Non ‐peptide‐based new class of platelet aggregation inhibitors: Design, synthesis, bioevaluation, SAR, and in silico studies
Abstract
A series of 2‐oxo‐2‐phenylethylidene linked 2‐oxo‐benzo[1,4]oxazine analogues 17a–x and 18a–o, incorporated with a variety of electron‐withdrawing as well as electron‐donating groups at ring A and ring C, were synthesized under greener conditions in excellent yields (up to 98%). These analogues 17a–x and 18a–o were evaluated for their arachidonic acid (AA)‐induced platelet aggregation inhibitory activities in comparison with the standard reference aspirin (IC50 = 21.34 ± 1.09 µg/mL). Among all the screened compounds, eight analogues, 17i, 17x, 18f, 18g, 18h, 18i, 18l, and 18o, w...
Source: Archiv der Pharmazie - March 9, 2018 Category: Drugs & Pharmacology Authors: Pradeep K. Jaiswal, Vashundhra Sharma, Surendra Kumar, Manas Mathur, Ajit K. Swami, Dharmendra K. Yadav, Sandeep Chaudhary Tags: FULL PAPER Source Type: research
Synthesis, p38 α MAP kinase inhibition, anti‐inflammatory activity, and molecular docking studies of 1,2,4‐triazole‐based benzothiazole‐2‐amines
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - March 8, 2018 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie, Ahead of Print. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - March 8, 2018 Category: Drugs & Pharmacology Source Type: research
Synthesis, docking, in vitro and in vivo antidiabetic activity of pyrazole ‐based 2,4‐thiazolidinedione derivatives as PPAR‐γ modulators
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 5, 2018 Category: Drugs & Pharmacology Source Type: research
Design, synthesis, and biological evaluation of novel 1,2 ‐diaryl‐4‐substituted‐benzylidene‐5(4H)‐imidazolone derivatives as cytotoxic agents and COX‐2/LOX inhibitors
Archiv der Pharmazie, EarlyView. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 5, 2018 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie, Ahead of Print. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 5, 2018 Category: Drugs & Pharmacology Source Type: research
Design, synthesis, and biological evaluation of novel 1,2 ‐diaryl‐4‐substituted‐benzylidene‐5(4H)‐imidazolone derivatives as cytotoxic agents and COX‐2/LOX inhibitors
Abstract
A new series of 1,2‐diaryl‐4‐substituted‐benzylidene‐5(4H)‐imidazolone derivatives 4a–l was synthesized. Their structures were confirmed by different spectroscopic techniques (IR, 1H NMR, DEPT‐Q NMR, and mass spectroscopy) and elemental analyses. Their cytotoxic activities in vitro were evaluated against breast, ovarian, and liver cancer cell lines and also normal human skin fibroblasts. Cyclooxygenase (COX)‐1, COX‐2 and lipoxygenase (LOX) inhibitory activities were measured. The synthesized compounds showed selectivity toward COX‐2 rather than COX‐1, and the IC50 values (0.25–1.7 µM) ...
Source: Archiv der Pharmazie - February 5, 2018 Category: Drugs & Pharmacology Authors: Phoebe F. Lamie, John N. Philoppes, Lucie R árová Tags: FULL PAPER Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (2/2018)
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (2/2018)
Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Source Type: research
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Archiv der Pharmazie,Volume 351, Issue 2, February 2018. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Source Type: research
Fungal biofilm inhibition by piperazine ‐sulphonamide linked Schiff bases: Design, synthesis, and biological evaluation
We report the synthesis of some new piperazine‐sulphonamide linked Schiff bases as fungal biofilm inhibitors with antibacterial and antifungal potential. The biofilm inhibition result of Candida albicans proposed that the compounds 6b (IC50 = 32.1 μM) and 6j (IC50 = 31.4 μM) showed higher inhibitory activity than the standard fluconazole (IC50 = 40 μM). Compound 6d (MIC = 26.1 μg/mL) with a chloro group at the para position was found to be the most active antibacterial agent of the series against Bacillus subtilis when compared with the standard ciprofloxacin (MIC = 50 μg/mL). Compound ...
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Authors: Rajendra H. Patil, Firoz A. Kalam Khan, Kaivalya Jadhav, Manoj Damale, Siddique Akber Ansari, Hamad M. Alkahtani, Azmat Ali Khan, Shantanu D. Shinde, Rajesh Patil, Jaiprakash N. Sangshetti Tags: FULL PAPER Source Type: research
Novel spiro ‐thiazolidin‐4‐one and thioether derivatives of benzylidene flavanones: New leads in cancer and microbial chemotherapy
Abstract
The synthesis of spiro‐thiazolidin‐4‐one and thioether derivatives of substituted E‐3‐benzylidene flavanones is reported for the first time. All new compounds were characterized by different spectroscopic techniques and elemental analyses. The in vitro anticancer activities were assessed against the full NCI 60 cell line panel representing nine types of human cancers, at 10‐fold dilutions at five different concentrations (0.01, 0.1, 1, 10, and 100 μM. Compound 2a gave noteworthy results in the case of colon (HT29), CNS (SNB‐75), melanoma (LOX‐IMVI), and renal (ACNH) cells, where the reduction in...
Source: Archiv der Pharmazie - February 1, 2018 Category: Drugs & Pharmacology Authors: Sayeed Mukhtar, Meshari A. Alsharif, Mohammed I. Alahmdi, Humaira Parveen, Asad U. Khan Tags: FULL PAPER Source Type: research
