Sepehri, Nima; Iraji, Aida; Yavari, Ali; Asgari, Mohammad Sadegh; Zamani, Saeed; Hosseini, Samanesadat; Bahadorikhalili, Saeed; Pirhadi, Somayeh; Larijani, Bagher; Khoshneviszadeh, Mahsima; Hamedifar, Halleh; Mahdavi, Mohammad; Khoshneviszadeh, Mehdi published the artcile< The natural-based optimization of kojic acid conjugated to different thio-quinazolinones as potential anti-melanogenesis agents with tyrosinase inhibitory activity>, Category: pyridine-derivatives, the main research area is kojic acid thio quinazolinone mol docking antimelanogenesis tyrosinase inhibition; Cytotoxicity; Hyperpigmentation; Kojic acid; Quinazolinone; Tyrosinase inhibitor.
Melanin pigment and melanogenesis are a two-edged sword. Melanin has a radioprotection role while melanogenesis has undesirable effects. Targeting the melanogenesis pathway, a series of kojyl thioether conjugated to different quinazolinone derivatives I (R = c-Pr, Ph, 2-pyridyl, etc.) were designed, synthesized, and evaluated for their inhibitory activity against mushroom tyrosinase. All the synthesized compounds were screened for their anti-tyrosinase activity and all derivatives displayed better potency than kojic acid as the pos. control. In this regard, compounds I (R = pyridin-2-ylmethyl) and I (R = 2-pyridyl) the most active compounds showed an IC50 value of 0.46 and 0.50μM, resp. In kinetic evaluation against tyrosinase, I (R = pyridin-2-ylmethyl) depicted an uncompetitive inhibition pattern. Designed compounds also exhibited mild antioxidant capacity. Moreover, compounds I (R = pyridin-2-ylmethyl) and I (R = 2-pyridyl) achieved good potency against the B16F10 cell line to reduce the melanin content, while showing limited toxicity against malignant cells. The proposed binding mode of new inhibitors evaluated through mol. docking was consistent with the results of structure-activity relationship anal.
Bioorganic & Medicinal Chemistry published new progress about Amines Role: RCT (Reactant), RACT (Reactant or Reagent). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Category: pyridine-derivatives.