コーパス検索結果 (1語後でソート)
通し番号をクリックするとPubMedの該当ページを表示します
1 er in DAT interaction than the corresponding bicyclics.
2 l)pyrazine 1h with sulfonyl azides to afford bicyclic 1,2,3-thiadiazoles 8 and 1,2,3-triazoles 9 conn
4 elimination, and C-C and P-H bond formation bicyclic 1-benzo-dihydrophosphetes (2) with PC(3) hetero
5 rs addressing nonprimed binding regions, and bicyclic 14-mer SFTI-1 analogues blocking both, primed a
6 ree, double cyclization for the synthesis of bicyclic 2-pyridones as peptidomimetics was developed.
7 isomerization, and lactamization, to furnish bicyclic 2-pyridones in up to 98% yield with retention o
11 nonretinoid RBP4 antagonists, represented by bicyclic [3.3.0]-octahydrocyclopenta[c]pyrrolo analogue
13 oadducts, which possess a basic structure of bicyclic 6-(menthyloxy)hexahydropyrano[4,3-c]pyrrol-7(6H
17 n of one substrate to give the corresponding bicyclic adduct in excellent yield at the gram scale.
19 (2) allowing the formation of functionalized bicyclic adducts in 55-91% isolated yields (18 products)
20 rming olefin to the bridgehead carbon of the bicyclic affect the efficiency and stereochemical outcom
23 or norbornadiene (NBD) readily generate the bicyclic alkyl-/alkenyl-substituted stannylenes, ArSn(no
24 trategy allows for the synthesis of storable bicyclic (alkyl)(amino)carbenes (BICAACs), which feature
27 by cyclization of the resulting urea to give bicyclic alpha-aryl hydantoin derivatives of substituted
29 ionship (3D-QSAR) studies of a new family of bicyclic alpha-iminophosphonates endowed with relevant a
31 odide (1a) catalyzes the ring opening of the bicyclic amidine system of DBU (1,8-diazabicyclo[5.4.0]u
32 sfully applied to the arylation of one spiro-bicyclic amine, a class of substrates that has not been
33 lactam starting materials as well as certain bicyclic amino acid products provided insight into their
36 lkyne analogue has been further converted to bicyclic and THF ring containing derivatives with a diff
38 D as halogenated C15-acetogenin 12-membered bicyclic and tricyclic ether bromoallene-containing mari
39 luding humulene (monocyclic); caryophyllene (bicyclic); and protoilludene, pentalenene, and isocomene
40 alent drugs, we have synthesized monocyclic, bicyclic, and tricyclic compounds containing 3 as an ele
41 t of furnishing unprecedented heterometallic bicyclic architectures with a high level of constitution
45 actions with different nucleophiles afforded bicyclic azasugars, cyclopropanated carbohydrate, dihydr
47 mechanisms of action, including a series of bicyclic azetidines that inhibit a new antimalarial targ
49 Here, we report a [3 + 3] ring expansion of bicyclic aziridines and rhodium-bound vinyl carbenes to
51 ation of synthetically useful chiral [3.1.0]-bicyclic aziridines with high diastereo- and enantiosele
52 ed, the reaction with phenols proceeds via a bicyclic aziridinium intermediate leading to the stereos
54 nstrating the unprecedented influence of the bicyclic backbone unsaturation for the preparation of th
59 ing isothiourea catalysts provided access to bicyclic beta-lactone-fused, N-heterocycles in moderate
60 of this donor results in the formation of a bicyclic beta-sulfonium ion that after addition of an al
61 inhibitors, particularly avibactam-like and bicyclic boronate compounds, have potential for treating
67 allographic results highlight the ability of bicyclic boronates to inhibit SBLs and MBLs via binding
69 coupled in a B-alkyl Suzuki reaction with a bicyclic bromoenone, which was a key intermediate for th
71 tion reactions were performed on a series of bicyclic C(2)-substituted pyranoside models to isolate a
73 nt and straightforward methodology to access bicyclic carbo- and heterocyclic scaffolds combining dif
74 ation into stereochemically dense, fused and bicyclic carbocycles containing transmutable functionali
75 antibiotics, beta-lactamase inhibitors, and bicyclic carbohydrate-beta-lactam monomers prepared by t
76 tanes as well as the construction of complex bicyclic carbon skeletons containing up to four contiguo
81 toisomer along with an unusual and uncolored bicyclic compound formed through an intramolecular photo
82 assay with seven human tumor cell lines, the bicyclic compounds inhibited selectively the growth of t
83 ation tactic for the construction of diverse bicyclic compounds possessing highly functionalized cycl
86 zolidines (BTZs) are carboxylate-containing, bicyclic compounds, considered as penicillin analogs wit
87 cally diverse structures, spanning mono- and bicyclic compounds, that either inhibited or activated M
89 lbenzenes 2 provides sulfonyl oxabenzo[3.3.1]bicyclic core 4 in a cosolvent of toluene and HOAc (v/v
90 ramolecular Heck reaction to build the fused bicyclic core and a cobalt-catalyzed peroxidation to ins
91 mits more comprehensive modifications of the bicyclic core and structure-activity relationship studie
92 and stereoselective formation of the [4.3.0] bicyclic core by incorporation of a symmetrizing geminal
94 yzed 5-exo-dig cycloisomerization provides a bicyclic core containing a methylenetetrahydrofuran moie
97 onist/delta-opioid receptor (DOR) antagonist bicyclic core peptidomimetics with promising analgesic a
98 lso demonstrated for the construction of the bicyclic core present in penostatin B in a concise and h
99 most known RiPPs, a tripeptide with a tight bicyclic core that appears to be cleaved from the middle
104 nic acids and gives access to functionalized bicyclic cyclopentenes, which can be converted into othe
106 s of several nitrogen nucleophiles to chiral bicyclic dehydroalanines have been assessed effectively
107 Salinamide A belongs to a rare class of bicyclic depsipeptide antibiotics in which the installat
108 talyst-free synthesis of nitrogen-containing bicyclic derivatives through a three-bond forming proces
111 due macrocycles, and three 11- to 14-residue bicyclic designs, are close to the computational models.
114 further intramolecularly cyclized into CF(3)-bicyclic dihydroanthracene derivatives ("helicopter"-lik
116 s were successfully achieved to afford fused bicyclic dihydropyridines in high yields (up to 94%) wit
117 pared in multigram quantities from the known bicyclic diketone 7 in four steps without the need for c
118 rticipation of remote esters through bridged bicyclic dioxacarbenium ions in organic solution in the
119 hosphate into a previously unknown 5,7-fused bicyclic diterpene, coined "pseudolaratriene." Combined
121 yclic N-heterocycle-fused beta-lactone and a bicyclic enamine derived from in situ decarboxylation of
122 loallene D as a pentahalogenated 12-membered bicyclic ether bromoallene was synthesized by a face-sel
124 t of the Al- by an Fe atom leads to a planar bicyclic frame with a terminal Al-O(*-) radical site, ac
125 onalized boronic acids to afford a cis-fused bicyclic framework containing an alpha,beta-unsaturated
127 The method allows for the rapid synthesis of bicyclic frameworks, generating all-carbon quaternary ce
128 sylation stereoselectivities for a series of bicyclic furanoside models have been carried out in the
129 one-pot approach to construct alpha-carbonyl bicyclic furans from easily accessible diynones is descr
130 ral information, we designed a new series of bicyclic G7 peptides that progressively constrain the st
133 A general synthetic strategy to cis-fused bicyclic gamma-butyrolactones via the retro-Diels-Alder
136 rofuran (THF) or tetrahydropyran (THP)-fused bicyclic gamma-lactones, two privileged scaffolds often
138 report a computational analysis of the [5,5] bicyclic guanidine-catalyzed asymmetric cycloaddition re
141 synthesis of a series of partially saturated bicyclic heteroaromatic scaffolds with enhanced sp(3) ch
142 eported on a number of structurally distinct bicyclic heteroarylsulfonamides as NaV1.7 inhibitors tha
144 The first syntheses of privileged [5,6]-bicyclic heterocycles, with ring-junction nitrogen atoms
146 mI2 -H2 O, provide straightforward access to bicyclic heterocyclic scaffolds containing bridgehead ni
147 occupy an "alkyl-induced" pocket and possess bicyclic hinge-binding motifs capable of forming more th
148 iomerically enriched fluorinated benzo-fused bicyclic homoallylic amines have been synthesized throug
149 The reaction of BCP-peroxy with NO produces bicyclic hydroxy nitrate with a branching ratio <0.2%, i
150 azines and biocatalytically generated chiral bicyclic imines selectively affords either tetracyclic p
152 ing from a common tetrahydrofuran-containing bicyclic intermediate and using the highly reactive brom
154 s it was later discovered that these bridged bicyclic intermediates can be trapped by various elimina
155 nsible for converting 8-oxogeranial into the bicyclic iridoid scaffold in a two-step reduction-cycliz
158 [3 + 2] cycloaddition can be used to obtain bicyclic isoxazolidines for which we report a set of rea
159 ne rearrangement of 2,4-cyclohexadienones to bicyclic ketones was found to proceed with high enantios
162 able by epoxidation of carboxamide-activated bicyclic lactam substrates derived from pyroglutamate us
163 esting results, including the formation of a bicyclic lactone arising from oxidative termination of t
165 stereoselectively a five-membered ring fused bicyclic lactone, the core structure present in gracilio
167 Through key structural modifications of a bicyclic lead, stepwise gains in spectrum of inhibition
168 aesthetically pleasing Fe-Pt heterometallic bicyclic metallacycles 6a and 6b, consisting of nine com
169 unctionalized hydrindanes, where the bridged bicyclic metallacyclopentenes from intramolecular [4 + 2
170 tion of rhodium-bound carbenes with strained bicyclic methylene aziridines results in a formal [3+1]
171 a bioinspired strain-driven ring opening of bicyclic methyleneaziridines to 2-amidopentadienyl catio
172 ouble bond of the allene to yield endocyclic bicyclic methyleneaziridines with excellent stereocontro
175 of Arabidopsis thaliana to a mixture of the bicyclic monoterpenes alpha-pinene and beta-pinene induc
177 owcased with stereoselective construction of bicyclic N-heterocycles, opens the door for future synth
178 ketones into all three topological types of bicyclic N-heterocycles: bridged, spiro-, and fused ring
179 logous amides for the efficient synthesis of bicyclic N-unprotected lactams similar to those in many
180 report identification of over 30 individual bicyclic naphthenic acids as the bicyclane hydrocarbons.
181 nimize the molecular weight to provide novel bicyclic next-generation PCSK9 inhibitor peptides such a
184 rculosis, there is now a renewed interest in bicyclic nitroimidazole scaffolds as a source of therape
187 T is especially noteworthy at high pH, where bicyclic nitroxyls are inhibited by formation of an oxoa
188 signatures consistent with conversion of the bicyclic norbornane repeat units into the ring-open isom
189 acene (TIPS-BP1') dimers utilizing a [2.2.1] bicyclic norbornyl bridge have been studied-primarily us
190 non-bile acid FXR agonists that introduce a bicyclic nortropine-substituted benzothiazole carboxylic
191 cked-nucleic-acid (LNA) or constrained-ethyl-bicyclic-nucleic-acid ((S)-cEt) modifications much more
193 1)-C(6) cyclization yields a highly strained bicyclic olefin whose surface chemistry was hitherto unk
195 cloadditions with carbonyl compounds to give bicyclic oxazolidine products in good overall yields.
196 tho-methoxycarbonylaryl isocyanates formed a bicyclic oxazolidinone, followed by a sequence of intram
197 philes displace one of the two bent bonds of bicyclic oxocarbenium ion intermediates in an antiperipl
198 e and metabolically stable nonphosphorylated bicyclic peptide as a potent and selective Pin1 inhibito
202 re, we determined the structure of the G7-B4 bicyclic peptide in complex with the Grb7-SH2 domain, bo
203 we report the crystal structure of a stapled bicyclic peptide inhibitor G7-B1 in complex with the Grb
205 silico rational design strategy to produce a bicyclic peptide to target the C-terminal region (residu
208 nce: This work demonstrates the potential of bicyclic peptides as a platform for the development of h
211 successfully developed for the selection of bicyclic peptides from large random-sequence libraries.
215 xample of a computational approach to design bicyclic peptides to target specific epitopes on disorde
216 al molecular insights into G4 recognition by bicyclic peptides via the precise positioning of amino a
217 e rapid tumor penetration characteristics of bicyclic peptides, coupled with high potency and chemica
219 egy was applied to generate a cell-permeable bicyclic peptidyl inhibitor against the NEMO-IKK interac
220 nolic compound or it can rearrange to form a bicyclic peroxy intermediate that subsequently undergoes
221 the effective production rates of phenol and bicyclic peroxy radical (BCP-peroxy) are experimentally
223 ived Salinospora sp. bacterium and contain a bicyclic phosphotriester core structure, which is a rare
225 on nucleophile with carbon dioxide to give a bicyclic product by P-CH(2) attack on CO(2) combined wit
228 r the preparation of both enantiomers of the bicyclic product with near-identical stereocontrol.
233 A prototropic shift leads to the observed bicyclic products in what can be viewed as an interrupte
235 ctrophilic activation of double bonds in the bicyclic products with m-CPBA is an efficient method for
236 moiety linked to the 4-position afforded the bicyclic products, which possess three stereogenic cente
240 Over the years, we have reported covalent bicyclic prolyl oligopeptidase inhibitors that were high
243 perative potency effects of the biphenylene, bicyclic pyrrolidine (Aoc), and methyl-threonine structu
246 inhibitors: cytochalasin B, a nine-membered bicyclic ring fused to a 14-membered macrocycle, which h
249 polynorbornene (VA-PNB), which has strained bicyclic ring repeat units along the polymer backbone.
250 ot all iridoids share the exact five- to six-bicyclic ring scaffold of the Catharanthus iridoids.
251 This transformation was further extended to bicyclic ring substrates, providing the opportunity to e
254 nt three-step synthesis of a series of fused bicyclic s-[1,2,4]triazolo[1,5-a]pyridines 1 was accompl
257 to the identification of multiple 5,6-fused bicyclic scaffolds that bind to the same allosteric tunn
258 of the newly synthesized 6,5- and 7,5-fused bicyclic scaffolds was then investigated to obtain vario
260 es a distinct approach for accessing [3.2.2] bicyclic scaffolds which are challenging to prepare thro
261 oriented synthesis of an array of cyclic and bicyclic scaffolds with polyhydroxylated appendages with
262 t, we described the optimization of a fused, bicyclic screening hit for potency, selectivity, and phy
263 ar reaction of a range of fused- and bridged-bicyclic secondary amines with a broad set of heteroaren
265 d allenes, which provides a distinct [4.2.1]-bicyclic skeleton containing two quaternary carbon cente
267 rally diverse scaffolds, ranging from simple bicyclic skeletons to complex polycyclic systems and nat
268 elded access to novel types of diastereopure bicyclic spiramycin derivatives containing tetrahydrofur
273 onverted into a conformationally constrained bicyclic structure through the formation of a pair of di
274 Despite the intrinsic constraints of the bicyclic structure, we demonstrate that their synthesis
275 ing of repeating units of fairly rigid fused bicyclic structures and alkenes separated by freely rota
277 termediates, which involves the formation of bicyclic structures from large Criegee intermediates con
279 recently described a nitroimidazopyrazinone bicyclic subclass with promising antitubercular and anti
280 reversible beta-hydride elimination from the bicyclic substituted aryl/alkyl stannylenes 2a or 2b and
281 , and biological characterization of a novel bicyclic-substituted hydroxyphenylmethanone 17beta-HSD2
283 someric quinolinone sulfonamide inhibitors [ Bicyclic sulfonamide compounds as sodium channel inhibit
285 database, Paquette's sultams (i.e., bridged bicyclic sultams with a bridgehead nitrogen atom) were o
286 nlocked the path to alternate monocyclic and bicyclic synthons representing the basis of a myriad of
287 pping from benzoxazine to chroman and indane bicyclic system followed by thiazole replacement on sulf
288 pansion of our approach, morphing the fused, bicyclic system into a novel monocyclic pyrimidinone sca
289 the 3-hydroxy-8-azabicyclo[3.2.1]octan-8-yl bicyclic system were potent (TTK IC50 < 10 nM, HCT116 GI
293 This resulted in a shift from our original bicyclic tetrahydroquinoline core to a monocyclic benzyl
296 to proceed through highly ordered cyclic or bicyclic transition states, leading to remarkable levels
297 perimentally unidentified class of condensed-bicyclic triazolo-thiadiazoles targeting PTP1B and its a