The Effect of Carboxamide/Sulfonamide Replacement in Arylpiperazinylalkyl Derivatives on Activity to Serotonin and Dopamine Receptors
A series of carboxamide and sulfonamide alkyl (p‐xylyl and benzyl) 1‐(2‐methoxyphenyl)piperazine (o‐OMe‐PhP) and 1‐(2,3‐dichlorophenyl)piperazine (2,3‐DCPP) analogs were prepared and tested for their affinity to bind to serotonin 5‐HT1A/5‐HT6/5‐HT7 and dopamine D2 receptors. This chemical modification let us explore the impact of the replacement of the carboxamide by the sulfonamide group on the affinity changes. In both the o‐OMe‐PhP and 2,3‐DCPP series, the relative activities of the carboxamides versus sulfonamides toward the 5‐HT1A/5‐HT6/5‐HT7 and D2 receptors show similar trends. Vari...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Piotr Kowalski, Pawe ł Śliwa, Grzegorz Satała, Rafał Kurczab, Ilona Bartos, Karol Zuchowicz Tags: Full Paper Source Type: research
Pharmacological Evaluation of Novel Isonicotinic Carboxamide Derivatives as Potential Anti ‐Hyperlipidemic and Antioxidant Agents
This study revealed the antihyperlipidemic activities of some of the newly synthesized, novel carboxamide derivatives, mainly C4 and C12 (p < 0.05). The majority of the compounds displayed a relatively low or no DPPH radical scavenging effect, with C20 possessing the best radical scavenging effect (22%) among all. This research opens the door for new potential antihyperlipidemic compounds derived from isonicotinic acid. N‐(3‐Benzoylphenyl)pyridine‐4‐carboxamide (C4) was found to have promising lipid‐lowering and antioxidant effects, which may create a protective effect against CVDs, by reducing the LDL‐C...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Rana Abu Farha, Yasser Bustanji, Yusuf Al ‐Hiari, Sanaa Bardaweel, Tariq Al‐Qirim, Ghassan Abu Sheikha, Rabab Albashiti Tags: Full Paper Source Type: research
Molecular Engineering of Tetracyclic 2,3 ‐Dihydro‐1H‐benzo[2,3]‐benzofuro[4,5‐e][1,3]oxazine Derivatives: Evaluation for Potential Anticancer Agents
Water‐mediated one‐pot Mannich type condensation of dibenzo[b,d]furan‐2‐ol with different amines resulted in a large library of novel 2,3‐dihydro‐1H‐benzo[2,3]benzofuro[4,5‐e][1,3]oxazine derivatives in moderate to excellent yields. The ortho‐aminomethylation of the dibenzofuranols proceeded smoothly in the presence of various aromatic/aliphatic amines and paraformaldehyde, followed by cyclization. All the newly synthesized tetracyclic 2,3‐dihydro‐1H‐benzo[2,3]benzofuro[4,5‐e][1,3]oxazine derivatives were chemically characterized and screened for their cytotoxicity activity by cell viability assay...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Vinayak Botla, NavyaSree Pilli, Dhevendar Koude, Sunil Misra, Chandrasekharam Malapaka Tags: Full Paper Source Type: research
Aromatic Regions Govern the Recognition of NADPH Oxidase Inhibitors as Diapocynin and its Analogues
In conclusion, targeting the aromatic region of p47phox through π‐interactions is important for inhibiting NOX activity.
Compound C8, one of the 18 designed compounds with chemical relationship to the NOX2 inhibitor diapocynin (C1), forms π–π interactions with the NOX2 subunit p47phox and exhibits antioxidant properties by inhibiting ROS production in endothelial cells. Targeting the aromatic region of p47phox through π‐interactions is important for inhibiting NOX activity. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Martha E. Mac ías Pérez, Maricarmen Hernández Rodríguez, Laura C. Cabrera Pérez, M. Jonathan Fragoso‐Vázquez, José Correa‐Basurto, Itzia I. Padilla‐Martínez, David Méndez Luna, Elvia Mera Jiménez, César Flores Sandoval, Feliciano Tamay Ca Tags: Full Paper Source Type: research
Diarylpyrazole Ligated Dihydropyrimidine Hybrids as Potent Non ‐Classical Antifolates and Their Efficacy Against Plasmodium falciparum
A series of diarylpyrazole clubbed dihydropyrimidine derivatives (J1–J30) was synthesized under microwave‐assisted heating conditions by employing Biginelli reaction methodology and utilizing triethylammonium acetate both as a catalyst and as reaction medium, leading towards a greener reaction pathway. The synthesized entities were screened for their antimalarial efficacy against a Plasmodium falciparum strain in vitro. The active entities (J9, J15, J21, J25, and J27) obtained out of the in vitro screening were further evaluated for their enzyme inhibitory potency against the Pf‐DHFR enzyme in vitro as well as in sil...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Jaimin D. Bhatt, Chaitanya J. Chudasama, Kanuprasad D. Patel Tags: Full Paper Source Type: research
Synthesis of Some Novel 2,6 ‐Disubstituted Pyridazin‐3(2H)‐one Derivatives as Analgesic, Anti‐Inflammatory, and Non‐Ulcerogenic Agents
Some novel 2,6‐disubstituted pyridazine‐3(2H)‐one derivatives were synthesized and evaluated for in vitro cyclooxygenase‐2 (COX‐2) inhibitory efficacy. Compounds 2‐{[3‐(2‐methylphenoxy)‐6‐oxopyridazin‐1(6H)‐yl]methyl}‐1H‐isoindole‐1,3(2H)‐dione (5a), 2‐propyl‐6‐(o‐tolyloxy)pyridazin‐3(2H)‐one (6a), and 2‐benzyl‐6‐(3,5‐dimethyl‐1H‐pyrazol‐1‐yl)pyridazin‐3(2H)‐one (16a) showed the most potent COX‐2 inhibitory activity with IC50 values of 0.19, 0.11, and 0.24 μM, respectively. The synthesized compounds with the highest COX‐2 selectivity indices were evalua...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Tamer H. Ibrahim, Yasser M. Loksha, Hosam A. Elshihawy, Dina M. Khodeer, Mohamed M. Said Tags: Full Paper Source Type: research
New Coumarin Derivatives as Anti ‐Breast and Anti‐Cervical Cancer Agents Targeting VEGFR‐2 and p38α MAPK
Breast and cervical cancers are the most common gender‐specific cancers affecting women worldwide. In this investigation, we highlighted the synthesis, VEGFR‐2 and p38α MAPK inhibitory activity of new series of fluorinated coumarin‐based derivatives featuring a variety of bioactive chemical moieties attached or fused to the coumarin nucleus at the 3 and/or 4 position. The bioactive inhibitors were further assessed for their anti‐proliferative effect against human MCF‐7 breast cancer and HeLa cervical cancer cell lines, respectively. Most of the tested compounds showed potent preferential inhibition effects again...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Rasha Z. Batran, Dina H. Dawood, Samia A. El ‐Seginy, Mamdouh M. Ali, Timothy J. Maher, Kuljeet S. Gugnani, Alejandro N. Rondon‐Ortiz Tags: Full Paper Source Type: research
Some Novel Mannich Bases of 5 ‐(3,4‐Dichlorophenyl)‐1,3,4‐oxadiazole‐2(3H)‐one and Their Anti‐Inflammatory Activity
Non‐steroidal anti‐inflammatory drugs (NSAIDs), which are widely used for the treatment of rheumatic arthritis, pain, and many different types of inflammatory disorders, cause serious gastrointestinal (GI) side effects. The free carboxylic acid group existing on their chemical structure is correlated with GI toxicity related with all routine NSAIDs. Replacing this functional group with the 1,3,4‐oxadiazole bioisostere is a generally used strategy to obtain an anti‐inflammatory agent devoid of GI side effects. In the present work, a novel group of 5‐(3,4‐dichlorophenyl)‐1,3,4‐oxadiazole‐2(3H)‐one Mannich...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Meric Koksal, Irem Ozkan ‐Dagliyan, Tugce Ozyazici, Beril Kadioglu, Hande Sipahi, Ayhan Bozkurt, Suleyman S. Bilge Tags: Full Paper Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (8/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Tags: Editorial Board Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (8/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
Design, Synthesis, and the Biological Evaluation of a New Series of Acyclic 1,2,3 ‐Triazole Nucleosides
A new strategy for the synthesis of N3‐benzoylated‐ and N3‐benzylated N1‐propargylquinazoline‐2,4‐diones 30a−d and 31a−d from isatoic anhydride 41 is reported. The alkynes 30a−d and 31a−d were applied in the 1,3‐dipolar cycloadditions with azides 27 and 28 to synthesize acyclic 1,2,3‐triazole nucleosides. The obtained alkynes and 1,2,3‐triazole were evaluated for antiviral activity against a broad range of DNA and RNA viruses. The alkyne 30d showed activity against adenovirus‐2 (EC50 = 8.3 μM), while compounds 37a and 37d were also active toward herpes simplex virus‐1 wild‐type and th...
Source: Archiv der Pharmazie - August 1, 2017 Category: Drugs & Pharmacology Authors: Iwona E. G łowacka, Graciela Andrei, Dominique Schols, Robert Snoeck, Katarzyna Gawron Tags: Full Paper Source Type: research
Centennial Anniversary of Mannich's Report on the Formation of β‐Amino‐Ketones in the Archiv der Pharmazie
In order to commemorate Carl Mannich's achievement with many implications in the fields of drug design and synthesis, stability of pharmaceutical preparations, and natural product chemistry, we invited researchers to submit their work related to Mannich's pioneering article at the occasion of its centennial anniversary to the Archiv der Pharmazie − where else? (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 3, 2017 Category: Drugs & Pharmacology Authors: Andreas Link Tags: Editorial Source Type: research
Editorial Board: Arch. Pharm. Chem. Life Sci. (7/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 3, 2017 Category: Drugs & Pharmacology Tags: Editorial Board Source Type: research
Cover Picture: Arch. Pharm. Chem. Life Sci. (7/2017)
(Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 3, 2017 Category: Drugs & Pharmacology Tags: Cover Picture Source Type: research
Design, Synthesis, and Docking Study of Pyrimidine –Triazine Hybrids for GABA Estimation in Animal Epilepsy Models
A series of new pyrimidine–triazine hybrids (4a–t) was designed and synthesized, from which potent anticonvulsant agents were identified. Most of the compounds exhibited promising anticonvulsant activity against the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) tests, along with minimal motor impairment with higher safety compared to the standard drugs, phenytoin and carbamazepine. In the series, 5‐(4‐(4‐fluorophenyl)‐6‐(4‐hydroxyphenyl)‐2‐thioxo‐5,6‐dihydropyrimidin‐1(2H)‐yl)‐1,2‐dihydro‐1,2,4‐triazin‐3(6H)‐one (4o) and 5‐(6‐(4‐hydroxy‐3‐methoxyphe...
Source: Archiv der Pharmazie - July 1, 2017 Category: Drugs & Pharmacology Authors: Meeta Sahu, Nadeem Siddiqui, Mohd. Javed Naim, Ozair Alam, Mohammad Shahar Yar, Vidushi Sharma, Sharad Wakode Tags: Full Paper Source Type: research
