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Iradyan, M. A.; Iradyan, N. S.; Stepanyan, G. M.; Arsenyan, F. G.; Paronikyan, G. M.; Darbinyan, G. A.; Kazaryan, E. V.; Garibdzhanyan, B. T.

doi:10.1023/a:1024077408895

Cited by 5 publications

(5 citation statements)

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“…Administration of toxic doses of the drug gave a characteristic pattern of poisoning by alkylating agents, i.e., decreased mass of thymus and spleen and produced internal organ anemia. However, tolerated doses did not cause visible toxic effects and mass loss in the animals [120].…”

Section: Imidazene a New Alkylating Agentmentioning

confidence: 90%

“…As the dose decreased, the antitumor activity decreased regularly. It completely disappeared with a 32-fold reduction of the dose [120].…”

Section: Imidazene a New Alkylating Agentmentioning

confidence: 97%

“…A pronounced antitumor effect (T% = 61 -76) was observed at long test times of 7 d after administration of the drug was complete [119]. Imidazene had a pronounced inhibiting action on growth of Pliss lymphosarcoma, Swetz leukemia, and AKATOL (T% = 65 -86) [120]. Triazene in tests with AKATOL exhibited a therapeutic action both immediately after treatment of animals was complete on the 14 th day (T% = 76) and on the 21 st day (T% = 65 -76) [120].…”

Section: Imidazene a New Alkylating Agentmentioning

confidence: 99%

“…Imidazene had a pronounced inhibiting action on growth of Pliss lymphosarcoma, Swetz leukemia, and AKATOL (T% = 65 -86) [120]. Triazene in tests with AKATOL exhibited a therapeutic action both immediately after treatment of animals was complete on the 14 th day (T% = 76) and on the 21 st day (T% = 65 -76) [120]. Moreover, the compound had a weak therapeutic effect on leukemia strains L 1210, P 388, and hemocytoblastosis La (increased lifespan by 25, 30, and 50%, respectively) [119,120].…”

Section: Imidazene a New Alkylating Agentmentioning

confidence: 99%

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Antitumor activity of imidazole derivatives: dacarbazine and the new alkylating agent imidazene (Review)

Iradyan

Stepanyan

et al. 2010

Pharm Chem J

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The physicochemical properties and antitumor activity of dacarbazine, its analogs, and the new alkylating agent imidazene are reviewed. It is shown that the activity of dacarbazine is superior to most of its analogs. Imidazene exhibits an advantage over dacarbazine with respect to both stability and activity and can be used for the treatment of malignant melanoma and sarcoma of soft tissues and in combined chemotherapy.

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Section: Imidazene a New Alkylating Agentmentioning

confidence: 90%

“…As the dose decreased, the antitumor activity decreased regularly. It completely disappeared with a 32-fold reduction of the dose [120].…”

Section: Imidazene a New Alkylating Agentmentioning

confidence: 97%

Section: Imidazene a New Alkylating Agentmentioning

confidence: 99%

Section: Imidazene a New Alkylating Agentmentioning

confidence: 99%

See 2 more Smart Citations

Antitumor activity of imidazole derivatives: dacarbazine and the new alkylating agent imidazene (Review)

Iradyan

Stepanyan

et al. 2010

Pharm Chem J

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“…Literature is enriched with lot of work on synthesis of potent substituted imidazole derivatives with diverse pharmacological activities [15,16] [17][18][19][20][21][22][23][24][25][26][27][28][29], a novel series of 3,5-diiodo-4-(2-methyl-1H-5-imidazolyl)benzoyl amino acids and peptides with an anticipation to get potent agents of more therapeutic efficacy with lesser adverse effects. Chemistry 4-Amino-3,5-diiodobenzoic acid (1) was prepared according to literature procedure [30] in good yields by iodination of p-aminobenzoic acid (PABA) using iodine monochloride.…”

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confidence: 99%

Synthesis, Spectral and Antimicrobial Studies on some Newer Imidazole Analogs

Dahiya

2008

Sci Pharm

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A novel series of 3,5-diiodo-4-(2-methyl-1H-imidazol-5-yl)benzoic acid analogs of amino acids, dipeptides and tripeptides was synthesized by using dicyclohexylcarbodiimide and diisopropylcarbodiimide (DCC/DIPC) as coupling agents and triethylamine (TEA) as base. Structures of all the newly synthesized compounds were confirmed by elemental analysis and IR, 1 H NMR, 13 C NMR and mass spectral data. Imidazolopeptides were investigated for their antimicrobial activity and some of newly synthesized compounds 2c, 2d, 2h and their hydrolyzed analogs 3b, 3d exhibited potent bioactivity against pathogenic fungi Candida albicans and dermatophytes Trichophyton mentagrophytes and Microsporum audouinii with MIC values of 12.5-6 μg/ml, as compared to the reference druggriseofulvin. In addition, moderate activity against gram negative bacteria Pseudomonas aeruginosa and Klebsiella pneumoniae was also observed for synthesized imidazolopeptides.

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Synthesis and Antimicrobial Evaluation of Some Novel 5‐Phenyl‐5H‐thiazolo[4,3‐b][1,3,4]thiadiazole Systems

Hamama

Ibrahim

Raoof

et al. 2017

Journal of Heterocyclic Chem

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Condensation of 2‐amino‐5‐phenyl‐5H‐thiazolo[4,3‐b] [1,3,4] thiadiazoles (1) with some carboxylic acid derivatives furnished corresponding compounds 2–4, respectively. Alkylation of 1 with benzoylchloride and 4‐chlorobenzyl chloride afforded thiazolo[4,3‐b][1,3,4]thiadiazole derivatives 5 and 6, respectively. Similarly, transformation of 1 with chloroacetyl chloride yielded chloroacetamide derivative 7. The later compound was subjected to react with potassium thiocyanate or piperazine whereby, the binary thiazolidinone derivative 8 and N1,N4‐disubstituted piperazine 9 were produced, respectively. Also, the reactivity of 1 toward various active methylene reagents was investigated. Accordingly, our attempts to synthesize the tricyclic heterocyclic system 10, 11′, 12′ by reaction of 1 with chloroacetonitrile, 4‐oxo‐4‐phenylbutanoic acid and/or diethylmalonate in presence of acetyl chloride was furnished 10, 11, and 12. The newly synthesized compounds were screened as antimicrobial agent.

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Cited by 5 publications

References 0 publications

Antitumor activity of imidazole derivatives: dacarbazine and the new alkylating agent imidazene (Review)

Antitumor activity of imidazole derivatives: dacarbazine and the new alkylating agent imidazene (Review)

Synthesis, Spectral and Antimicrobial Studies on some Newer Imidazole Analogs

Synthesis and Antimicrobial Evaluation of Some Novel 5‐Phenyl‐5H‐thiazolo[4,3‐b][1,3,4]thiadiazole Systems

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