63177-38-8Relevant academic research and scientific papers
Myma bioactivated thioalkylbenzoxazole prodrug family active against mycobacterium tuberculosis
Moure, Abraham L.,Narula, Gagandeep,Sorrentino, Flavia,Bojang, Adama,Tsui, Clement K. M.,Sao Emani, Carine,Porras-De Francisco, Esther,Díaz, Beatriz,Rebollo-López, María José,Torres-Gómez, Pedro Alfonso,López-Román, Eva María,Camino, Isabel,Casado Castro, Patricia,Guijarro López, Laura,Ortega, Fátima,Ballell, Lluis,Barros-Aguirre, David,Remui?án Blanco, Modesto,Av-Gay, Yossef
, p. 4732 - 4748 (2020)
Screening of a GSK-proprietary library against intracellular Mycobacterium tuberculosis identified 1, a thioalkylbenzoxazole hit. Biological profiling and mutant analysis revealed that this compound is a prodrug that is bioactivated by the mycobacterial enzyme MymA. A hit-expansion program including design, synthesis, and profiling of a defined set of analogues with optimized drug-like properties led to the identification of an emerging lead compound, displaying potency against intracellular bacteria in the low micromolar range, high in vitro solubility and permeability, and excellent microsomal stability.
Antiprotozoal activity of bicyclic diamines with a N-methylpiperazinyl group at the bridgehead atom
Faist, Johanna,Seebacher, Werner,Kaiser, Marcel,Brun, Reto,Saf, Robert,Weis, Robert
, p. 4988 - 4996 (2013/09/02)
ω-Aminoacyl and -alkyl derivatives of 4-(4-methylpiperazin-1-yl) bicyclo[2.2.2]octan-2-amines and of 5-(4-methylpiperazin-1-yl)-2-azabicyclo[3.2. 2]nonanes were prepared and their activities were examined in vitro against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). Some of the newly synthesized compounds showed very promising antiprotozoal activity and selectivity. A few of the alkylamino-2-azabicyclo[3.2.2]nonanes exhibited high antiplasmodial activity, whereas a single bicyclo[2.2.2]octane derivative was the most potent antitrypanosomal compound. The results of the newly synthesized compounds were compared with the activities of already synthesized compounds and of drugs in use. Structure-activity relationships were discussed.
Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity
Faist, Johanna,Seebacher, Werner,Kaiser, Marcel,Brun, Reto,Saf, Robert,Weis, Robert
experimental part, p. 6796 - 6804 (2010/10/20)
Dialkylaminoalkyl derivatives of 2-azabicyclo[3.2.2]nonanes and of bicyclo[2.2.2]octanes were prepared and their activities determined in vitro against the multiresistant K1 strain of Plasmodium falciparum. Several of the new compounds exhibited very promising antiplasmodial activity and selectivity. The results were compared to those of formerly synthesized analogues and of drugs in use. Structure-activity relationships were detected. Some of the more potent compounds were tested in vivo against Plasmodium berghei showing weak to moderate activity. A single compound was able to increase the mean survival days of infected mice.
Compositions of matter D-hetero-1,1-(α-thiocyanoacetyl) compounds
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, (2008/06/13)
This invention discloses new chemical compositions of matter having the formula: STR1 wherein A is a saturated or mono unsaturated aliphatic hydrocarbon chain having from 3 to 7 carbon atoms which optionally contains a maximum of three substituents selected from the group consisting of alkyl, alkoxy and halogen; and n is an integer from 1 to 3. This invention further discloses an insecticidal and fungicidal composition which comprises an inert carrier and, as an essential active ingredient, in a quantity toxic to insects and fungi, a compound of the above description; and a method for the control of insects and fungi which comprises applying to the locus of said insects or fungi an insecticidal and fungicidal composition heretofore described.
