Synthesis and biological property of some novel 1,3,4-oxadiazoles☆

Novel synthetic organic compounds inspired from antifeedant marine alkaloids as potent bacterial biofilm inhibitors

“…These compounds, consisting of N-methyl-4,5-dibromopyrrole motif integrated with 1,3,4-oxadiazole were chosen for the current study based on their resemblance to known marine antibiofilm agents, QS inhibitors as well as reported antibiotics (Figs. 1 and 2) [13][14][15][16][17]. Based on the potent activity of synthesized adducts towards bacterial biofilm formation, a structure-activity analysis was developed, that can direct future studies involved in the search of novel compounds for biofilm control.…”

Microwave‐assisted synthesis of triazole derivatives conjugated with piperidine as new anti‐enzymatic agents

“…Triazoles and their derived compounds have promising activities in the field of agriculture, medicine, biology, nano‐chemistry, and material science . Triazole‐based compounds have the ability to act as active antiviral, antifungal, antibacterial, anti‐inflammatory, anticonvulsant, and anticancer agents . It is evident from literature review that the triazole‐based derivatives are biologically active compounds and frequently synthesized by using conventional technique.…”

Synthesis and docking studies of N‐(5‐(alkylthio)‐1,3,4‐oxadiazol‐2‐yl)methyl)benzamide analogues as potential alkaline phosphatase inhibitors

“…It is a membrane bound glycosylated enzyme, a potent inhibitor of calcification, and its role is to hydrolyze inorganic pyrophosphate therefore this enzyme is essential for the skeletal mineralization (Desai, Bhatt, Somani, & Trivedi, 2013;Lanier et al, 2010;Miao, Bai, Panda, Karaplis, Goltzman, & McKee, 2004;Millán, 2006b). These inhibitors of the reported drug are poorly selective, and the reported IC 50 value is above 5 μM for all three ALPs, and their inhibition is of rare uncompetitive type (Chang et al, 2011). 1,3,4-Oxadiazoles have great significance in the heterocyclic compounds, and their derivatives show a wide range of biological activities such as painkillers, act as anti-hyperlipidemic agents, produce or develop ulceration, anti-tubercular (Jha et al, 2010), antiviral (Llinas-Brunet et al, 2004;Wei et al, 2013), hypoglycemic, antimicrobial (Xu et al, 2012), antineoplastic, fungicidal, anticancer, inhibition of tyrosinase cathepsin K (Munawar et al, 2015), analgesic, antimicrobial, anticancer (El-Din, El-Gamal, Abdel-Maksoud, Yoo, & Oh, 2015, antioxidant activities (Ma et al, 2013), anti-inflammatory (Ramaprasad, Kalluraya, Kumar, & Hunnur, 2010;Şahin, Palaska, Ekizo glu, & Özalp, 2002), hypnotic, genotoxic, serve as muscle anti-epileptic and anti-seizure, inhibitor of oxidative degradation of lipid (Zawawi et al, 2015), and vasodilator. If IAP gets elevated then it causes problems such as obesity caused by inappropriate deposition of fats within the cell (Buchet, Millán, & Magne, 2013), neurological disorders (Fonta, Barone, Martinez, & Négyessy, 2015;Pan et al, 2017;Sebastian-Serrano et al, 2015), chronic kidney disease (Debray et al, 2013), breast cancer, prostate cancer (Lin, Huang, Zeng, & Wu, 2019;Miao et al, 2004;Ooi, Shiraki, Morishita, & Nobori, 2007), congestion or obstruction of the biliary tract, also damage kidney, and liver.…”