synthesis of substituted 6-(2-aminophenyl)-4-(4-substitutedphenyl)-3-thioxo-3,4-dihydro-1,2, 4-triazin-5(2H)-one and 8-substituted-3,5-dihydro-2H-[1,2,4]triazino[5,6-b] indole is carried out in aqueous medium under microwave irradiation. Improved synthesis of potent bioactive Schiff and N-Mannich bases of hexahydro-1H-indole- 2,3-dione is also reported. The title compounds are easily accessible by various approaches; even waste free approaches have been developed. The operational simplicity, environmentally benign conditions and high yield achieved in a very short reaction time are major benefits that meet the requirements of green production, including saving energy and high efficiency. The results obtained under microwaves are compared with that of conventional heating. Structural assignments are based on spectroscopic data. Compounds have also been screened for antibacterial and antifungal activities.
Transcription factor modulating compounds and methods of use thereof
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Page/Page column 60, (2008/06/13)
Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.
Transcription factor modulating compounds and methods of use thereof
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, (2008/06/13)
Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.
Transcription factor modulating compounds and methods of use thereof
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Page 43, (2008/06/13)
Methods for identifying compound useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. In one embodiment, the method comprises contacting a microbial cell comprising: 1) a selectable marker under the control of
SEMICARBAZONES AND THIOSEMICARBAZONES OF THE HETEROCYCLIC SERIES. XLVIII. REACTION OF 1-ACETYLISATINS WITH THIOSEMICARBAZIDES
Tomchin, A. B.,Krylova, I. M.
, p. 2173 - 2186 (2007/10/02)
In reaction with thiosemicarbazides 1-acylisatins form the thiosemicarbazides of N-acylisatinic acids in addition to the thiosemicarbazones.The yields of the thiosemicarbazides increase with increase in the electron-withdrawing effect of the acyl residue or with substitution of a hydrogen atom in the primary thioamide group of the initial thiosemicarbazides by alkyl radicals.The reaction products are capable of transformation to the 3-thiosemicarbazones of 1-acylisatins.The latter were isolated in the form of E and Z isomers, and their mutual transitions were investigated.The five-membered ring of 1-acetylisatin thiosemi carbazone opens in an alkaline medium with the formation of the thiosemicarbazone of N-acetylisatinic acid.Contrary to previous data, this compound does not undergo direct cyclization to the 1,2,4-triazinoindole derivatives.
1,2,4-TRIAZINE DERIVATIVES, XXII. A NOVEL SYNTHESIS OF 5-SUBSTITUTED 3-ALKYLAMINO-5H-TRIAZINOINDOLE DERIVATIVES
Doleschall, G.,Simon-Ormai, K.
, p. 107 - 112 (2007/10/02)
A novel synthesis of 5-substituted 3-alkylamino-5H-triazinoindole derivatives, starting with primary amines and 6-(2-aminophenyl)-3-methylthio-1,2,4-triazin-5-(2H)-one or 6,6-dimethyl-3-methylthio-6,7-dihydro-triazinoquinazolin
