Synthesis and biological evaluation of novel N-pyridylpyrazolecarboxamides containing benzothiazole

Biological evaluation of a series of benzothiazole derivatives as mosquitocidal agents

“…Benzothiazole (BT) is a privileged bicyclic ring system present in a wide variety of synthetic and natural products. BT and its derivatives play a distinctive role in medicinal chemistry due to their diverse biological activities such as antiprotozoal, antimicrobial, anticancer, antischizophrenia, antihypertensive, antiinflammatory, and antiviral activities [21][22][23][24][25]. Venugopala et al 2013 [26], also screened benzothiazole analogs for their mosquitocidal and repellent properties against Anopheles arabiensis by mosquito feeding-probing assay, cone bio-assay and standard World Health Organization (WHO) larvicidal assay.…”

Modern Approaches to the Synthesis and Transformations of Practically Valuable Benzothiazole Derivatives

“…They also possess antimicrobial [ 14 , 15 , 16 , 17 , 18 , 19 , 20 ], antioxidant [ 20 ], anti-inflammatory [ 21 , 22 , 23 , 24 ], analgesic [ 24 ], antidepressant [ 25 , 26 ], anticonvulsant [ 27 , 28 , 29 ], anti-diabetic [ 21 , 30 ], antitumor [ 31 , 32 , 33 , 34 , 35 ], antituberculosis [ 14 , 36 ] activity. Their derivatives show also antimalarial [ 37 , 38 ], insecticide [ 39 ] and herbicide effect [ 40 ]. They are also used as key intermediates in fine organic synthesis and the resins’ components [ 41 ].…”

“…Many researchers were engaged in the search for new families of biologically active 2,5(6)-substituted 2-aminobenzothiazoles. The starting 2-unsubstituted 2-aminobenzothiazoles were obtained from the easily available anilines, potassium thiocyanate and bromine, then acylated by chloroacetyl chloride and introduced in the reactions with various N -heterocycles [ 7 , 14 , 17 , 20 , 25 , 26 , 27 , 28 , 29 , 31 , 36 , 38 , 39 ]. Thus, a large benzothiazole-piperazine series of compounds 16a – v was synthesized in three steps ( Scheme 15 ) [ 25 , 26 ].…”

“…antimicrobial [ 18 , 19 , 66 , 67 , 68 , 69 ], anti-inflammatory and antioxidant [ 69 , 70 , 71 ], antitumor [ 72 , 73 , 74 ]. Agrochemicals with 2-mercaptobenzothiazole moiety in the molecule are used as fungicides of a wide spectrum [ 75 , 76 , 77 ], herbicides [ 78 ], insecticides [ 39 , 78 , 79 ]. In industry, they are used as metal corrosion inhibitors in different media [ 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 ], additives to lubricants [ 89 , 90 ], sorbents of trace amounts of metals, including noble metals [ 91 , 92 , 93 ] and rubber vulcanization accelerators [ 94 , 95 , 96 ].…”

Synthesis of biologically active derivatives of 2-aminobenzothiazole

“…1 Molecules with a benzothiazole moiety have a pronounced spectrum of biological activity, exhibiting, along with antiviral, 2 – 5 also antimicrobial, 6 – 10 anti-inflammatory, 10 – 15 antidiabetic, 14 analgesic, 12 , 13 antioxidant, 6 , 14 , 15 antidepressant, 16 anticonvulsant, 17 , 18 antianginal, 19 antitumor, 20 , 21 immunomodulatory effects. BTA derivatives also have anthelmintic, 6 , 7 antimalarial, 23 fungicidal, 6 , 24 insecticidal, 24 , 25 and herbicidal 26 effects.…”