Preparation, Isolation, and Structural Characterization of Lewis Base Iminium Salts of 1,8-Diazabicyclo[5.4.0]undec-7-ene and Their Application as Green Reagents in an Aqueous Medium.

We report a state-of-the-art synthesis and isolation procedure for 13 Lewis base iminium salts (LBI) of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU), confirming their structures meticulously by different spectral data.

Review on recent advances in cellulose nanofibril based hybrid aerogels: Synthesis, properties and their applications.

With the depletion of fossil fuels and growing environmental concerns, the modernized era of technology is in desperate need of sustainable and eco-friendly materials. The industrial sector surely has enough resources to produce cost-effective, renewable, reusable, and sustainable raw materials. The family of very porous solid materials known as aerogels has a variety of exceptional qualities, such as high porosity, high specific surface area, ultralow density, and superior thermal, acoustic, and dielectric properties.

Recent Progress in the Multicomponent Synthesis of Pyran Derivatives by Sustainable Catalysts under Green Conditions.

Pyrans are one of the most significant skeletons of oxygen-containing heterocyclic molecules, which exhibit a broad spectrum of medicinal applications and are constituents of diverse natural product analogues. Various biological applications of these pyran analogues contributed to the growth advances in these oxygen-containing molecules. Green one-pot methodologies for synthesising these heterocyclic molecules have received significant attention.

Recent Progresses in the Multicomponent Synthesis of Dihydropyridines by Applying Sustainable Catalysts Under Green Conditions.

The synthesis of dihydropyridines, valuable molecules with diverse therapeutic properties, using eco-friendly heterogeneous catalysts as a green alternative received significant consideration. By selecting appropriate precursors, these compounds can be readily modified to induce the desired properties in the target product. This review focused on synthesising diverse dihydropyridine derivatives in single-pot reactions using magnetic, silica, and zirconium-based heterogeneous catalytic systems.

Multicomponent reaction for the synthesis of new 1,3,4-thiadiazole-thiazolidine-4-one molecular hybrids as promising antidiabetic agents through α-glucosidase and α-amylase inhibition.

A simple and efficient protocol was developed to synthesize a new library of thiazolidine-4-one molecular hybrids (4a-n) via a one-pot multicomponent reaction involving 5-substituted phenyl-1,3,4-thiadiazol-2-amines, substituted benzaldehydes and 2-mercaptoacetic acid. The synthesized compounds were evaluated in vitro for their antidiabetic activities through α-glucosidase and α-amylase inhibition as well as their antioxidant and antimicrobial potentials. Compound 4e exhibited the most promising α-glucosidase and α-amylase inhibition with an IC value of 2.

Advances in Pyranopyrazole Scaffolds' Syntheses Using Sustainable Catalysts-A Review.

Heterogeneous catalysis plays a crucial role in many chemical processes, including advanced organic preparations and the design and synthesis of new organic moieties. Efficient and sustainable catalysts are vital to ecological and fiscal viability. This is why green multicomponent reaction (MCR) approaches have gained prominence.

A Facile and Catalyst-Free Microwave-Promoted Multicomponent Reaction for the Synthesis of Functionalised 1,4-Dihydropyridines With Superb Selectivity and Yields.

We report a highly efficient green protocol for developing a novel library of 1,2,4-triazole-tagged 1,4-dihydropyridine analogs through the one-pot process from the four-component fusion of the 1-1,2,4-triazol-3-amine with different chosen aldehydes, diethyl acetylenedicarboxylate, and active methylene compounds in a water medium under microwave irradiation and catalyst-free conditions. Excellent yields (94-97%) of the target products were achieved with high selectivity with a short reaction time (<12 min) at room temperature. The structures of the synthesized pyrimidine analogs were established by NMR and HRMS spectroscopic analysis.

Synthesis of 1H-1,2,3-Triazole-Linked Quinoline-Isatin Molecular Hybrids as Anti-Breast Cancer and Anti-Methicillin-Resistant Staphylococcus aureus (MRSA) Agents.

Background: The persistence of breast cancer as the leading cause of mortality among women, coupled with drug resistance to tamoxifen, the standard endocrine therapy for the disease, exacts continuous attention. To this effect, molecular hybridisation offers an attractive route to drugs with improved bioactivity profiles.

Objective: The primary goal of this study was to examine the potential of 1H-1,2,3-triazole linked quinolineisatin molecular hybrids as drug candidates against breast cancer and Methicillin-Resistant Staphylococcus aureus (MRSA) cells.

Synthesis of indole-tethered [1,3,4]thiadiazolo and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids as anti-pancreatic cancer agents.

New indole-tethered [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one (8a-j) and [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids (9a-e) were synthesized using [4+2] cycloaddition reactions of functionalized 1,3-diazabuta-1,3-dienes with indole-ketenes. All molecular hybrids were structurally characterized by spectroscopic techniques (IR, NMR, and HRMS) and screened for their anti-pancreatic cancer activity in vitro. The [1,3,4]oxadiazolo[3,2-a]pyrimidin-5-one hybrids (9a-e) showed stronger anti-pancreatic cancer activity than the [1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one hybrids (8a-j) against the PANC-1 cell line.

Synthesis, antimicrobial evaluation, and in silico studies of quinoline-1H-1,2,3-triazole molecular hybrids.

Antimicrobial resistance has become a significant threat to global public health, thus precipitating an exigent need for new drugs with improved therapeutic efficacy. In this regard, molecular hybridization is deemed as a viable strategy to afford multi-target-based drug candidates. Herein, we report a library of quinoline-1H-1,2,3-triazole molecular hybrids synthesized via copper(I)-catalyzed azide-alkyne [3 + 2] dipolar cycloaddition reaction (CuAAC).

Green synthesis and characterisation of novel [1,3,4]thiadiazolo/benzo[4,5]thiazolo[3,2-]pyrimidines multicomponent reaction using vanadium oxide loaded on fluorapatite as a robust and sustainable catalyst.

We synthesised materials with different loadings of vanadia on fluorapatite (VO/FAp), fully characterised their structural properties using various spectral techniques including TEM, BET, XRD, FT-IR, SEM and EDX and assessed their prowess as catalysts. The 2.5% VO/FAp exhibited excellent activity for the synthesis of novel [1,3,4]thiadiazolo[3,2-]pyrimidines and benzo[4,5]thiazolo[3,2-]pyrimidines.

A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications.

The analogs of nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In the forthcoming decade, a much greater share of new nitrogen-based pharmaceuticals is anticipated.

A comparison between observed and DFT calculations on structure of 5-(4-chlorophenyl)-2-amino-1,3,4-thiadiazole.

The crystal and molecular structure of 5-(4-chlorophenyl)-2-amino-1,3,4-thiadiazole 3 was reported, which was characterized by various spectroscopic techniques (FT-IR, NMR and HRMS) and single-crystal X-ray diffraction. The crystal structure 3 (CHClNS) crystallized in the orthorhombic space group Pna2 and the unit cell consisted of 8 asymmetric molecules. The unit cell parameters were a = 11.

Therapeutic significance of β-glucuronidase activity and its inhibitors: A review.

The emergence of disease and dearth of effective pharmacological agents on most therapeutic fronts, constitutes a major threat to global public health and man's existence. Consequently, this has created an exigency in the search for new drugs with improved clinical utility or means of potentiating available ones. To this end, accumulating empirical evidence supports molecular target therapy as a plausible egress and, β-glucuronidase (βGLU) - a lysosomal acid hydrolase responsible for the catalytic deconjugation of β-d-glucuronides has emerged as a viable molecular target for several therapeutic applications.

Green synthesis and characterization of novel 1,2,4,5-tetrasubstituted imidazole derivatives with eco-friendly red brick clay as efficacious catalyst.

Use of cheaper and recyclable materials contributes positively to economic growth with environmental sustainability. We report the prospect of utilizing red brick clay as catalyst, which exhibited excellent activity in rapid one-pot four-component condensation of 1,2,4,5-tetrasubstituted imidazoles with high conversion and yields (91-96%) in aqueous medium at 60 °C in short reaction times (25-40 min). The red brick clay material was fully characterized by XRD, FT-IR, SEM, TEM, EDX and BET analyses.

Efficient synthesis of novel pyrazole-linked 1,2,4-triazolidine-3-thiones using bismuth on zirconium oxide as a recyclable catalyst in aqueous medium.

The BiO loading on ZrO as heterogeneous catalyst was established as an extremely efficient catalyst for the synthesis of a series of novel 5-(1-(2,4-dinitrophenyl)-3-substituted-phenyl-1H-pyrazol-4-yl)-1,2,4-triazolidine-3-thione derivatives (3a-o) with high yields (90-96%) by reaction of 1-(2,4-dinitrophenyl)-3-substituted-phenyl-1H-pyrazole-4-carbaldehydes and thiosemicarbazide using water as a greener solvent at 80 °C within 30-45 min. Materials with different percentages of BiO on ZrO were prepared by simple wet impregnation method. The synthesized material has been characterized by various techniques (XRD, TEM, SEM, BET).

Synthesis, computational studies and antiproliferative activities of coumarin-tagged 1,3,4-oxadiazole conjugates against MDA-MB-231 and MCF-7 human breast cancer cells.

A novel library of coumarin tagged 1,3,4 oxadiazole conjugates was synthesized and evaluated for their antiproliferative activities against MDA-MB-231 and MCF-7 breast cancer cell lines. The evaluation studies revealed that compound 9d was the most potent molecule with an IC value of <5 µM against the MCF-7 cell line. Interestingly, compounds 10b and 11a showed a similar trend with lower inhibitory concentration (IC = 7.

Current anti-diabetic agents and their molecular targets: A review.

Diabetes mellitus is a medical condition characterized by the body's loss of control over blood sugar. The frequency of diagnosed cases and consequential increases in medical costs makes it a rapidly growing chronic disease that threatens human health worldwide. In addition, its unnerving statistical projections are perilous to both the economy of the nation and man's life expectancy.

Design, synthesis, neuroprotective, antibacterial activities and docking studies of novel thieno[2,3-d]pyrimidine-alkyne Mannich base and oxadiazole hybrids.

A series of thieno[2,3-d]pyrimidine alkyne Mannich base derivatives (7a-e, 8a-e) and thieno[2,3-d]pyrimidine 1,3,4-oxadiazole derivatives (9a-e, 10a-e) have been synthesized and evaluated for their neuroprotective and neurotoxicity activities where 9a, 10d displayed good neuroprotection 10.6 and 11.88 µg/mL respectively against the HO induced cell death at the EC values and 9b, 9d showed respective toxic effects on PC12 cells at CC 86.

Recent advances (2015-2016) in anticancer hybrids.

In spite of the development of a large number of novel anticancer drugs over the years, Cancer remains as a prominent cause of death, worldwide. Numerous drugs that are currently in clinical practice have developed multidrug resistance along with fatal side effects. Therefore, the utilization of single-target therapy is incapable of providing an effective control on the malignant process.

A Review of Recent Advancements in Anti-tubercular Molecular Hybrids.

Tuberculosis (TB) accounts for millions of deaths worldwide every year. Diverse survival strategies adopted by Mycobacterium tuberculosis (Mtb) have substantially hindered the existing anti-TB regimen thereby leading to multidrug-resistant (MDR) and extremely drug-resistant (XDR) strains of TB. The steady decrease in current antibiotics' efficacy against these adversities is an indicator that their adequate replenishment in future is almost impossible, placing society on the precipice of a catastrophe.