626-48-2Relevant articles and documents
SYNTHESIS AND STUDY OF THE RADIOPROTECTIVE PROPERTIES OF THE PYRIMIDINE ANALOGS OF ISOTHIOURONIUM
Golomolzin, B. V.,Tarakhtii, E. A.,Tregubenko, I. P.,Perova, N. M.
, p. 621 - 623 (1984)
-
Novel triazole-sulfonamide bearing pyrimidine moieties with carbonic anhydrase inhibitory action: Design, synthesis, computational and enzyme inhibition studies
Hoda, Nasimul,Manzoor, Shoaib,Petreni, Andrea,Raza, Md Kausar,Supuran, Claudiu T.
supporting information, (2021/07/16)
A series of new triazole-sulfonamide bearing pyrimidine derivatives were designed and synthesized via click chemistry. All new compounds (SH-1 to SH-28) were validated by 1HNMR, 13CNMR, HRMS, and SH-3 was further structurally validated by X-Ray single diffraction study. These compounds (SH-1 to SH-28) were tested as inhibitors of human carbonic anhydrase (hCA) isoforms, such as hCA I, II, IX and XII, using a stopped flow CO2 hydrase assay. Most of the compounds exhibited significant inhibitory activity against hCA II and weak inhibitory activity against hCA I. The target compounds also displayed moderate to excellent inhibitory activity against tumor-related hCAs IX and XII. Some compounds, e.g., SH-20 (Ki = 9.4 nM), SH-26 (Ki = 1.8 nM) and SH-28 (Ki = 0.82 nM) exhibited excellent inhibitory activity and selectivity profile against hCAs XII over IX. SH-23 displayed promising inhibitory activity and selectivity profile against both tumor-related hCAs IX (Ki = 2.9 nM) as well as XII (Ki = 0.82 nM) over hCA I and II. To understand the molecular interactions, molecular docking study of compounds SH-20, SH-23, SH-26 and SH-28 with hCA XII and SH-23 also with hCA IX were performed. The computational study evidenced favorable interaction between the inhibitors and active residues of both proteins. Some of these derivatives are promising leads for the development of selective, anticancer agents based on CA inhibitors.
Production method of dipyridamole bulk drug
-
Paragraph 0005; 0017, (2018/06/04)
The invention provides a production method of a bulk drug of dipyridamole, which relates to the field of the synthesis of chemical bulk drugs. The production method comprises the following steps: protecting carbonyl of urea, performing condensation reaction with 2,3-diaminosuccinic acid, performing chlorination for hydroxyl of a condensation reactant, replacing chlorine with piperidine, hydrolyzing an obtained product, obtaining a compound containing two carbonyls, separating the product, enabling the separated product to have condensation reaction with diethanol amine, obtaining dipyridamole,and refining to obtain a finished product. By adopting the production method, the synthetic procedure of the dipyridamole is simplified, the conversion rate of raw materials can be greatly increased,and the production cost is decreased.
Synthesis of new 2,4-diaryl-6-methyl-5-nitropyrimidines as antibacterial and antioxidant agents
Sura, Mallikarjun Reddy,Peddiahgari, Vasu Govardhana Reddy,Bhoomireddy, Rajendra Prasad Reddy,Vadde, Rama Krishna
, p. 1395 - 1399 (2014/01/06)
A new series of 2,4-diaryl-6-methyl-5-nitropyrimidines (5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i) were synthesized in good yields by Suzuki-Miyaura coupling of 2,4-dichloro-6-methyl-5-nitropyrimidine (3) with various aryl boronic esters (4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i) in the presence of 1,1′- bis(diphenylphosphino)ferrocene dichloropalladium(II) (Pd(dppf) 2Cl2). Further, antibacterial and antioxidant properties were screened for the title compounds 5a, 5b, 5c, 5d, 5e, 5f, 5g, 5h, 5i. Most of the compounds possessed significant activity against Gram-positive bacteria Staphylococcus aureus and Bacillus subtilis and Gram-negative bacteria Escherichia coli and Klebsiella pneumoniae. The antioxidant activity of the title compounds showed significant antioxidant activity when compared with vitamin C.
