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Start Over Descriptor "[1" Journal chemical biology & drug design
3 results on '"[1"'

1. Design, synthesis, and biological evaluation of piperidinyl‐substituted [1,2,4]triazolo[1,5‐a]pyrimidine derivatives as potential anti‐HIV‐1 agents with reduced cytotoxicity

Author

Boshi Huang, Ye Tian, Peng Zhan, Dirk Daelemans, Dongwei Kang, Erik De Clercq, Christophe Pannecouque, and Xinyong Liu

Subjects
Etravirine, Chemistry, Medicinal, anti-HIV-1 potency, 01 natural sciences, Biochemistry, chemistry.chemical_compound, Drug Discovery, Pharmacology & Pharmacy, DRUG, Cytotoxicity, Biological evaluation, Chemistry, reduced cytotoxicity, HIV Reverse Transcriptase, Molecular Docking Simulation, Reverse Transcriptase Inhibitors, Molecular Medicine, Life Sciences & Biomedicine, medicine.drug, Biochemistry & Molecular Biology, Pyrimidine, Anti-HIV Agents, Cell Survival, Stereochemistry, Cell Line, Structure-Activity Relationship, reverse transcriptase, medicine, Humans, Potency, OPTIMIZATION, EC50, Pharmacology, Science & Technology, Binding Sites, 010405 organic chemistry, Organic Chemistry, BEARING BRIDGEHEAD NITROGEN, molecular docking, Triazoles, DIARYLPYRIMIDINES, Reverse transcriptase, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Pyrimidines, 4]Triazolo[1, Design synthesis, DISCOVERY, Drug Design, 5-a]pyrimidines, HIV-1, POTENCY, [1, HIV-1 NNRTIS, INHIBITORS
Abstract

Taking the previously reported compound BH-7d as the lead, we designed and synthesized a series of piperidinyl-substituted [1,2,4]triazolo[1,5-a]pyrimidines, and their anti-HIV activities as well as cytotoxicities were evaluated. Several compounds exhibited moderate anti-HIV (IIIB) potency, among which 2b was the most active one (EC50 = 4.29 μM). Structure-activity relationships derived from the antiretroviral results were analyzed. Additionally, most compounds demonstrated reduced cytotoxicity (CC50 > 200 μM) compared with those of BH-7d and etravirine. Molecular docking study further revealed the binding conformation of 2b in the binding pocket of HIV-1 reverse transcriptase. ispartof: CHEMICAL BIOLOGY & DRUG DESIGN vol:97 issue:1 pages:67-76 ispartof: location:England status: published

Published
2020

2. Synthesis of 2-(4-Substitutedbenzyl-[1,4]Diazepan-1-yl)- N-(1-Methyl-4,5-Dihydro-[1,2,4]Triazolo[4,3- A]Quinolin-7-Yl)Acetamides as Inotropic Agents.

Author

Bai-Jun Ye, Xue-Kun Liu, Sheng-Ming Jiang, Xun Cui, and Hu-Ri Piao

Subjects
*CARDIOTONIC agents, *MILRINONE, *ACETAMIDE, *HEART atrium, *CEREBROVASCULAR disease
Abstract

In an attempt to search for more potent positive inotropic agents, a series of N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3- a]quinolin-7-yl)-2-(substitutedbenzyl-[1,4]diazepan-1-yl)acetamides were synthesized and evaluated for positive inotropic activity by measuring left atrium stroke volume in isolated rabbit heart preparations. Some of these derivatives exhibited favorable activity compared with the standard drug, milrinone, among which 2-(4-(4-methylbenzyl)-[1,4]-diazepan-1-yl)- N-(4,5-dihydro-1-methyl-[1,2,4]triazolo[4,3- a]quinolin-7-yl)acetamide () was the most potent, increasing stroke volume by 8.38 ± 0.16% (milrinone 2.45 ± 0.06%) at 3 × 10 . The chronotropic effects of those compounds having inotropic effects were also evaluated in this work. [ABSTRACT FROM AUTHOR]

Published
2011
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3. Synthesis and Biological Evaluation of Mercapto Triazolo-Benzothiadiazine Linked Aminobenzothiazoles as Potential Anticancer Agents.

Author

Kamal, Ahmed, Khan, Mohammed Naseer A., Srikanth, Yellamelli V. V., and Rajesh, Shetti V. C. R. N. C.

Subjects
*ANTINEOPLASTIC agents, *BIOSYNTHESIS, *CANCER cells, *REGULATION of cell growth, *CELL lines, *CHEMICAL reactions, *THIOLS, *DRUG development, *THERAPEUTICS, *CANCER treatment
Abstract

The synthesis of a series of 10-substituted 5,5-dioxo-5,10-dihydro[1,2,4]triazolo[4,3- b][1,2,4]benzothiadiazine coupled with sulfanylacetamido benzothiazole pharmacophores ( 5a– g) is described. All the synthesized compounds have been evaluated for their anticancer activity. Most of the compounds showed significant growth inhibitory activity against selected human tumor cell lines. Interestinlgy, one of the synthesized compounds 5d, exhibited GI50 values of 1.4 and 2.1 μm against RPMI-8226 (leukemia) and HOP-62 (lungs) cell lines, respectively. [ABSTRACT FROM AUTHOR]

Published
2009
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