2-Arylacetamido-4-phenylamino-5-substituted pyridazinones as formyl peptide receptors agonists

2-Arylacetamido-4-phenylamino-5-substituted pyridazinones as formyl peptide receptors agonists.

N-Formyl peptide receptors (FPRs: FPR1, FPR2, and FPR3) are G protein-coupled receptors that play key roles in modulating immune cells. FPRs represent potentially important therapeutic targets for the development of drugs that could enhance endogenous anti-inflammation systems associated with various pathologies, thereby reducing the progression of inflammatory conditions. Previously, we identi...

Evaluation of novel 1-(4-(substituted)piperazin-1-yl)- 2-(phenylamino)ethanone derivatives as Falcipain-2 inhibitors

Background: Malaria, an infectious disease transmitted by mosquitoes, has affected the world since the beginning of recorded human history and it remains an ensconced global health challenge even today. Among the various proteases, expressed in the life cycle of parasite, cysteine protease falcipain-2 plays a pivotal role in parasite food assimilation and inhibition of this protease cause delet...

Microbial Infection Prevent Development of Severe Sepsis after The Agonists of Formyl Peptide Receptors

Gastrin-releasing peptide/neuromedin B receptor antagonists PD176252, PD168368, and related analogs are potent agonists of human formyl-peptide receptors.

N-Formyl peptide receptors (FPRs) are G protein-coupled receptors (GPCRs) involved in host defense and sensing cellular dysfunction. Thus, FPRs represent important therapeutic targets. In the present studies, we screened 32 ligands (agonists and antagonists) of unrelated GPCRs for their ability to induce intracellular Ca²+ mobilization in human neutrophils and HL-60 cells transfected with human...

Synthesis, Characterization and Study of Some N-Substituted Aryl-2- ({4-[(Substituted Aryl Carbamoyl) Methyl]-5-(Pyridin-4-yl)-4H-1, 2, 4-Triazol-3-yl} Sulfanyl) Acetamide

Pathogenic infections and inflammation are very common ailments humans suffer. Upsurge of resistant pathogens has impeded the antimicrobial drug development process in recent years and the search of new antimicrobial agents is clearly evident from the literature. In line with these developments the synthesis of N-substituted aryl-2-({4-[(substituted aryl carbamoyl) methyl]-5-(pyridin-4-yl)-4H-1...