81975-20-4Relevant academic research and scientific papers
Exploration of diphenylalkyloxadiazoles as novel cardiac myosin activator
Manickam, Manoj,Boggu, Pulla Reddy,Pillaiyar, Thanigaimalai,Sharma, Niti,Jalani, Hitesh B.,Venkateswararao, Eeda,Jung, Sang-Hun
supporting information, p. 2369 - 2374 (2018/06/25)
To explore novel cardiac myosin activator, a series of diphenylalkyl substituted 1,3,4-oxadiazoles and 1,2,4-oxadiazoles have been prepared and tested for cardiac myosin ATPase activation in vitro. In all cases, three carbon spacer between the oxadiazole core and one of the phenyl ring was considered crucial. In case of 1,3,4-oxadiazole, zero to two carbon spacer between oxadiazole core and other phenyl ring are favorable. Phenyl ring can be replaced by cyclohexyl moiety. In case of 1,2,4-oxadiazole, zero or one carbon spacer between the oxadiazole and other phenyl ring are favorable. Introduction of hydrogen bonding donor (NH) group at the 2nd position of the 1,3,4-oxadiazole enhances the activity. Substitutions on either of the phenyl rings or change of phenyl ring to other heterocycle are not tolerated for both the oxadiazoles. The prepared oxadiazoles showed selective activation for cardiac muscle over smooth and skeleton muscles.
Synthesis of novel 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds and their evaluation for tuberculostatic activity
Gobis, Katarzyna,Foks, Henryk,Bojanowski, Krzysztof,Augustynowicz-Kope?, Ewa,Napiórkowska, Agnieszka
experimental part, p. 137 - 144 (2012/03/08)
A series of novel 3-cyclohexylpropanoic acid derivatives and 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds (1-8) have been synthesized and evaluated for tuberculostatic activity. Compounds 1a, 1c, 1e and 1f bearing benzimidazole or benzimidazole-like systems showed the most potent tuberculostatic activity against Mycobacterium tuberculosis strains with MIC values ranging from 1.5 to 12.5 μg/mL. More importantly 1a (6-chloro-2-(2-cyclohexylethyl)-4-nitro-1H-benzo[d]imidazole) and 1f (2-(2-cyclohexylethyl)-1H-imidazo[4,5-b]phenazine) appeared selective for M. tuberculosis as compared with eukaryotic cells (human fibroblasts), and other antimicrobial strains. These compounds may thus represent a novel, selective class of antitubercular agents. Additionally compound 1a stimulated type I collagen output by fibroblasts, in vitro.
Synthesis, antimicrobial activity and cytotoxicity of novel oxadiazole derivatives
Kaplancikli, Zafer Asim,Altintop, Mehlika Dilek,Turan-Zitouni, Gulhan,Ozdemir, Ahmet,Ozic, Rasime,Akaliin, Guelsen
scheme or table, p. 51 - 57 (2012/04/05)
In the present study, 5-substituted-1,3,4-oxadiazolin-2-thiones (1ab) were synthesized via the ring closure reactions of appropriate acid hydrazides with carbon disulphide. N-(Benzothiazol-2-yl)-2-[[5-substituted-1,3,4-oxadiazol-2-yl] sulfanyl]acetamide d
Synthesis and biological evaluation of some hydrazone derivatives as anti-inflammatory agents
Kaplancikli, Zafer Asim,Altintop, Mehlika Dilek,Oezdemir, Ahmet,Turan-Zitouni, Guelhan,Khan, Shabana I.,Tabanca, Nurhayat
experimental part, p. 310 - 315 (2012/06/04)
In the present study, some hydrazone derivatives were synthesized via the reaction of 3-cyclohexylpropionic acid hydrazide with various benzaldehydes. The chemical structures of the compounds were elucidated by spectroscopic techniques such as IR, 1H-NMR and FAB-MS and elemental analyses. The compounds were evaluated for their antiinflammatory and cytotoxic activities. Anti-inflammatory activity was determined in terms of inhibition of NF-κB, ROS generation and iNOS activity. Several derivatives inhibited NF-κB and iNOS, but no effect was observed on intracellular ROS generation. Furthermore no cytoxicity was observed. Biological activity compared with the chemical structural information suggests that different functional groups on the phenyl ring influence the physicochemical properties and thus modulate biological activity.
