17846-15-0Relevant articles and documents
Synthesis and structure insights of two novel broad-spectrum antibacterial candidates based on (E)-N0-[(Heteroaryl)methylene]adamantane-1carbohydrazides
Al-Mutairi, Aamal A.,Al-Wahaibi, Lamya H.,Alvarez, Natalia,Blacque, Olivier,El-Emam, Ali A.,Veiga, Nicolás
, (2020)
Two new N0-heteroarylidene-1-carbohydrazide derivatives, namely; E-N0-[(pyridine-3yl)methylidene]adamantane-1-carbohydrazide (1) and E-N0-[(5-nitrothiophen-2-yl)methylidene] adamantane-1-carbohydrazide (2), were produced v
In-silico identification of the binding mode of synthesized adamantyl derivatives inside cholinesterase enzymes
Al-Aboudi, Amal,Al-Qawasmeh, Raed A.,Shahwan, Alaa,Mahmood, Uzma,Khalid, Asaad,Ul-Haq, Zaheer
, p. 879 - 886 (2015)
Aim: To investigate the binding mode of synthesized adamantly derivatives inside of cholinesterase enzymes using molecular docking simulations. Methods: A series of hybrid compounds containing adamantane and hydrazide moieties was designed and synthesized
Novel adamantane-pyrazole and hydrazone hybridized: Design, synthesis, cytotoxic evaluation, SAR study and molecular docking simulation as carbonic anhydrase inhibitors
Ammar, Yousry A.,Elhag Ali, Gameel A. M.,Mehany, Ahmed B. M.,Ragab, Ahmed,Wassel, Mohammed M. S.
, (2020)
A series of pyrazole derivatives 4, 5, 6, 12, 13, 14 as well as hydrazone derivatives 7, 10, 11 were synthesized starting from adamantane-1-carbohydrazide as the bioactive core. All newly designed adamantane derivates were established by full characterized using different spectroscopic methods. The novel derivatives were investigated for their antitumor activity against three cell line MCF-7, HepG-2 and A549. They displayed good IC50 values ranged between 1.55 to 42.17 μM in comparison to Doxorubicin (IC50 =3.58–8.19 μM). Surprisingly, adamantine derivatives revealed more sensitivity and selectivity to lung cancer cells (A549) with eight compounds (4, 5, 9a, 9b, 9c, 12, 13a and 14c) having IC50 less than or equal ten micromoles. The most promising three adamantane derivatives 9a, 12 and 13a with IC50 values less than 5 μM were selected to study enzymatic assay for isoenzyme hCAIX and hCAXII. Also, pyrazole core 13a and 12 showed higher KI values than hydrazone derivatives 9a with submicromolar between (0.085–0.527 μM), in comparison to Acetazolamide (0.041–0.068 μM). Compound 13a is the most promising derivatives with anti-proliferative (A549) (IC50=1.55 ± 0.08 μM) which showed CAIX/XII inhibitory activity (KI = 0.085 and 0.14 μM), respectively. Finally, molecular docking simulation was performed to determine the binding modes and possible interaction of the adamantane derivatives within the active site of 3IAI and 1JD0 for CAIX / XII respectively with low binding affinity.
Facile synthesis and antimycobacterial activity of isoniazid, pyrazinamide and ciprofloxacin derivatives
Alsayed, Shahinda S. R.,Lun, Shichun,Payne, Alan,Bishai, William R.,Gunosewoyo, Hendra
, p. 1137 - 1150 (2021/03/18)
Several rationally designed isoniazid (INH), pyrazinamide (PZA) and ciprofloxacin (CPF) derivatives were conveniently synthesized and evaluated in vitro against H37Rv Mycobacterium tuberculosis (M. tb) strain. CPF derivative 16 displayed a modest activity
FLOW CHEMISTRY SYNTHESIS OF ISOCYANATES
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, (2021/06/22)
The disclosure provides, inter alia, safe and environmentally-friendly methods, such as flow chemistry, to synthesize isocyanates, such as methylene diphenyl diisocyanate, toluene diisocyanate, hexamethylene diisocyanate, isophorone diisocyanate, and tetramethylxylene diisocyanate.