Bioisosterism: a useful strategy for molecular modification and drug design
LM Lima, EJ Barreiro - Current medicinal chemistry, 2005 - ingentaconnect.com
… concept isosterism to design bioactive molecules, … biological activity of bioreceptor, whether
through agonist or antagonist actions. However, Friedman introduced the term bioisosterism …
through agonist or antagonist actions. However, Friedman introduced the term bioisosterism …
Bioisosterism in drug design
CA Lipinski - Annual Reports in Medicinal Chemistry, 1986 - Elsevier
… Peptide isosteres have been discussed in reviews on the rational design of peptide hormones
and neurotransmitters12 and conformational restrictions of biologically active peptides.13 …
and neurotransmitters12 and conformational restrictions of biologically active peptides.13 …
Bioisosterism: a rational approach in drug design
… biological activity has given rise to the term bioisosterism. As … have a similar type of biological
activity, which may even be … The critical component for bioisosterism is that bioisosteres …
activity, which may even be … The critical component for bioisosterism is that bioisosteres …
[PDF][PDF] The use of bioisosterism in drug design and molecular modification
PL Gaikwad, PS Gandhi, DM Jagdale, VJ Kadam - Am. J. PharmTech Res, 2012 - ajptr.com
… in drug design and lead optimization process as it may enhance the desired biological or …
parameters to obtain molecules having similar biological activity. Few of the popular examples …
parameters to obtain molecules having similar biological activity. Few of the popular examples …
[PDF][PDF] Input of isosteric and bioisosteric approach in drug design
… its biological activities, characterized as structure activity relationship (SAR) [14-15]. This
study of SAR is used in drug design … In summary, bioisosterism is a special process of rational …
study of SAR is used in drug design … In summary, bioisosterism is a special process of rational …
Bioisosterism in drug design: Identification of and structure-activity relationships in a series of glycine anilide ACAT inhibitors
WH Roark, J Padia, GL Bolton, CJ Blankley… - Bioorganic & Medicinal …, 1995 - Elsevier
… Abstract--To examine the effects of bioisosteric replacement on the biological activity of
our previously disclosed disubstituted urea inhibitors of the enzyme acyl-CoA:cholesterol …
our previously disclosed disubstituted urea inhibitors of the enzyme acyl-CoA:cholesterol …
Isosterism and molecular modification in drug design
CW Thornber - Chemical Society Reviews, 1979 - pubs.rsc.org
… concept of bioisosterism can be an aid to the design of such … (B) Whether the same or a
different biological activity results … may be suggestive to the drug designer, the idea is probably …
different biological activity results … may be suggestive to the drug designer, the idea is probably …
Structure-based Bioisosterism design, synthesis, biological activity and toxicity of 1, 2, 4-oxadiazole substituted benzamides analogues containing pyrazole rings
MT Tu, YY Shao, S Yang, BL Sun, YY Wang, CX Tan… - Molecules, 2022 - mdpi.com
… -linked 1,2,4-oxadiazoles were designed by means of bioisosterism. The preliminary bioassay
showed that most compounds exhibited good lethal activities against Mythimna separate, …
showed that most compounds exhibited good lethal activities against Mythimna separate, …
Synopsis of some recent tactical application of bioisosteres in drug design
NA Meanwell - Journal of medicinal chemistry, 2011 - ACS Publications
… bioisosterism given the similarities between the two isotopes, but there are circumstances in
drug design … to increased HLM stability but poor biological activity, attributed to the electron …
drug design … to increased HLM stability but poor biological activity, attributed to the electron …
Applications of bioisosteres in the design of biologically active compounds
NA Meanwell - Journal of Agricultural and Food Chemistry, 2023 - ACS Publications
… Bioisosterism is a principle exploited in the design of … design, some applications of the
sulfoximine functionality, the … BCP is a substructure in studies with biological activity or where the …
sulfoximine functionality, the … BCP is a substructure in studies with biological activity or where the …
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