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Bioisosterism: a useful strategy for molecular modification and drug design.
This review aim to demonstrate the role of bioisosterism in rational drug design as well as in the molecular modification and optimization process aiming to improve pharmacodynamic andExpand
Synthesis and analgesic activity of novel N-acylarylhydrazones and isosters, derived from natural safrole.
The NAH compounds described herein were structurally planned by molecular hybridization and classical bioisosterism strategies on previously reported analgesic NAH in order to identify the pharmacophoric contribution of the N-acylarylhydrazone moiety and investigate the structure-activity relationship (SAR) in these series. Expand
Synthesis and anti-inflammatory activity of phthalimide derivatives, designed as new thalidomide analogues.
In these series, compound 3e (LASSBio 468), having a sulfonyl-thiomorpholine moiety, showed potent inhibitory activity on LPS-induced neutrophil recruitment with ED(50)=2.5mg kg(-1), which was correlated with its inhibitory effect on TNF-alpha level. Expand
Selective activity against Mycobacteriumtuberculosis of new quinoxaline 1,4-di-N-oxides.
The potency, low cytotoxicity and selectivity of these compounds make them valid lead compounds for synthesizing new analogues, particularly compound 7-methyl-3-(4'-fluoro)phenylquinoxaline-2-carbonitrile 1,4-di-N-oxide (MIC <0.2 microg/mL and SI > 500). Expand
Novel 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors.
The biological data obtained proved the potential of 2-chloro-4-anilino-quinazoline derivatives as EGFR and VEGFR-2 dual inhibitors and demonstrated the importance of a hydrogen bond donor at the para position of the aniline moiety for interaction with conserved Glu and Asp amino acids in EGFRs binding sites. Expand
Design, synthesis, and pharmacological evaluation of novel hybrid compounds to treat sickle cell disease symptoms.
These compounds are novel lead drug candidates with multiple beneficial actions in the treatment of sickle cell disease symptoms and offer an alternative to hydroxyurea treatment. Expand
Discovery of new orally effective analgesic and anti-inflammatory hybrid furoxanyl N-acylhydrazone derivatives.
The success in the exploitation of hybridization strategy for identification of novel N-acylhydrazones (NAH) with optimized activities was confirmed and the lack of mutagenicity of the active derivatives 17, 31, and 42, allow them as candidates for further clinical studies. Expand
Synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazones, designed as cruzain inhibitors candidates.
In this paper, we report the structural design, synthesis, trypanocidal activity and docking studies of novel quinoxaline-N-acylhydrazone (NAH) derivatives, planned as cruzain inhibitors candidates,Expand
Hybrid furoxanyl N-acylhydrazone derivatives as hits for the development of neglected diseases drug candidates.
The adequate stability, in simulated biological system and plasma, and the lack of mutagenicity of these derivatives allow us to propose them as candidates for further pre-clinical studies. Expand
Therapeutic potential of a new phosphodiesterase inhibitor in acute lung injury
Agent that inhibit phosphodiesterase 4 and 5 simultaneously may be a useful adjunct therapy for acute lung injury and modulated the lung inflammatory process and had the potential to block fibroproliferation. Expand