Deepak Kumar

Angiotensin I-converting enzyme (ACE) is a key therapeutic target for combating hypertension and related cardiovascular diseases. ACE inhibitory novel designed substituted 1, 4-benzothiazine derivatives offer the prospect of enhanced potency, high specificity, and no or low side effect. Novel 1,4-benzothiazine derivatives were designed keeping in view the structural requirement of pharmacophore and Quantitatively structure Activity Relationship (QSAR).In the docking study, the most active compounds of the series were, AR 1, AR 2 and AR 3 exhibited good binding properties. Result reveals that the protein-ligand interaction energy of derivatives AR 1, AR 2 and AR 3 were -7.51 kcal/mol, -8.80 kcal/mol and -7.63 kcal/mol, which is slightly greater than the marketed antihypertensive Losartan drug as -5.51 kcal/mol, so that the derivatives have satisfactory affinity with established hypertensive receptor namely Angiotensin converted enzyme II. A computational study was also carried out including prediction of pharmacokinetic properties, toxicity and bioactivity studies. The percentage of absorption (%ABS) was calculated and observed that all titled compounds exhibited a better %ABS %ABS ranging 90.54, 91.42 and 90.55 respectively and compared than standard Losartan drug as %ABS 77.06.Although other pharmacological parameters were better than the standard drug. The above observation suggested that these compounds would serve as better lead compound for antihypertensive screening for future drug design perspective.

A new class of heterocyclic compounds 1,3,4-thiadiazolo[3,2-a]-s-triazine have been synthesized as schiff’s base of 1,3,4- thiadiazole mix with ammonium acetate and various aromatic aldehyde treated in MW irradiation at 480 W. Reaction is based on microwave mediate multi-component reaction (MCRs). The structures of these compounds have been elucidated by spectral (IR, NMR & Mass) analysis. The title compounds were then evaluated for their in-vitro microbial activity against 2 gram –Ve bacteria (E.coli, K. pneumoniae), 2 gram +Ve bacteria (S.aerues, B.subtilis) and 1 fungal specie (A.niger). The some newly synthesized compounds have shown promising antimicrobial activity.

Alzheimer’s disease is the most prevalent form of dementia. Neuropathogenesis is proposed to be a result of the accumulation of amyloid β- peptides in the brain together with oxidative stress mechanisms and neuroinflammation. Drugs effective in Alzheimer’s disease (AD) should have several aims: to improve the cognitive impairment, control the behavioral and neurological symptoms, delay the progression of the disease, and prevent the onset. This review discusses the molecular mechanism of Alzheimer’s disease with a focus on the different agents those are inhibit the progression of the disease and improved patients condition and status.. Key words: Alzheimer’s disease, β-amyloid, Tacrine, Rivastigmine

  Triazine is the chemical species of six-membered heterocyclic ring compound with three nitrogens replacing carbon-hydrogen units in the benzene ring structure. The names of the three isomers indicate which of the carbon-hydrogen units on the benzene ring position of the molecule have been replaced by nitrogens, called 1,2,3-triazine, 1,2,4-triazine, and 1,3,5-triazine respectively. Symmetrical 1, 3, 5-triazine is the common.  Triazines are prepared from cyanic acid amide by trimerization (1, 3, 5-triazine). Pyridine is the aromatic nitrogen heterocyclic compound having only one nitrogen, and diazines are with 2 nitrogen atoms, triazine having three nitrogen and tetrazines are with 4 nitrogen atoms on the benzene ring system. Triazines are weak base. Triazines have much weaker resonance energy than benzene, so nucleophilic substitution is preferred than electrophilic substitution. Heterocyclic bearing a symmetrical s-triazines or 1, 3, 5-triazines moieties, represent an interesting class of compounds possessing a wide spectrum of biological activities such as anti-cancer, antiviral, fungicidal, insecticidal, bactericidal, herbicidal and antimicrobial, antimalarial agents. They also find applications as dyes, lubricants and analytical reagents.   Key words: Triazine, Nucleophilic substitution, Cyanuric chloride, 1, 3, 5-triazine, s- Triazine