300667-79-2Relevant academic research and scientific papers
P-dodecylbenzenesulfonic acid (DBSA), a Br?nsted acid-surfactant catalyst for Biginelli reaction in water and under solvent free conditions
Bigdeli, Mohammad Ali,Gholami, Ghazaleh,Sheikhhosseini, Enayatollah
, p. 903 - 906 (2011)
We report herein the use of p-dodecylbenzenesulfonic acid (DBSA) as a catalyst for a one-pot Biginelli reaction to afford 3,4-dihydropyrimidinone derivatives in good to excellent yields. This reaction proceeds efficiently in water and under solvent free conditions. Comparisons of results indicate that although the yields are high and comparable for both methods, the reaction times are considerably shorter under solvent free conditions.
Design, Synthesis, and Anti-HIV-1 Evaluation of a Novel Series of 1,2,3,4-Tetrahydropyrimidine-5-Carboxylic Acid Derivatives
Sepehri, Saghi,Soleymani, Sepehr,Zabihollahi, Rezvan,Aghasadeghi, Mohammad R.,Sadat, Mehdi,Saghaie, Lotfollah,Memarian, Hamid R.,Fassihi, Afshin
, (2018/04/10)
A series of tetrahydropyrimidine derivatives (2a – 2l) were designed, synthesized, and screened for anti-HIV-1 properties based on the structures of HIV-1 gp41 binding site inhibitors, NB-2 and NB-64. A computational study was performed to predict the pharmacodynamics, pharmacokinetics, and drug-likeness features of the studied molecules. Docking studies revealed that the carboxylic acid group in the molecules forms salt bridges with either Lys574 or Arg579. Physiochemical properties (e.g., molecular weight, number of hydrogen bond donors, number of hydrogen bond acceptors, and number of rotatable bonds) of the synthesized compounds confirmed and exhibited that these compounds were within the range set by Lipinski's rule of five. Compounds 2e and 2k with 4-chlorophenyl substituent and 4-methylphenyl group at C(4) position of the tetrahydropyrimidine ring was the most potent one among the tested compounds. This suggests that these compounds may serve as leads for development of novel small-molecule HIV-1 inhibitors.
