Synthesis and Biological Activity of Chiral Dihydropyrazole: Potential Lead for Drug Design

X.-H.      Liu; B.-F.      Ruan; J.      Li; F.-H.      Chen; B.-A.      Song; H.-L.      Zhu; P.      S. Bhadury; J.      Zhao

doi:10.2174/138955711796355285

Abstract

Dihydropyrazole, a small bioactive molecule, is a prominent structural motif found in numerous pharmaceutically active compounds. The chiral dihydropyrazole structure has been demonstrated to bear important biological activities such as anticancer, antimicrobial, antimalarial, antinociceptive, antiviral, antitubercular, antiinflammatory, anticonvulsant and steroidal, and can also act as MAO inhibitors, CB1 receptor antagonists and nitric oxide synthase inhibitors. The review describes the latest advances in the synthesis of dihydropyrazole derivatives incorporating physiologically active substances. It is the first attempt at a general and systematic account of the extensive literature data on this subject.

Keywords: Dihydropyrazole, biological activities, SAR, lead, Cannabinoid Receptor 1, Monoamine Oxidase, Structure Activity Relationship, Human Promyelocytic Leukemia, Mouse Lymphoma, Human Prostate Cancer, Human Epidermoid Carcinoma Cancer, T Lymphocytic Leukemia, Human Gastric Cancer, Hman Lukemic Lmphoblasts, Human Myeloma, National Cancer Institute, Epidermal Growth Factor Receptor, Minimum Inhibitory Concentrations, Human Breast Adenocarcinoma, 3-(4,5-Dimethyl-2-Thiazyl)-2,5-Diphenyl-2H-Tetrazolium Bromide, Dimethyl Sulfoxide, Mueller-Hinton, Phosphate Buffered Saline, Enzymelinked Immunosorbentassy, Tlomere Rpeat Aplification Potocol