21239-87-2Relevant academic research and scientific papers
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials
McConville, Matthew,Fernández, Jorge,Angulo-Barturen, í?igo,Bahamontes-Rosa, Noemi,Ballell-Pages, Lluis,Casta?eda, Pablo,De Cózar, Cristina,Crespo, Benigno,Guijarro, Laura,Jiménez-Díaz, María Belén,Martínez-Martínez, Maria S.,De Mercado, Jaime,Santos-Villarejo, ángel,Sanz, Laura M.,Frigerio, Micol,Washbourn, Gina,Ward, Stephen A.,Nixon, Gemma L.,Biagini, Giancarlo A.,Berry, Neil G.,Blackman, Michael J.,Calderón, Félix,O'Neill, Paul M.
supporting information, p. 6448 - 6455 (2015/09/08)
(Graph Presented) Screening of the GSK corporate collection, some 1.9 million compounds, against Plasmodium falciparum (Pf), revealed almost 14000 active hits that are now known as the Tres Cantos Antimalarial Set (TCAMS). Followup work by Calderon et al.
Synthesis of novel 1, 3-Substituted 1 H-[1, 2, 4]-Triazole-3-Thiol derivatives
Eliazyan, Karine A.,Shahbazyan, Lusya V.,Pivazyan, Vergine A.,Ghazaryan, Emma A.,Yengoyan, Aleksandr P.
experimental part, p. 405 - 410 (2010/08/05)
By means of regioselective S-alkylation of 1 H-1, 2, 4-triazole-3-thiol (1), a series of S-substituted derivatives 2a-j were synthesized. In certain conditions, the reaction of 2 with arylsul-fochlorides, arylisocyanates, and quaternary ammonium salts of
Synthesis and antimycobacterial activity of 1,2,4-triazole 3-benzylsulfanyl derivatives
Klimesova, Vera,Zahajska, Lenka,Waisser, Karel,Kaustova, Jarmila,Moellmann, Ute
, p. 279 - 288 (2007/10/03)
Series of 3-benzylsulfanyl derivatives of 1,2,4-triazole and 4-methyl-1,2,4-triazole were synthesized by alkylation of starting triazole-3-thiol with appropriately substituted benzyl halide. All members of the set were evaluated for in vitro antimycobacte
Pharmaceutical use of N-Carbamoylazole derivatives
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Page 13, (2010/11/29)
The present invention relates to use of 1-carbamoylazole derivatives as medicaments and pharmaceutical compositions containing 1-carbamoylazole derivatives as the active ingredient, based on their DPPIV inhibiting effects. The present invention provides a dipeptidyl peptidase IV inhibiting agent comprising a compound represented by the general formula (I):
A Unified Approach to Systematic Isoesteric Substitution for Acidic Groups and Application to NMDA Antagonists Related to 2-Amino-7-phosphonoheptanoate
Chenard, B. L.,Lipinski, C. A.,Dominy, B. W.,Mena, E. E.,Ronau, R. T.,et al.
, p. 1077 - 1083 (2007/10/02)
A systematic approach to the replacement of acidic groups with potential bioisoesteres is described.The strategy involves simple nucleophilic displacement of a common alkyl halide precursor with a variety of mercaptoazoles and related molecules.The mercaptoazoles and their oxidized derivatives (sulfinyl- and sulfonylazoles) represent a series of possible surrogates for acidic groups which span a pKa range from about 4.5-11.5.This simple strategy was extended to include 2-hydroxy- or 2-aminothiophenyl groups which function as relatively nonacidic isoesteres for a phosphonic acid.By replacing the phosphonic acid of 2-amino-7-phosphonoheptanoate (AP-7) with these groups, we have synthesized novel N-methyl-d-aspartate (NMDA) antagonists.
Benzylsulfonyl diethylcarbamyl triazole and use as a selective herbicide
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, (2008/06/13)
The novel compound having the structural formula STR1 is disclosed, as well as its use by pre-emergent application to control noxious grasses and some broadleaf weeds in cool season crops such as rape, sugar beets and flax.
