Ozkan, Synthesis and biological evaluation of new N-(2-hydroxy-4(or5)-nitro/aminophenyl) benzamides and phenylacetamides as antimicrobial agents, Bioorgan.
Summary: A series of novel benzamide derivatives according to fluopicolide were designed and synthesized following the rule of combination carboxylic acid amides and amines derivatives together.
Keywords: Design, Synthesis, Fluopicolide, Benzamide derivatives, Antifungal activity.
As the reason of fungicide resistance , in order to discover new fungicides which possess high efficacy, low toxicity and safety to non-target organisms, a series of heterocyclic/homocyclic benzamide derivatives based on fluopicolide have been designed according to the rule of connecting bioactive substructures together (Fig.
bifunctional molecule was found to be active for class I deacetylases (HDAC3) and class II deacetylases (HDAC6) and was potent in nM concentration in breast cancer models.
Several HDAC inhibitors are in clinical trial, namely, hydroxamic acid derivatives, benzamide derivatives, cyclic peptides, and short-chain fatty acids .
The chemotype A is N(2-aminophenyl)-benzamide [20-31] and chemotype B is N-hydroxy benzamide derivatives (see supplementary Figure 1 in the Supplementary Material available online at http://dx.doi.org/10.1155/2014/812148) [32-34].
The binding mode of the compound shown in Figure 4(g) shows Hypo1 of HBA mapped nitrogen of thiazole forms hydrogen bonding with Arg39, HBD mapped on oxygen of N-hydroxy has hydrogen bond interaction with His183, benzamide of nitrogen has interaction with His146, and nitrogen of formamide has interaction with Asp181.
When o-ethoxycarbonylamino benzamide
and its 4-methyl derivatives are heated over their melting points, then they lose water and form 1,2,3,4-tetrahydro-2,4-dioxoquinazoline (see Scheme 16).
Chatterjee previously reported that PARP activation contributes in part to postreperfusion renal dysfunction and damage to renal tissue with previous ischemia, based on the following experimental evidence: (1) an increased immunohistochemical expression of PARP after renal IR, (2) a significant improvement in renal alterations (reduced urea and creatinine levels and increased glomerular filtrate) with the use of benzamide
analogs, selective PARP inhibitors, (3) the lack of effect on IR-induced renal dysfunction of aminobenzoic and nicotinic acids, which do not inhibit PARP , and (4) protection by PARP inhibitors of primary cultures of rat proximal kidney tubules against lesion and oxidative stress-mediated cell death .
4a-4d and 4a'-4d' were obtained in excellent yields after filtration or solvent extraction.
Sapienza et al., "Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides
," Bioorganic and Medicinal Chemistry Letters, vol.