SAR of novel benzothiazoles targeting an allosteric pocket of DENV and ZIKV NS2B/NS3 proteases

2-Sulfonylpyrimidines as Privileged Warheads for the Development of S. aureus Sortase A Inhibitors

“…Fluorometric assays of the ZIKV/DENV NS2B/NS3 protease were performed as described previously ( Maus et al, 2021 ). The assay was carried out in triplicates at 25°C in assay buffer (50 mM Tris, pH 9.0, 20% glycerol (v/v), and 1 mM CHAPS).…”

Seeking heterocyclic scaffolds as antivirals against dengue virus

“…Maus et al (2021) investigated several new benzothiazole scaffolds to target the allosteric pocket of the DENV NS2B/NS3 protease [ 184 ]. The authors synthesized several sequences of Y-shaped benzothiazole scaffolds, but only a few of them, 127 – 129 ( Table 23 ), displayed promising inhibition activity against the DENV.…”

Synthesis and Antimicrobial, Anticancer and Anti-Oxidant Activities of Novel 2,3-Dihydropyrido[2,3-d]pyrimidine-4-one and Pyrrolo[2,1-b][1,3]benzothiazole Derivatives via Microwave-Assisted Synthesis

“…Pyrido [2,3-d]pyrimidine ring systems have assorted biological and pharmacological activities such as being analgesic, anti-inflammatory [1-3], antitubercular [4], antimicrobial [5][6][7], a threonine tyrosine kinase (TTK) inhibitor [8], an adenosine kinase inhibitor [9], antiviral [10], antioxidant [11][12][13][14], a dihydrofolate reductase inhibitor [15,16], and an efficient glucosidase inhibitor [17,18]. Moreover, the 1,3-benzothiazole nucleus is a highly significant scaffold in the drug design, due to important pharmacological and medicinal activities, such as being antiviral [19], antituberculosis [20], an identifier of selective CB2 receptor ligands [21], antitumor [22][23][24], antimicrobial [25][26][27], anticonvulsant [28], a schistosome BCL-2 inhibitor [29], antidiabetic [30], antioxidant [31], an anti-Alzheimer drug [32] and a urease inhibitor [33] among the heterocyclic compounds containing a pyrimidine and benzothiazole nucleus that exhibits biological activity [34][35][36] (Figure 1). kinase (TTK) inhibitor [8], an adenosine kinase inhibitor [9], antiviral [10], antioxidant [11][12][13]…”

“…kinase (TTK) inhibitor [8], an adenosine kinase inhibitor [9], antiviral [10], antioxidant [11][12][13][14], a dihydrofolate reductase inhibitor [15,16], and an efficient glucosidase inhibitor [17,18]. Moreover, the 1,3-benzothiazole nucleus is a highly significant scaffold in the drug design, due to important pharmacological and medicinal activities, such as being antiviral [19], antituberculosis [20], an identifier of selective CB2 receptor ligands [21], antitumor [22][23][24], antimicrobial [25][26][27], anticonvulsant [28], a schistosome BCL-2 inhibitor [29], antidiabetic [30], antioxidant [31], an anti-Alzheimer drug [32] and a urease inhibitor [33] among the heterocyclic compounds containing a pyrimidine and benzothiazole nucleus that exhibits biological activity [34][35][36] (Figure 1). Accordingly, with all of the previous observations of the biological importance and in continuation of our program in the synthesis of pyrido [2,3-d]pyrimidine [37], this study aims to design and develop highly selective and efficacious antimicrobial and anticancer agents of a novel series of pyrido [2,3-d]pyrimidine derivatives bearing different heterocyclic and aryl moieties such as benzothiazole, thiophene, furan, piperonal, naphthalene, and fluorophenyl as a side chain and various aryl derivatives by the microwave irradiation technique.…”