Sentence examples for modification of lead from inspiring English sources
Pyrroloazepinones 8a j and 9a j were designed by structural modification of lead compound 3.
Indolones 4 and 5, and indolyl-aminoacids 6a e, 7a e, and 8a and 8b were designed by structural modification of lead compound 3.
Our extensive chemical modification of lead compound 2 successfully led to fluoropyridine analogs 7j and 1 with improved in vivo antagonistic activities.
Modification of lead compound 7 by transformation of its N-oxide 6 6 biaryl ring system and fused aromatics produced a series of non-basic fXa inhibitors with excellent potency in anti-fXa and anticoagulant assays.
The C-4 side chain modification of lead compound 1 has resulted in the identification of a potent and selective Candida albicans N-myristoyltransferase (CaNmt) inhibitor RO-09-4609, which exhibits antifungal activity against C. albicans in vitro.
The chemical modification of lead compound 1, focusing on the N-substituent, was carried out to further improve the free scavenging ability.
Study of the properties of approved drug structures in the 1990's led to the concept of a restricted range of physicochemical parameters that appeared optimal for orally administered drugs many researchers have used the 'rule of five' as a guide for 'drug-like' compounds during screening and structure modification of leads to optimise their potency, metabolism and exposure.
Analysis of molecular dynamics simulations provided important guidelines for the further modification of the lead compounds.
The study provides insight into the binding mechanism of HAPs-HBV and would be useful for the rational design and modification of new lead compounds of HAP drugs.
Chemical modification of the lead structures showed that the structure activity relationship profiles for both of these series were dependent on the electronic properties of the molecules.
Finally, a 3D-QSAR study was carried out using Comparative Molecular Field Analysis (CoMFA), aiming to deduce rational guidelines for the further structural modification of these lead compounds.
