135795-55-0Relevant articles and documents
New 2-Thiopyridines as potential candidates for killing both actively growing and dormant mycobacterium tuberculosis cells
Salina, Elena,Ryabova, Olga,Kaprelyants, Arseny,Makarov, Vadim
, p. 55 - 60 (2014)
From in vivo observations, a majority of M. tuberculosis cells in latently infected individuals are in a dormant and probably nonculturable state, display little metabolic activity, and are phenotypically resistant to antibiotics. Despite many attempts, no specific antimicrobials effective against latent tuberculosis have yet been found, partly because of a lack of reliable and adequate in vitro models for screening of drug candidates. We propose here a novel in vitro model of M. tuberculosis dormancy that meets the important criteria of latency, namely, nonculturability of cells, considerable reduction of metabolic activity, and significant phenotypic resistance to the first-line antibiotics rifampin and isoniazid. Using this model, we found a new group of 2-thiopyridine derivatives that had potent antibacterial activity against both actively growing and dormant M. tuberculosis cells. By means of the model of M. tuberculosis nonculturability, several new 2-thiopyridine derivatives were found to have potent antitubercular activity. The compounds are effective against both active and dormant M. tuberculosis cells. The bactericidal effects of compounds against dormant M. tuberculosis was confirmed by using three different in vitro models of tuberculosis dormancy. The model of nonculturability could be used as a reliable tool for screening drug candidates, and 2-thiopyridine derivatives may be regarded as prominent compounds for further development of new drugs for curing latent M. tuberculosis infection.
Synthesis and biological evaluation of 2,4,6-functionalized derivatives of pyrido[2,3-d]pyrimidines as cytotoxic agents and apoptosis inducers
Sanmartin, Carmen,Dominguez, Maria Victoria,Cordeu, Lucia,Cubedo, Elena,Garcia-Foncillas, Jesus,Font, Maria,Palop, Juan Antonio
, p. 28 - 41 (2008)
In the search for new derivatives with anticancer activity that are able to induce a selective proapoptotic mechanism in cancer cells, we have designed, synthesized, and evaluated a series of new 2-(alkylsulfanyl)-N-alkylpyrido[2,3- d]pyrimidine-4-amine derivatives as cytotoxic and apoptosis inducers. The potential antitumor activity of the compounds was evaluated in vitro by examining their cytotoxic effects against human breast, colon, and bladder cancer-cell lines. The IC50 values of the compounds that showed cytotoxic activity were calculated. The cytotoxic compounds were then tested for their ability to induce caspase-3 activation and nuclear-chromatin degradation. Some compounds, such as 6c, 6d, 6e, 6j, 6o, and 6p, show significant in-vitro cytotoxicity in at least two of the three tested cell lines, induced apoptosis, and also produced a rapid dose-dependent increase in the caspase-3 level in some of the cell lines tested. In order to test the selectivity of the compounds, two non-tumoral human cell lines were used. Several compounds of the did not show cytotoxicity in these cell lines.
SULFONAMIDE COMPOUNDS HAVING TNAP INHIBITORY ACTIVITY
-
Page/Page column 112; 113; 114; 115; 177; 178; 187; 188; 197; 198, (2018/07/29)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.
3-cyanopyrazolopyrimidine [1,5-a] derivative as well as preparation method and application thereof
-
Paragraph 0074-0076, (2018/11/22)
The invention belongs to the field of chemical medicines and specifically relates to a 3-cyanopyrazolopyrimidine [1,5-a] derivative as well as a preparation method and application thereof. The invention provides the 3-cyanopyrazolopyrimidine [1,5-a] derivative, and the structure of the 3-cyanopyrazolopyrimidine [1,5-a] derivative is shown as a formula I. The invention further provides the preparation method and the application of the 3-cyanopyrazolopyrimidine [1,5-a] derivative. (The formula I is shown in the description).
PYRIDO-OXAZINONE DERIVATIVES AS TNAP INHIBITORS
-
Page/Page column 64; 65, (2017/02/09)
The present invention relates to a compound or a pharmacologically acceptable salt thereof having excellent tissue non-specific alkaline phosphatase inhibitory activity. The present invention provides a compound represented by the formula (I) : wherein R
4 H - pyrido [3, 2 - e] [1, 3] thiazine - 4 - ketone derivative and its application
-
Paragraph 0097-0098, (2017/11/16)
The invention relates to the technical field of medicines, discloses a novel 4H-pyridino-[3,2-e][1,3]thiazine-4-ketone derivate and an application thereof, and designs and synthesizes a series of novel-structure 4H-pyridino-[3,2-e][1,3]thiazine-4-ketone c
METHODS FOR PREPARING NAPHTHYRIDINES
-
Page/Page column 19-20, (2012/12/13)
The present invention provides methods of synthesizing compounds of formula (1) and intermediates thereto. The present invention also provides intermediates useful in the synthesis of compounds of formula (1).
THE NITROPYRIDINYL ETHYLENEIMINE COMPOUND, THE PHARMACEUTICAL COMPOSITION CONTAINING IT, THE PREPARATION METHOD AND USE THEREOF
-
, (2011/10/10)
The present invention discloses a nitropyridinyl ethyleneimine compound as shown in the formula I and a preparation method of the same, as well as use of the compound in manufacture of a prodrug and in manufacture of a drug for treating a tumor.
Dipyridodiazepinone derivatives; synthesis and anti HIV-1 activity
Khunnawutmanotham, Nisachon,Chimnoi, Nitirat,Techasakul, Supanna,Thitithanyanont, Arunee,Saparpakorn, Patchreenart,Hannongbua, Supa,Choowongkomon, Kiattawee,Pungpo, Pornpan
supporting information; experimental part, (2010/04/22)
Ten dipyridodiazepinone derivatives were synthesized and evaluated for their anti HIV-1 reverse transcriptase activity against wildtype and mutant type enzymes, K103N and Y181C. Two of them were found to be promising inhibitors for HIV-1 RT.
Transformations of ortho-methoxyaryl(hetaryl)carboxamides into quinazolin-4-one and pyrido[2,3-d]pyrimidin-4-one derivatives
Ryabova,Makarov,Alekseeva,Shashhov,Chernyshev,Granik
, p. 1907 - 1914 (2007/10/03)
ortho-Chloroaryl(hetaryl)carboxamides containing one or two nitro groups at positions 3 and/or 5 of the ring undergo condensation accompanied by the pyrimidine ring closure on refluxing in an excess of sodium methoxide to form bicyclic products, viz., qui