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1  found that the amide can be replaced with a bioisosteric 1,3,4-oxadiazole with improved potency.
2 indolin-2-ones, which were superseded by the bioisosteric 2-(1H-indazol-6-yl)spiro[cyclopropane-1,3'-
3 )indolin-2-ones, which are superseded by the bioisosteric 2-(1H-indazol-6-yl)spiro[cyclopropane-1,3'-
4                                  A series of bioisosteric 4-(aminomethyl)-1-hydroxypyrazole (4-AHP) a
5 ctional groups, such as -OH, -NH(2), and the bioisosteric 5-substituted indole moiety in both di and
6                                            A bioisosteric amide to ester substitution yielded a serie
7                       We hypothesized that a bioisosteric amide-to-ester substitution could lead to i
8                                  The 3-amino bioisosteric analogues (40 and 41) displayed reasonably
9 derivatives (i.e., 7 and 8) were designed as bioisosteric analogues based on the phenol prototype 4.
10              Compounds 6 and 7 are potential bioisosteric analogues of gamma-aminobutyric acid (GABA)
11 es of a key intermediate in the synthesis of bioisosteric analogues of the angiotensin II receptor bl
12 thalen-2- ol further to include heterocyclic bioisosteric analogues.
13  excretion) were substantially improved by a bioisosteric approach.
14 he recently discovered hydroxamic acids, all bioisosteric attempts to replace the carboxylic acid of
15 e indole molecular core was replace with the bioisosteric benzofuran or benzothiophene ring systems,
16  aim for high selectivity by introducing the bioisosteric (BIS) concept, a widely used drug design st
17 that mimics p-benzene-based moieties using a bioisosteric (BIS) strategy on pacs, trans-1,3-cyclobuta
18 2e(-) chemistry) to a range of underexplored bioisosteric building blocks.
19 y reported BIBR1591 were conducted to obtain bioisosteric candidates with improved activities.
20 urring antibiotic heronapyrrole C carrying a bioisosteric carboxylate in place of the nitro group, wa
21 tional approach of modulation/replacement of bioisosteric chemical groups, which allowed us to identi
22 cially available thiols are divided into 231 bioisosteric clusters, whose compositions agree at least
23  synthetic strategies for the preparation of bioisosteric compounds is a demanding undertaking in med
24 and the reliance on the isatin moiety as key bioisosteric contributors.
25                                              Bioisosteric deaza analogues of 6-methyl-9-beta-D-ribofu
26 ptimization campaign by synthesizing various bioisosteric derivatives.
27 s with sulfoximines to achieve a synergistic bioisosteric design.
28 acement of the benzophenone carboxylate with bioisosteric equivalents could lead to potent analogues.
29 placed with a higher selenium atom (9f) or a bioisosteric ethenyl group (9h) retained potency.
30                                              Bioisosteric H/F or CH(2)OH/CF(2)H replacement was intro
31 e NK3R antagonist chemotype achieved through bioisosteric lead change from the high-throughput screen
32 orus compounds were synthesized as potential bioisosteric mimics of peptide alpha-ketoesters and alph
33 haracterization of bicyclic analogues of the bioisosteric non-opioid analgesics Flupirtine and Retiga
34                                    For these bioisosteric pairs, 1/4 and 6/5, the sulfamate compound
35 and predictive in silico evaluation of their bioisosteric potential, with validation provided by in v
36 imulates SERCA2a, we synthesized a series of bioisosteric PST3093 analogues devoid of Na(+)/K(+) ATPa
37 further modifications to the trifluoroethoxy bioisosteric replacement allowed rebalancing of properti
38              For this purpose, the effect of bioisosteric replacement and the role of flexibility hav
39               To address this, we utilized a bioisosteric replacement approach to synthesize phenylbo
40 ators is prone to rapid glucuronidation, its bioisosteric replacement by an indazole was envisaged.
41              We applied scaffold hopping and bioisosteric replacement concepts to eliminate unwanted
42 nd a molecular size that makes it a targeted bioisosteric replacement for phenylene and acetylene gro
43 moiety proved to be a suitable non-classical bioisosteric replacement for the higher halogen-pai aryl
44 oxy) with a fluorine atom is a commonly used bioisosteric replacement in medicinal chemistry.
45 t of bioisosterism and the implementation of bioisosteric replacement is fundamental to medicinal che
46                           In particular, the bioisosteric replacement of a metabolically sensitive te
47 , this study represents the first example of bioisosteric replacement of an acetate group by a spirob
48 tracted considerable recent attention is the bioisosteric replacement of aromatic rings, internal alk
49 tif has increasingly received attention as a bioisosteric replacement of benzene rings due to its abi
50 c elaboration and exciting opportunities for bioisosteric replacement of hydroxyl with fluorine in na
51                                              Bioisosteric replacement of one of the phenyl rings of t
52  More specifically, the best changes involve bioisosteric replacement of one of the two phenyl rings
53 rs into drug candidates, thus enabling ideal bioisosteric replacement of ortho-, meta- and para-subst
54 f these novel antiviral compounds, including bioisosteric replacement of the 4H-thieno[3,2-b]pyrrole
55                                        Thus, bioisosteric replacement of the 5-guanidine with an acet
56                                              Bioisosteric replacement of the acrylic acid to overcome
57                                            A bioisosteric replacement of the alpha-ketoamide moiety o
58      The key structural changes to 1 include bioisosteric replacement of the amide with oxadiazole an
59  such as alpha-alkylation, homologation, and bioisosteric replacement of the aminoguanidine all were
60                                              Bioisosteric replacement of the aromatic phenyl group by
61 oieties connected to the piperazine ring and bioisosteric replacement of the aromatic tetralin moieti
62 imidine-5-carboxylates (16) were designed by bioisosteric replacement of the carbonyl group at positi
63   Series of compounds were generated via the bioisosteric replacement of the carboxylate of 4-ACPCA (
64           Herein, we report the results from bioisosteric replacement of the carboxylic acid group of
65                                  We explored bioisosteric replacement of the drug's carboxylate motif
66 eptide conjugation based on the nonclassical bioisosteric replacement of the guanidine group in argin
67 ge urinary incontinence (UUI), we found that bioisosteric replacement of the N-cyanoguanidine moiety
68  computer-assisted design was focused on the bioisosteric replacement of the N1 atom by a CH group in
69 tides was prepared with a major focus on the bioisosteric replacement of the original methionine resi
70                                              Bioisosteric replacement of the original thiazole guanid
71 Analogue 23 containing a thiophene ring as a bioisosteric replacement of the phenyl ring Ar(1) displa
72                                      Initial bioisosteric replacement of the pyrophosphate linkage ab
73 eration of utrophin modulators, based on the bioisosteric replacement of the sulfone group with a pho
74                                              Bioisosteric replacement of this biaryl moiety by arylpi
75  to support more informed decision-making in bioisosteric replacement selection in drug design and in
76 bioisostere, which could be of importance in bioisosteric replacement strategies for future ligand de
77 terature referring to a variety of different bioisosteric replacement strategies, ranging from simple
78 IC(50): 0.13-0.37 muM) were designed using a bioisosteric replacement strategy and proved to be effec
79     Here, we report a further study of amide bioisosteric replacement with a variety of azoles contai
80 sed on their diversification potential using bioisosteric replacement.
81 ize a lead molecule for further development, bioisosteric replacements are generally adopted as one o
82 eliberates on the design and applications of bioisosteric replacements for a phenyl ring that have pr
83 mplished by use of aza-amino acids, that are bioisosteric replacements for alpha-amino acids that per
84 y are often used with the intention of being bioisosteric replacements for ester and amide functional
85                  A systematic exploration of bioisosteric replacements for furan and thiophene cores
86 we evaluated 7-fluoro-substituted indoles as bioisosteric replacements for the 7-azaindole scaffold o
87 covered that these compounds can function as bioisosteric replacements for the corresponding WIN 35,0
88 ple substitution, single atom mutations, and bioisosteric replacements for the guanidine and carboxyl
89  effort has focused on the identification of bioisosteric replacements for the usual oxazolidinone A-
90                                        While bioisosteric replacements have been extensively investig
91 ed, capabilities to undertake more ambitious bioisosteric replacements have emerged.
92 tantly, we used novel CF(3)-alkoxy groups as bioisosteric replacements of a fluorinated phenyl ring a
93 il the potential of aromatic azaborinines as bioisosteric replacements of naphthalene in drug discove
94 nsporter (VAChT) inhibitor analogues through bioisosteric replacements of piperidine with azetidine m
95            They have found particular use as bioisosteric replacements of several heteroatomic functi
96            Prostaglandin E analogs involving bioisosteric replacements of the carboxyl group, such as
97 iological evaluation of topologically based, bioisosteric replacements of the quinoxaline moiety in t
98 cyclic oxocarbanion derivatives as potential bioisosteric replacements of ureas and related functiona
99 ed physicochemical profiles of C(sp(3))-rich bioisosteric scaffolds relative to arenes.
100 ly convert, or "scaffold hop", between these bioisosteric subclasses through single-atom skeletal edi
101 compound properties is contextual in nature, bioisosteric substitution can lead to enhanced potency,
102                                        Using bioisosteric substitution methods, here, we report the i
103 tuents in the 4, 4', or 5' positions and the bioisosteric substitution of the distal carboxylic acid
104 paper examines the relative effectiveness of bioisosteric sulfamate and sulfamide derivatives for inh
105 -chain 5-hydroxy-1,2,3-triazoles potentially bioisosteric to hydroxamic acids.
106         To this end, cyclizations, which are bioisosteric to the lactam-type side-chain to side-chain
107  peptidic small molecules bearing natural or bioisosteric unnatural amino acids.
108 h that the tricyclic naphthofuran nucleus is bioisosteric with, and directly superimposable upon, the

 
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