138775-02-7Relevant academic research and scientific papers
Solid-phase synthesis and biological evaluation of piperazine-based novel bacterial topoisomerase inhibitors
Felding, Jakob,Flagstad, Thomas,Givskov, Michael,Jakobsen, Tim H.,Nielsen, Thomas E.,Pedersen, Mette T.,Qvortrup, Katrine,Tolker-Nielsen, Tim
, (2021/12/24)
There is an emerging global need for new and more effective antibiotics against multi-resistant bacteria. This situation has led to massive industrial investigations on novel bacterial topoisomerase inhibitors (NBTIs) that target the vital bacterial enzym
SAR studies on a series of N-benzyl-4-heteroaryl-1-(phenylsulfonyl) piperazine-2-carboxamides: Potent inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus
Gentles, Robert G.,Ding, Min,Zheng, Xiaofan,Chupak, Louis,Poss, Michael A.,Beno, Brett R.,Pelosi, Lenore,Liu, Mengping,Lemm, Julie,Wang, Ying-Kai,Roberts, Susan,Gao, Min,Kadow, John
scheme or table, p. 3142 - 3147 (2011/06/24)
Described herein is the initial optimization of (+/-) N-benzyl-4- heteroaryl-1-(phenylsulfonyl)piperazine-2-carboxamide (1), a hit discovered in a high throughput screen run against the NS5B polymerase enzyme of the hepatitis C virus. This effort resulted in the identification of (S)-N-sec-butyl-6-((R)-3- (4-(trifluoromethoxy)benzylcarbamoyl)-4-(4-(trifluoromethoxy)phenylsulfonyl) piperazin-1-yl)pyridazine-3-carboxamide (2), that displayed potent replicon activities against HCV genotypes 1b and 1a (EC50 1b/1a = 7/89 nM).
FARNESYL PROTEIN TRANSFERASE INHIBITORS
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Page/Page column 31-32, (2010/02/11)
Disclosed are compounds of formula (1.0), wherein R represents a cyclic moiety to which is bound an imodazolylalkyl group; R represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.
Piperazine compounds as inhibitors of MMP or TNF
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, (2008/06/13)
A compound of formula (I) wherein A is a sulfonyl or a carbonyl; R1is an optionally substituted aryl, an optionally substituted heterocyclic group, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; R2is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R3is an optionally substituted lower alkyl, an optionally substituted lower alkoxy, an optionally substituted aryloxy, an optionally substitued lower alkenyl, an optionally substituted aryl, an optionally substituted heterocyclic group or an optionally substitued amino; R4is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; R5is a hydrogen, an optionally substituted lower alkyl, an optionally substituted aryl or an optionally substituted heterocyclic group; and R10is a hydroxy or a protected hydroxy, and a pharmaceutically acceptable salt thereof. The compound of the present invention is useful as a medicament for prophylactic and therapeutic treatment of MMP- or TNFα-mediated diseases.
