Synthesis and Smo Activity of Some Novel Benzamide Derivatives

Ding, Huaiwei; Chen, Kai; Song, Bingke; Deng, Chenglong; Li, Wei; Niu, Li Ying; Bai, Ming; Song, Haiyan; Zhang, Lijuan

doi:10.3390/molecules23010085

Cited by 2 publications

(1 citation statement)

References 17 publications

(18 reference statements)

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“…For example proteins play an essential role in all biological process such as immune protection, enzyme catalysis, transport or storage (hemoglobin's) and mechanical support (collagen). In amides, all the three atoms O=C=N chain are reactive which make useful moiety in synthesis of organic compounds 5,6,7 . They have a wide range of biological activities like Antimicrobial, Anti-HIV, Anti-psychotic action (especially block D2 receptors), Anti-diabetic (especially treatment of type-2 diabetes), Anti-Alzheimer's, Anti-Depressants, Anti-Oxidant properties.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Insilico Toxicity Prediction, Anti-Microbial Study of Ortho-Amino Substituted Benzamide Derivatives

Ammaji¹,

Pavan

Likhith

et al. 2019

Int J Life Sci Pharm Res

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Benzamides are most widely used in medicinal chemistry and play a key role in biological action for treatment of various disorders such as anti-microbial, anti-malarial, anti-cancer, anti HIV, anti-viral, anti ameobic, anti-psychotic. The benzamide was used as an intermediate for synthesis of various medicinal compounds, in the present work; synthesization was carried out by using isatoic anhydride treated with various substituted anilines under acidic condition to form different substituted ortho-amino benzamide derivatives. Evaluation of the synthesized compounds were done by using the Insilico toxicity prediction methods with the aid of online software's like OSIRIS, OCHEM, Molinspiration. These three softwares gave the drug score value of 3a, 3c, 3f, 3d and they are nearer to standard drug score value of 0.8. Toxicity prediction inferred that except 3e, other derivatives were safe to inhibit enzyme cytochrome P450 a subunit of CYP 1A2. The enzyme located in endoplasmic reticulum metabolizes the polyunsaturated fatty acids, steroidal hormones, vitamins, and also catalyzes hydroxylation reaction like hydroxyl estrogen from estrogen, 17-beta estradiols and has a major role in synthesis of all Trans retinol biosynthesis in liver. Invitro evaluation of Anti-microbial activity done by disc diffusion method, confirmed the compounds3eand3f had significant activity against Pseudomonas aeruginosa and the compounds3aand3dshowed significant activity against Bacillus subtilis, whereas the compounds 3c showed good activity against the organism Bacillus pumilus. Compound 3a showed moderate antifungal activity against Candida albicans. Thus in future benzamides can be considered as an effective intermediate for synthesis of different substituted quinoxaline derivatives.

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Section: Introductionmentioning

confidence: 99%

Synthesis, Characterization and Insilico Toxicity Prediction, Anti-Microbial Study of Ortho-Amino Substituted Benzamide Derivatives

Ammaji¹,

Pavan

Likhith

et al. 2019

Int J Life Sci Pharm Res

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Targeting the Oncoprotein Smoothened by Small Molecules: Focus on Novel Acylguanidine Derivatives as Potent Smoothened Inhibitors

Pietrobono¹,

Stecca²

2018

Cells

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Hedgehog-GLI (HH) signaling was originally identified as a critical morphogenetic pathway in embryonic development. Since its discovery, a multitude of studies have reported that HH signaling also plays key roles in a variety of cancer types and in maintaining tumor-initiating cells. Smoothened (SMO) is the main transducer of HH signaling, and in the last few years, it has emerged as a promising therapeutic target for anticancer therapy. Although vismodegib and sonidegib have demonstrated effectiveness for the treatment of basal cell carcinoma (BCC), their clinical use has been hampered by severe side effects, low selectivity against cancer stem cells, and the onset of mutation-driven drug resistance. Moreover, SMO antagonists are not effective in cancers where HH activation is due to mutations of pathway components downstream of SMO, or in the case of noncanonical, SMO-independent activation of the GLI transcription factors, the final mediators of HH signaling. Here, we review the current and rapidly expanding field of SMO small-molecule inhibitors in experimental and clinical settings, focusing on a class of acylguanidine derivatives. We also discuss various aspects of SMO, including mechanisms of resistance to SMO antagonists.

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Synthesis and Smo Activity of Some Novel Benzamide Derivatives

Cited by 2 publications

References 17 publications

Synthesis, Characterization and Insilico Toxicity Prediction, Anti-Microbial Study of Ortho-Amino Substituted Benzamide Derivatives

Synthesis, Characterization and Insilico Toxicity Prediction, Anti-Microbial Study of Ortho-Amino Substituted Benzamide Derivatives

Targeting the Oncoprotein Smoothened by Small Molecules: Focus on Novel Acylguanidine Derivatives as Potent Smoothened Inhibitors

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