5325-89-3Relevant articles and documents
Design, synthesis, docking and biological evaluation of chalcones as promising antidiabetic agents
Bhaskar, Baki Vijaya,Gu, Wei,Rammohan, Aluru,Venkateswarlu, Nagam,Zyryanov, Grigory V.
, (2020/01/08)
Diabetes mellitus (DM) is a serious chronic metabolic disorder which occurs due to dysfunction of insulin and therapeutic approaches are poor. It is an under estimation that 387 million people currently suffering globally with diabetic and more than 592 m
Design, synthesis, molecular modeling, and ADMET studies of some pyrazoline derivatives as shikimate kinase inhibitors
James, Jainey P.,Ishwar Bhat,More, Uttam A.,Joshi, Shrinivas D.
, p. 546 - 559 (2017/11/16)
A series of pyrazoline derivatives were synthesized and their structures have been characterized by IR, 1H NMR, 13C NMR, mass spectral and elemental analysis. The novel compounds were designed as Mycobacterium tuberculosis shikimate
Synthesis and antibacterial evaluation of novel cationic chalcone derivatives possessing broad spectrum antibacterial activity
Chu, Wen-Chao,Bai, Peng-Yan,Yang, Zhao-Qing,Cui, De-Yun,Hua, Yong-Gang,Yang, Yi,Yang, Qian-Qian,Zhang, En,Qin, Shangshang
supporting information, p. 905 - 921 (2017/12/26)
There is an urgent need to identify new antibiotics with novel mechanisms that combat antibiotic resistant bacteria. Herein, a series of chalcone derivatives that mimic the essential properties of cationic antimicrobial peptides were designed and synthesized. Antibacterial activities against drug-sensitive bacteria, including Staphylococcus aureus, Enterococcus faecalis, Escherichia coli and Salmonella enterica, as well as clinical multiple drug resistant isolates of methicillin-resistant S. aureus (MRSA), KPC-2-producing and NDM-1-producing Carbapenem-resistant Enterobacteriaceae were evaluated. Representative compounds 5a (MIC: 1 μg/mL against S. aureus, 0.5 μg/mL against MRSA) and 5g (MIC: 0.5 μg/mL against S. aureus, 0.25 μg/mL against MRSA) showed good bactericidal activity against both Gram-positive and Gram-negative bacteria, including the drug-resistant species MRSA, KPC and NDM. These membrane-active antibacterial compounds were demonstrated to reduce the viable cell counts in bacterial biofilms effectively and do not induce the development of resistance in bacteria. Additionally, these representative molecules exhibited negligible toxicity toward mammalian cells at a suitable concentration. The combined results indicate that this series of cationic chalcone derivatives have potential therapeutic effects against bacterial infections.
Chalcone derivatives with drug-resistant bacteria resistance activity
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Paragraph 0035; 0036, (2016/10/27)
The invention belongs to the field of pharmaceutical chemistry, and discloses novel chalcone derivatives with drug-resistant bacteria resistance activity and a synthesis method thereof. The two reaction steps are performed to simply and quickly obtain the
In vitro antioxidant activity and scavenging effects of some synthesized 4-Aminochalcones
Prasad, Y.Rajendra,Rani, V. Jhansi,Rao, A. Srinivasa
, p. 52 - 58 (2013/02/22)
A new series of substituted 4'-aminochalcones were synthesized by Claisen-Schmidt condensation of 4-aminoacetophenone with various substituted aromatic/heteroaromatic aldehydes. The antioxidant activity for all these compounds were studied on various reac
A study of anti-inflammatory and analgesic activity of new 2,4,6-trisubstituted pyrimidines
Yejella, Rajendra Prasad,Atla, Srinivasa Rao
scheme or table, p. 1079 - 1082 (2011/10/05)
Chalcone derivatives (3a - m) were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes according to Claisen-Schmidt condensation. These chalcones, on reaction with guanidine hydrochloride under basic alcoholic conditions gave 2,4,6-trisubstituted pyrimidines (5a - m) in quantitative yields. All the newly synthesized pyrimidines were characterized by means of IR, 1H- and 13CNMR, Electron Ionization (EI)-mass and elemental analyses and screened for anti-inflammatory and analgesic activities by in vivo. 2-Amino-4-(4-aminophenyl)-6-(2,4-dichlorophenyl)pyrimidine (5b) and 2-amino-4-(4-aminophenyl)- 6-(3-bromophenyl) pyrimidine (5d) were found to be the most potent anti-inflammatory and analgesic activity compared with ibuprofen, reference standard. And also it was found that compound 5b identified as lead structure among all in both the activities. Pyrimidines which showed good anti-inflammatory activity also displayed better analgesic activity.
Synthesis and antimicrobial activity of some new 2,4,6-trisubstituted pyrimidines
Prasad, Y. Rajendra,Rao, B. Bhaskar,Agarwal,Rao, A. Srinivasa
scheme or table, p. 641 - 644 (2011/12/15)
Chalcone derivatives [3(a-m)] were prepared by condensing 4-aminoacetophenone with various substituted aromatic and hetero aromatic aldehydes in dilute ethanolic potassium hydroxide solution at room temperature according to Claisen-Schmidt condensation. These chalcones react with guanidine hydrochloride in a basic alcoholic media to give 2,4,6-trisubstituted pyrimidines [5(a-m)]. All these pyrimidines were characterized by means of their IR, 1H NMR and elemental analyses and screened for their antimicrobial activity. Some of these compounds showed significant antimicrobial activity.
Synthesis and analgesic activity of some chalcones
Srinivasa Rao
experimental part, p. 4373 - 4376 (2012/02/14)
A series of novel 1-(4′-aminophenyl)-3-(substituted aryl/heteroaryl)-2-propen-1-ones (1-16) have been synthesized by treating 4-amino acetophenone with various substituted aromatic and unsubstituted heterocyclic aldehydes in presence of methanol and aqueous alkaline solution at room temperature. Their structures were confirmed by IR, 1H NMR, 13C NMR, EI-MS spectra and elemental analyses data. The synthesized compounds were investigated for their analgesic activity. Compounds 6 and 15 exhibited maximum analgesic activity. Chalcones with electron releasing substituent like amino, hydroxyl, methyl, halogens etc exhibited good analgesic activity.
Benzamide compounds as apo b secretion inhibitors
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, (2008/06/13)
The present invention relates to compounds of the formula (I) wherein R1 and R2 are each independently lower alkyl lower alkenyl, acyl, amino, lower alkoxy, lower cycloalkyloxy, aryl, aryloxy, sulfooxy, mercapto, sulfo, hydrogen, halogen, nitro, cyano or hydroxy, or may form a ring structure; Q1 is N or CH; L is optionally substituted unsaturated 3 to 10-membered heterocyclic group; X is optionally substituted monocyclic arylene or monocyclic heteroarylene; Y is -(A1)m-(A2)n-(A4)k-; Z is directbond, —CH2-, —NH— or —O—; and R is hydrogen or lower alkyl, or a salt thereof The compounds of the present invention inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.