62984-48-9Relevant academic research and scientific papers
(Hetero-)(arylidene)arylhydrazides as Multitarget-Directed Monoamine Oxidase Inhibitors
Palakkathondi, Ashique,Oh, Jong Min,Dev, Sanal,Rangarajan,Kaipakasseri, Swafvan,Kavully, Fathima Sahla,Gambacorta, Nicola,Nicolotti, Orazio,Kim, Hoon,Mathew, Bijo
, p. 592 - 599 (2020)
Fourteen (hetero-)(arylidene)arylhydrazide derivatives (ABH1-ABH14) were synthesized, and their inhibitory activities against monoamine oxidases (MAOs) and acetylcholinesterase (AChE) were evaluated. Compound ABH5 most potently inhibited MAO-B with an IC5
Synthesis of some 2,3-dihydro-1,3,4-oxadiazoles and 4,5-dihydro-1,2,4-triazoles as anticancer agents
Abdullah, Jalal H.,Yahya, Tawfeek A.
, p. 92 - 99 (2020/09/02)
Objective: The main objective of this work was to synthesize and evaluate the novel 2,3-dihydro-1,3,4-oxadiazole and 4,5-dihydro-1,2,4-triazole derivatives for cytotoxic activities. Methods: The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were synthesized by cyclization of N'-(substituted-benzylidene) isonicotinohydrazide 3a-e in refluxing acetic anhydride. The 2,3-dihydro-1,3,4-oxadiazole derivatives 4a-h were converted into the corresponding 4,5-dihydro-1,2,4-triazoles 5a-h using ammonia. All the synthesized compounds were identified, depending on the physical and spectral data. Title compounds were assessed for their cytotoxic activity against human cancer cell line (MCF-7) by using Sulforhodamine B (SRB) colorimetric assay. Results: All the synthesized compounds showed characteristic peaks in FTIR, 1HNMR and Mass spectral analysis. The results of the in vitro cytotoxic activity revealed that the compound 4c exhibited equipotent cytotoxic activity with an IC50 value of 8.04 μM when compared with that of standard drug doxorubicin (IC50= 8.02 μM). The reminder compounds have shown good to moderate cytotoxic activities when compared with that of a reference standard. Conclusion: We synthesized a series of title compounds in quantitative yields. Most derivatives showed moderate to good cytotoxic activity.
New isoniazid derivatives with improved pharmaco-toxicological profile: Obtaining, characterization and biological evaluation
Dragostin, Ionut,Dragostin, Oana M.,Samal, Sangram Keshari,Dash, Saumya,Tatia, Rodica,Dragan, Maria,Confederat, Lumini?a,Ghiciuc, Cristina M.,Diculencu, Daniela,Lupu?oru, C?t?lina E.,Zamfir, Carmen L.
, (2019/07/02)
Tuberculostatic drugs are the most common drug groups with global hepatotoxicity. Awareness of potentially severe hepatotoxic reactions is vital, as hepatic impairment can be a devastating and often fatal condition. The treatment problems that may arise, within this class of medicines, are mainly of two types: adverse reactions (collateral, toxic or hypersensitive reactions) and the initial or acquired resistance of Mycobacterium tuberculosis to one or more antituberculosis drugs. Prevention of adverse reactions, increase treatment adherence and success rates, providing better control of tuberculosis (TB). In this regard, obtaining new drugs with low toxicity and high tuberculostatic potential is essential. Thus, in this work, we have designed or synthesized new derivatives of isoniazid (INH), such as new Isonicotinoylhydrazone (INH-a, INH-b and INH-c). These derivatives demonstrated good biocompatibility, antimicrobial property similar to that of parent isoniazid and last but not least, a significantly improved Pharmacotoxicological profile compared to that of isoniazid.
Spectroscopic, molecular docking and structural activity studies of (E)-N′-(substituted benzylidene/methylene) isonicotinohydrazide derivatives for DNA binding and their biological screening
Arshad, Nasima,Perveen, Fouzia,Saeed, Aamer,Channar, Pervaiz Ali,Farooqi, Shahid Iqbal,Larik, Fayaz Ali,Ismail, Hammad,Mirza, Bushra
, p. 371 - 380 (2017/03/27)
Acid catalyzed condensation of isoniazid with a number of suitably substituted aromatic and heterocyclic aldehydes was carried out in dry ethanol to afford the title (E)-N′-(substituted benzylidene/methylene) isonicotinohydrazides (SF 1 – SF 4) in good yi
Isonicotinohydrazones as inhibitors of alkaline phosphatase and ecto-5′-nucleotidase
Channar, Pervaiz Ali,Shah, Syed Jawad Ali,Hassan, Sidra,Nisa, Zaib un,Lecka, Joanna,Sévigny, Jean,Bajorath, Jürgen,Saeed, Aamer,Iqbal, Jamshed
, p. 365 - 370 (2017/04/03)
A series of isonicotinohydrazide derivatives was synthesized and tested against recombinant human and rat ecto-5′-nucleotidases (h-e5′NT and r-e5′NT) and alkaline phosphatase isozymes including both bovine tissue-non-specific alkaline phosphatase (b-TNAP)
Synthesis and testing of 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4- oxadiazole derivatives for antifungal activity against selected Candida species
De Oliveira, Cledualdo S.,Lira, Bruno F.,Barbosa-Filho, Jose? M.,Lorenzo, Jorge G. F.,De Menezes, Camilla P.,Dos Santos, Jessyca M. C. G.,De Lima, Edeltrudes O.,De Athayde-Filho, Petro?nio F.
, p. 115 - 120 (2013/04/24)
A series of 21 1,3,4-oxadiazoline derivatives was synthesized by cyclization of N-acylhydrazones with acetic anhydride and evaluated for their in vitro antifungal activity against six Candida strains: Candida albicans (ATCC 90028 and LM V-42), C. krusei (ATCC 6258 and LM 12 C) and C. tropicalis (ATCC 13803 and LM 14). The Candida strains were found to be sensitive to some of the compounds, which inhibited the growth by 50-90percent, with minimum inhibitory concentration (MIC) in the range of 64-512 μg mL-1. The compounds' structures were fully confirmed and characterized by Fourier transform infrared spectroscopy (FTIR), 1H and 13C nuclear magnetic resonance (NMR) and mass spectrometry (MS).
Synthesis, characterization and pharmacological evaluation of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives as potent anticonvulsant agents
Malhotra, Manav,Monga, Vikramdeep,Sharma, Sagun,Jain, Jainendra,Samad, Abdul,Stables, James,Deep, Aakash
, p. 2145 - 2152 (2012/11/07)
A series of (E)-N′-(substituted-benzylidene)isonicotinohydrazide derivatives were synthesized by coupling it with different substituted aldehydes, acetophenone, and benzophenones in presence of absolute ethanol along with catalytic amount of glacial aceti
Preparation and antitubercular activities in vitro and in vivo of novel Schiff bases of isoniazid
Hearn, Michael J.,Cynamon, Michael H.,Chen, Michaeline F.,Coppins, Rebecca,Davis, Jessica,Joo-On Kang, Helen,Noble, Abigail,Tu-Sekine, Becky,Terrot, Marianne S.,Trombino, Daniella,Thai, Minh,Webster, Eleanor R.,Wilson, Rebecca
experimental part, p. 4169 - 4178 (2009/12/04)
Structural modification of the frontline antitubercular isonicotinic acid hydrazide (INH) provides lipophilic adaptations (3-46) of the drug in which the hydrazine moiety of the parent compound has been chemically blocked from the deactivating process of N2-acetylation by N-arylaminoacetyl transferases. As a class, these compounds show high levels of activity against Mycobacterium tuberculosis in vitro and in tuberculosis-infected macrophages. They provide strong protection in tuberculosis-infected mice and have low toxicity. With some representatives of this class achieving early peak plasma concentrations approximately three orders of magnitude above minimum inhibitory concentration, they may serve as tools for improving our understanding of INH-based treatment modalities, particularly for those patients chronically underdosed in conventional INH therapy.
Synthesis and anti-mycobacterial activity of (E)-N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives
Lourenco, Maria Cristina da Silva,Ferreira, Marcelle de Lima,de Souza, Marcus Vinicius Nora,Peralta, Monica Amado,Vasconcelos, Thatyana Rocha Alves,Henriques, Maria das Gracas M.O.
, p. 1344 - 1347 (2008/09/21)
A series of 22 (E)-N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using Alamar Blue susceptibility test and
