Studies on Antiulcer Agents. II. Antiulcer Properties of N-(1H-Tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamides Inhibiting Release of Histamine from Passively Sensitized Rat Peritoneal Mast Cells.

Terashima, Koichi; Tanimura, Teru; Shimamura, Hiroshi; Kawase, Akira; Uenishi, Keiji; Tanaka, Yuji; Kimura, Isami; Kamisaki, Toshiaki; Ishizuka, Yasuhiro; Sato, Makoto

doi:10.1248/cpb.43.1042

Cited by 18 publications

(8 citation statements)

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“…For example “Losartan” is an angiotensin II receptor antagonist , “Tomelukast” (LY‐171883) mimics the cysteinyl glycine terminus of growth hormone LTD 4 also functions as a potent anti‐asthmatic drug , and “BMS‐317180” is a potent oral agonist of the human growth hormone secretagogue receptor . Their derivatives were also reported to possess broad spectrum of biological activity in both medicinal and pharmaceutical areas such as antibacterial , antinociceptive , immunosuppressive , antifungal , anticancer, anti‐inflammatory , antiulcer , antiproliferative , antianalgesic , and antiallergic activities.…”

Section: Introductionmentioning

confidence: 99%

Retracted: Synthesis, Molecular Properties, and Biological Evaluation of Hybrid 1,2,3‐Triazolylpolyaza Heterocyclic Compounds

Dasari

Subbaiah

Vadali

et al. 2018

Journal of Heterocyclic Chem

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In this research article, a highly efficient, cost‐effective synthesis of various hybrid molecules possessing 1,2,3‐triazolyltetrazoles and evaluation of their biological activity have been addressed. The structure elucidation of these new library hybrid molecules has been carried out by IR, 1H NMR, 13C NMR, and mass spectral analysis. The compounds have been screened for their anticancer activity against human colon cancer cell line Colo‐205 and human lung cancer cell line HOP‐205, and the results attest that most of the compounds have shown very good therapeutic nature. In particular, compounds 3d, 3j, 6a, and 6e were more cytotoxic than Adriamycin against all tested human cancer cell lines with 68%, 101.8%, 94%, and 104.5% growth, respectively. In the present investigation, a series of 3a–j and 6a–h were subjected to molecular properties prediction, drug likeness by Molinspiration, and toxicity risks by Molsoft software programs. All the 18 analogues were chosen on the basis of Lipinski “Rule of five” for the synthesis, screening their antibacterial and anticancer as oral bioavailable drugs/leads.

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Section: Introductionmentioning

confidence: 99%

Retracted: Synthesis, Molecular Properties, and Biological Evaluation of Hybrid 1,2,3‐Triazolylpolyaza Heterocyclic Compounds

Dasari

Subbaiah

Vadali

et al. 2018

Journal of Heterocyclic Chem

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“…This functional group can take different roles including as a ligand in coordination chemistry, as a metabolically stable surrogate for a carboxylic acid group in medicinal chemistry, 13,14 and as a carboxylic acid isostere. 15 5-Substituted-tetrazoles are reported to possess antibacterial, 16 antifungal, 17 antiviral, 18 analgesic, 19−23 anti-inflammatory, 24,25 antiulcer, 26 and antihypertensive activities; 27 for instance, irbesartan (22), valsartan (23), tasosartan (24), and losartan (25) (Figure 1). Moreover, it needs to be added that the whole tetrazole function is metabolically stable.…”

Section: Introductionmentioning

confidence: 99%

New tetrazolic azo dyes linked to (thio)barbiturate and electron-rich aromatics as potential antimicrobial agents

Pesyan

Soleimani²,

Jazani³

2015

Turk J Chem

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A series of new tetrazolic azo dyes based on (thio)barbiturate and electron-rich aromatics were synthesized in excellent yield. The electron-donor and tetrazole ring moieties were linked by a p -phenylazo bridge and the structural characterizations were achieved by FT IR, 1 H and 13 C NMR, and UV-visible spectrometry. The antibacterial activity of the synthesized compounds was tested against gram-positive and gram-negative bacterial strains, namely Acinetobacter calcoaceticus (ATCC23055), Escherichia coli (ATCC2592), Pseudomonas aeruginosa (ATCC27853), and Staphylococcus aureus (ATCC25923). As a result, potential antimicrobial effects were seen for some of the synthesized compounds.

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“…5-Substituted tetrazoles are reported to possess antibacterial 1 , antifungal 2 , antiviral 3 , analgesic 4,5 , anti-inflammatory 6 , antiulcer 7 and antihypertensive 8 activities. The tetrazole function is metabolically stable 9 .…”

Section: Introductionmentioning

confidence: 99%

X-Ray, IR, NMR, UV-visible spectra and DFT analysis of 5-aryloxy-(1H)-tetrazoles, structure, conformation and tautomerism

Pesyan¹,

Bavafa²,

Enayati³

et al. 2014

10.5267/j.ccl

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The predominant tautomeric forms of N1-H, N2-H of 5-(2,6-dimethyl-and 5-(2,6-diisopropylphenoxy)-(1H)-tetrazoles were analyzed at B3LYP method using 6-311G(d,p) basis set in the gas phase. The N1-H form of tetrazoles was found to be more stable than N2-H form in both solid and gas phases. Crystal structures of both tetrazoles show an intermolecular Hbond between N1-H and N4 atom of other tetrazole space. The hydrogen bonds between each tautomer of tetrazoles were evaluated at B3LYP/6-311G(d,p) level. The geometrical parameters and spectral data of tetrazoles and their variation were studied in both solid and gas phases.

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Studies on Antiulcer Agents. II. Antiulcer Properties of N-(1H-Tetrazol-5-yl)-2-anilino-5-pyrimidinecarboxamides Inhibiting Release of Histamine from Passively Sensitized Rat Peritoneal Mast Cells.

Cited by 18 publications

References 0 publications

Retracted: Synthesis, Molecular Properties, and Biological Evaluation of Hybrid 1,2,3‐Triazolylpolyaza Heterocyclic Compounds

Retracted: Synthesis, Molecular Properties, and Biological Evaluation of Hybrid 1,2,3‐Triazolylpolyaza Heterocyclic Compounds

New tetrazolic azo dyes linked to (thio)barbiturate and electron-rich aromatics as potential antimicrobial agents

X-Ray, IR, NMR, UV-visible spectra and DFT analysis of 5-aryloxy-(1H)-tetrazoles, structure, conformation and tautomerism

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