An efficient synthesis, characterization, and antimicrobial screening of tetrahydropyrimidine derivatives

被引：10

作者：

Godhani, Dinesh R. ^{[1
]}

Dobariya, Purvesh B. ^{[1
]}

Jogel, Anand A. ^{[1
]}

Sanghani, Anil M. ^{[2
]}

Mehta, Jignasu P. ^{[1
]}

机构：

[1] Maharaja Krishnakumarsinhji Bhavnagar Univ, Dept Chem, Bhavnagar 364022, Gujarat, India

[2] Sir PP Inst Sci, Dept Chem, Bhavnagar 364002, Gujarat, India

来源：

MEDICINAL CHEMISTRY RESEARCH | 2014年 / 23卷 / 05期

关键词：

Tetrahydropyrimidine; Biginelli reaction; Hantzsch reaction; Antibacterial activity; Antifungal activity; CONDENSATION; CHEMISTRY; POTENT;

D O I：

10.1007/s00044-013-0840-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Several new substituted 1,2,3,4-tetrahydropyrimidine derivatives 2a-h have been synthesized by the modified Biginelli and Hantzsch reactions and compounds were characterized by spectral techniques. All compounds were evaluated for their in vitro antimicrobial activity against different strains of Gram-negative (E. coli and P. aeruginosa) and Gram-positive (S. aureus and S. pyogenus) bacteria and selected fungi C. albicans, A. niger, and A. clavatus using serial Broth dilution method (Mueller-Hinton broth dilution method). Compound 2e was found active against both Gram-negative and -positive bacterial strains used for present study, while compound 2b was good active against Gram-negative and S. pyogenus bacterial strains. Compounds 2a-h were not that much significant against (C. albicans, A. niger, and A. clavatus) selected fungal strains.

引用

页码：2417 / 2425

页数：9

共 27 条

[1] Multiple-component condensation strategies for combinatorial library synthesis [J].

Armstrong, RW ;

Combs, AP ;

Tempest, PA ;

Brown, SD ;

Keating, TA .

ACCOUNTS OF CHEMICAL RESEARCH, 1996, 29 (03) :123-131

[2] Microwave-induced bismuth nitrate-catalyzed synthesis of dihydropyrimidones via Biginelli condensation under solventless conditions [J].

Banik, Birnal K. ;

Reddy, Anupama T. ;

Datta, Arup ;

Mukhopadhyay, Chhanda .

TETRAHEDRON LETTERS, 2007, 48 (41) :7392-7394

[3] In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective α1A receptor antagonists for the treatment of benign prostatic hyperplasia [J].

Barrow, JC ;

Nantermet, PG ;

Selnick, HG ;

Glass, KL ;

Rittle, KE ;

Gilbert, KF ;

Steele, TG ;

Homnick, CF ;

Freidinger, RM ;

Ransom, RW ;

Kling, P ;

Reiss, D ;

Broten, TP ;

Schorn, TW ;

Chang, RSL ;

O'Malley, SS ;

Olah, TV ;

Ellis, JD ;

Barrish, A ;

Kassahun, K ;

Leppert, P ;

Nagarathnam, D ;

Forray, C .

JOURNAL OF MEDICINAL CHEMISTRY, 2000, 43 (14) :2703-2718

[4]

Biginelli P., 1893, GAZZ CHIM ITAL, V23, P360

[5]

Clinical and Laboratory Standards Institute (CLSI

[6]

formerly NCCLS), 2008, M7A7 CLSI

[7]

CLSI, 2008, REF METH BROTH DIL A, V28

[8] Solid- and solution-phase synthesis of bioactive dihydropyrimidines [J].

Dallinger, D ;

Stadler, A ;

Kappe, CO .

PURE AND APPLIED CHEMISTRY, 2004, 76 (05) :1017-1024

[9] Inhibition of hepatitis B virus replication by drug-induced depletion of nucleocapsids [J].

Deres, K ;

Schröder, CH ;

Paessens, A ;

Goldmann, S ;

Hacker, HJ ;

Weber, O ;

Krämer, T ;

Niewöhner, U ;

Pleiss, U ;

Stoltefuss, J ;

Graef, E ;

Koletzki, D ;

Masantschek, RNA ;

Reimann, A ;

Jaeger, R ;

Gross, R ;

Beckermann, B ;

Schlemmer, KH ;

Haebich, D ;

Rübsamen-Waigmann, H .

SCIENCE, 2003, 299 (5608) :893-896

[10] An efficient, solvent-free microwave-assisted synthesis and antimicrobial screening of 1,6-dihydropyrimidine analogues [J].

Desai, N. C. ;

Pandya, D. D. ;

Satodiya, H. M. ;

Rajpara, K. M. ;

Joshi, V. V. ;

Vaghani, H. V. .

MEDICINAL CHEMISTRY RESEARCH, 2012, 21 (12) :4412-4421

← 1 2 3 →