1,3,4-Oxadiazole Scaffold in Antidiabetic Drug Discovery: An Overview.

Diabetes mellitus is one of the biggest challenges for the scientific community in the 21st century. With the increasing number of cases of diabetes and drug-resistant diabetes, there is an urgent need to develop new potent molecules capable of combating this cruel disease. Medicinal chemistry concerns the discovery, development, identification, and interpretation of the mode of action of biologically active compounds at the molecular level.

An Insight into the Combat Strategies for the Treatment of Type 2 Diabetes Mellitus.

Diabetes is a chronic, and metabolic disorder that has gained epidemic proportions in the past few decades creating a threat throughout the globe. It is characterized by increased glucose levels that may be due to immune-mediated disorders (T1DM), insulin resistance or inability to produce sufficient insulin by β-pancreatic cells (T2DM), gestational, or an increasingly sedentary lifestyle. The progression of the disease is marked by several pathological changes in the body like nephropathy, retinopathy, and various cardiovascular complications.

A comprehensive review on the antidiabetic attributes of thiazolidine-4-ones: Synthetic strategies and structure-activity relationships.

The thiazolidine-4-one scaffold has recently emerged as a potential pharmacophore having clinical significance for medicinal chemists. This heterocyclic ring has been reported to possess a plethora of biological activities, including antidiabetic activity that has inspired researchers to integrate this core with different pharmacophoric fragments to design novel and effective antidiabetic leads. The antidiabetic activity has been observed due to the ability of the thiazolidine-4-one nucleus to interact with different biological targets, including peroxisome proliferator-activated receptor γ, protein tyrosine phosphatase 1B, aldose reductase, α-glucosidase, and α-amylase.

A complete review of empagliflozin: Most specific and potent SGLT2 inhibitor used for the treatment of type 2 diabetes mellitus.

Sodium-glucose co-transporter 2 (SGLT2) inhibitors are the latest class of drugs to be introduced for the treatment of type 2 diabetes mellitus (T2DM). They reduce hyperglycemia by increasing urinary glucose excretion and exert favorable effects beyond glucose control with consistent body weight, blood pressure, and serum uric acid reductions. Empagliflozin is a potent SGLT2 inhibitor used to improve glycemic control in adults with T2DM.

1,2,4-Oxadiazole as a Privileged Scaffold for Anti-inflammatory and Analgesic Activities: A Review.

1,2,4-Oxadiazole is one of the important heterocycles used by medicinal chemists in designing a new therapeutic molecule. The compounds containing this nucleus are reported to have a wide range of pharmaceutical and biological applications including anti-inflammatory and analgesic activities. The fused and pendent 1,2,4-oxadiazole moiety has been traced in a number of well established, commercially available drugs.

Chemical Modifications of Ketoprofen (NSAID) in Search of Better Lead Compounds: A Review of Literature From 2004-2016.

Background: Ketoprofen, a potent anti-inflammatory, analgesic and anti-pyretic drug belonging to the propionic acid class was synthesized in 1968. Rapid absorption, simple metabolism, faster blood brain barrier crossing and high antinociceptive activity are the features responsible for its high use. But, free acidic moiety present in its structure is the major factor that declines its popularity by causing various gastric side effects.

Exploring 1,3,4-Oxadiazole Scaffold for Anti-inflammatory and Analgesic Activities: A Review of Literature From 2005-2016.

1,3,4-Oxadiazole derivatives are found to have a wide range of pharmacological activities and attracting the researchers to work on this nucleus. Literature survey indicates that many 1,3,4- oxadiazoles have been synthesized with the aim to get compounds of significant anti-inflammatory and analgesic activities with reduced adverse effects. The purpose of this review is to compile the reports on 1,3,4-oxadiazole derivatives possessing anti-inflammatory and analgesic activities.

Synthesis and pharmacological evaluation of pyrazolo[4,3-c]cinnoline derivatives as potential anti-inflammatory and antibacterial agents.

A series of pyrazolo[4,3-c]cinnoline derivatives was synthesized, characterized and evaluated for anti-inflammatory and antibacterial activity. Test compounds that exhibited good anti-inflammatory activity were further screened for their ulcerogenic and lipid peroxidation activity. Compounds 4d and 4l showed promising anti-inflammatory activity with reduced ulcerogenic and lipid peroxidation activity when compared to naproxen.

Synthesis and antimicrobial screening of N-[2-(2/4-substituted phenyl)-1-(5/6 substituted 1H- benzimidazol-2-yl)vinyl]benzamides.

A series of (benzamidostyryl)benzimidazole derivatives were synthesized by hydrolyzing 2-phenyl-4-(substituted)benzylidene-5-oxazolones, the azlactone precursors in an acidic medium and treating the product with substituted o-phenylenediamine (OPDA) in situ. The structures of the synthesized compounds were confirmed by spectral and elemental analyses. All synthesized compounds were screened for their in vito antimicrobial activities against some identifiable strains.

Syntheses and evaluation of anti-inflammatory, analgesic and ulcerogenic activities of 1,3,4-oxadiazole and 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazole derivatives.

Several 2,5-disubstituted-1,3,4-oxadiazoles (4a-f) and 3,6-disubstituted-1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles (7a-f) were synthesized and characterized by elemental analyses and spectral data. These compounds were screened for their anti-inflammatory, analgesic, ulcerogenic and lipid peroxidation activities. Compound 7c showed excellent anti-inflammatory and remarkable analgesic activity with reduced ulcerogenic and lipid peroxidation activity when compared with ibuprofen.

Design & synthesis of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one as potential anticonvulsant agents.

A series of 2-(substituted aryloxy)-5-(substituted benzylidene)-3-phenyl-2,5-dihydro-1H-[1,2,4] triazin-6-one were designed & synthesized using appropriate synthetic route keeping in view the structural requirement of pharmacophore and evaluated for anticonvulsant activity and CNS activities. After intraperitoneal injection to mice, some synthesized derivatives were examined in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazol (scPTZ) induced seizure and neurotoxicity screens. Those found potent were also evaluated for behavioural impairment and depression activity.

N'-[(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene] 2/4-substituted hydrazides: synthesis and anticonvulsant activity.

A series of N'-[(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene] 2/4-substituted hydrazides were synthesized using appropriate synthetic route and characterized by elemental analysis and spectral data. The anticonvulsant activity of some of the synthesized compounds were evaluated against maximal electroshock induced seizure (MES) and subcutaneous pentylenetetrazol (scPTZ) induced seizure models in mice. The neurotoxicity were assessed using the rotorod method.