Abstract In pursuit of potential agents to treat Chagas disease and leishmaniasis, we report the design, synthesis, and identification novel naphthoquinone hydrazide-based molecular hybrids. The compounds were subjected to in vitro trypanocide and leishmanicidal activities. N’-(1,4-Dioxo-1,4-dihydronaphthalen-2-yl)-3,5-dimethoxybenzohydrazide (13) showed the best performance against Trypanosoma cruzi (IC50 1.83 µM) and Leishmania amazonensis (IC50 9.65 µM). 4-Bromo-N’-(1,4-dioxo-1,4-dihydronaphthalen-2-yl)benzohydrazide (16) exhibited leishmanicidal activity (IC50 12.16 µM). Regarding trypanocide activity, compound 13 was low cytotoxic to LLC-MK2 cells (SI = 95.28). Furthermore, through molecular modeling studies, the cysteine proteases cruzain, rhodesain and CPB2.8 were identified as the potential biological targets. leishmaniasis design synthesis hydrazidebased hydrazide based hybrids activities N1,4Dioxo1,4dihydronaphthalen2yl3,5dimethoxybenzohydrazide N14Dioxo14dihydronaphthalen2yl35dimethoxybenzohydrazide NDioxodihydronaphthalenyldimethoxybenzohydrazide N 1,4 Dioxo dihydronaphthalen 2 yl 3,5 dimethoxybenzohydrazide 1 4 3 5 (13 IC50 IC (IC5 183 83 1.8 µM 965 9 65 9.6 µM. . 4BromoN1,4dioxo1,4dihydronaphthalen2ylbenzohydrazide 4BromoN14dioxo14dihydronaphthalen2ylbenzohydrazide BromoNdioxodihydronaphthalenylbenzohydrazide Bromo dioxo benzohydrazide 16 (16 1216 12 12.1 LLCMK2 LLCMK LLC MK2 MK LLC-MK SI 95.28. 9528 95.28 95 28 95.28) Furthermore studies cruzain CPB28 CPB CPB2 8 CPB2. targets N1 4Dioxo1 4dihydronaphthalen2yl3 5dimethoxybenzohydrazide 14 1, 35 3, (1 IC5 (IC 18 1. 96 6 9. 4BromoN1 4dioxo1 4dihydronaphthalen2ylbenzohydrazide BromoN ylbenzohydrazide 121 12. 952 95.2 4Dioxo dihydronaphthalenyl 4dihydronaphthalen2yl ( 4BromoN 4dioxo dihydronaphthalenylbenzohydrazide 95.

Octocrylene (2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate) is present in several sunscreens and is known to work synergistically with UV filters. We prepared eight octocrylene-related compounds to test their photoprotective activities by measuring diffuse transmittance. The compounds had varied photoprotection profiles, with Sun Protection Factors (SPF) ranging from 1 to 5 and UVA Protection Factors (UVAPF) ranging from 1 to 8. Compounds 4, 5, and 7 showed the best protection against UVB sunrays, while compounds 5, 6, and 7 presented the best results for protection from UVA, so compound 7 had the most balanced protection overall. Results for compounds 4, 8, and 9 are reported for the first time in the literature.

alpha-Bromoacetophenones are important in organic synthesis. They have been widely used as precursors of several natural products. Several methods of bromination aiming at their synthesis have been described, however they furnish a mixture of starting material 10, mono 8 and dibromide 11 products. We developed a novel, simple and efficient synthesis of these compounds with applications in the synthesis of benzoylbenzofurans 9, compounds with important pharmacological properties, such as the ability of dilating the coronary artery and analgesic action. Such compounds have also been used as key intermediates to obtain quinone systems.