Herein, we used bicyclo [1.1.1] pentane a benzene bioisostere as a replacement for these phenyl groups. In total, seven analogous 1a, 1b, 1c, 2a, 2b, 2c, and 3 were designed and investigated theoretically. Their drug-likeness, physicochemical properties, bioactivity, and pharmacokinetics ...
4-oxazolin-2-onealpha-bromoketonecyclizationherbicidebiological isostereThe reaction of semicarbazones of 3,5-diphenylcyclohex-2-enone 2 and 3,5-diphenyl... DB Reddy,AS Reddy,V Padmavathi - 《Journal of Chemical Research Synopses》 被引量: 31发表: 1998年 Synthesis of 3,3′- di-2-pyrony...
The other as the bioisostere of 1,3,4-thiadiazole, to sulfur Lawesson's reagent followed by ucsyicnligzaPt2ioSn536anandddethhyioduroresau3l7f.uTrihziaotinoantiwonasorfepacoyrtlehdydtorapzriondeus cbey1t,h3,e4-trtheaiatdmiaeznotloesf in good yields38,39. Recently, there has been ...
A Convenient Preparation of (2SR,3S)-3-Amino-2-hydroxy-4-phenylbutanoic Acid; an Important Peptide Bond Isosteredoi:10.1080/00397919908086259We present an efficient synthesis of N-Z-(2SR,3S)-3-amino-2-hydroxy-4-phenylbutanoic acids by hydroxylation of an enolate derived from methyl (3S)-N...
The title compounds (14a,b) were 5' epimers of a derivative of a phosphonate isostere of ATP in which the CH2OP alpha system of ATP was replaced by CH(R)CH... F Kappler,TT Hai,RJ Cotter,... - 《Journal of Medicinal Chemistry》 被引量: 45发表: 1986年 Reaction of o-carboxyphenyl...
货号(SKU)包装规格是否现货价格数量 T670981-1mg 1mg期货 原价:¥2,999.90 +- 大包装询价添加到收藏夹比较SDS中文版DATASHEET Skip to the end of the images gallery Skip to the beginning of the images gallery 基本描述 别名替利那韦 英文别名Telinavir | (Hydroxyethyl)urea Isostere deriv. 11 | Tel...
Recently, we reported a novel substrate-based octapeptide BACE1 inhibitor KMI-008 containing hydroxymethylcarbonyl (HMC) isostere as a transition-state mimic. Using KMI-008 as a lead compound, a small-sized and highly potent BACE1 inhibitor KMI-370 (IC50=3.4 nM) was designed and synthesized. Gr...
Here, we show the design, synthesis, and validation of its new saturated bioisostere with improved physicochemical properties 2-oxabicyclo[2.2.2]octane. The design of the structure is based on the analysis of the advantages and disadvantages of the previously used bioisosteres: bicyclo[1.1.1]...
2 R-Benzyl-5 S- tert-butoxycarbonylamino-4 R-( tert-butyldimethylsilanyloxy)-6-phenyl-hexanoic acid, a hydroxyethylene dipeptide isostere corresponding to Phe–Phe, has been synthesized in a practical, stereocontrolled fashion from ( l)-phenylalanine....
SUBSTITUTED 2-PHENYL-2- (PYRIDYLOXY) -ETHYLAMINE AND ISOSTERE COMPOUNDS METHOD FOR THE PRODUCTION AND USE THEREOFCompounds of the formula wherein one of R1 and R2 is hydrogen, halogen, methyl, methoxy, amino or nitro and the other is hydrogen; or R1 and R2 are both halogen; R3 is ...