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Infectious Diseases

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A glimpse into the focused therapeutic areas

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Most used technologies in drug development

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Disease Domain	Count

Infectious Diseases	3

Top 5 Drug Type	Count

Small molecule drug	4

Top 5 Target	Count

DNA	2
TLR7(Toll like receptor 7)	1

Epilepsy affects millions of people worldwide, about one-third patients with epilepsy exhibits resistance to available antiseizures medications, known as drug-resistant epilepsy (DRE). Mitochondrial dysfunction has been implicated as a hallmark in drug-resistant epilepsy via activation of microglial kynurenine 3-monooxygenase (KMO) and cyclooxygenase (COX) enzymes, leading to neuroinflammation and oxidative stress. Diclofenac, an equipotent non selective cyclooxygenase inhibitor, has inhibitory action on KMO enzyme and has also shown anti-inflammatory and antioxidant properties in animal models of epilepsy. These properties make it a suitable candidate for amelioration of DRE. However, its potential in drug-resistant epilepsy remained unexplored till date. In this study, dose dependent effect of diclofenac (5 mg/kg, 10 mg/kg, 20 mg/kg) has been explored in rotenone corneal kindling model of mitochondrial DRE. The results of our study revealed the induction of drug resistance to antiseizure medications and induced kynurenine 3-monooxygenase activity in rotenone corneal kindled epileptic mice in comparison to naive mice. Treatment of rotenone corneal kindled epileptic mice with diclofenac resulted in a significant decrease in drug resistance to antiseizure medications as evident by a reduction in seizure score in the treatment groups as compared to control group, in post-treatment resistance validation. The kynurenine 3-monooxygenase inhibitory activity (as evidenced by decreased levels of neurotoxic quinolinic acid) and the antioxidant effect (as evident by significantly reduced oxidative stress) in the diclofenac treated groups, emerged as a major contributor for its ameliorative action. Findings of this study suggests, diclofenac can be used as an adjunct therapy in amelioration of drug-resistant epilepsy.

01 Jan 2025·Journal of Molecular Structure

Unveiling the potential of novel 5α-reductase inhibitors via ligand based drug design, molecular docking and ADME predictions to manage BPH

Author: Agarwal, Subhash Mohan ; Dhingra, Neelima ; Rana, Priyanka ; Kaur, Tanzeer ; Sharma, Shiwani ; Das, Agneesh Pratim

Benign prostatic hyperplasia (BPH), a prevalent condition among elderly males characterized by the non-cancerous enlargement of the prostate gland is due to the increased stromal and epithelial cell numbersThe enlargement is driven by an active dihydrotestosterone (DHT), synthesized from its prohormone testosterone under the catalytic effect of 5α-reductase Type-II (5-AR2) enzyme.To reduce the increased DHT levels and ultimately to control prostate growth, inhibition of the 5-AR represent an interesting therapeutic target.The 3D crystallog. structure 5-AR2, a member of the steroid 5-AR family belonging to the class of oxidoreductase has been resolved recently and opened the door to develop selective novel inhibitors of 5-AR Type-II isoform using mol. modeling techniques.The Force field and Gaussian-field three-dimensional quant. structure-activity relationship (3D-QSAR) models have been developed using 42 selective 5-AR2 inhibitors belonging to chem. class of steroidal androstene.Partial least squares anal. produced statistically significant model with R²_training = 0.9367, 0.9459 and predictability Q²_test = 0.7233, 0.8595.Developed 3D-QSAR model include steric, electrostatic, hydrophobic, and hydrogen bond acceptor and donor field indicators, whereas the potential field contributions indicated the importance of steric feature in governing their biol. activity.Protein-ligand interaction pattern anal. revealed that amino acid residues GLU57, ARG114, TYR91 present in the active site of 5-AR2 are crucial for lower energy complexes with good binding affinity.Identified hits were finally adjudged for their druggability by determining in-silico pharmacokinetic parameters.Further, RMSD, binding free energy calculations and post MD anal. demonstrated the enhanced binding affinity with better ΔG_bind value (-79.6 ± 3.9 kcal/mol) of identified ligand A-10 than the reference mol. finasteride (-69.13 ± 4.69 kcal/mol).Combined approach of ligand-based and structure-based models have provided an improved understanding of the structural properties of androstene class that may be further used to develop novel 5-AR2 inhibitors to be useful in BPH.

01 Jan 2025·Journal of Molecular Structure

Development of a triazole-linked bis-organosilane compound as dual-function agent: Sensing of Al3+ ion in aqueous environments and inhibition of HIV-1 protease

Author: Kumar, T. J. Dhilip ; Ritika ; Sushma ; Malik, Pooja ; Singh, K.N. ; Kumar, T.J. Dhilip ; Khurana, Sumesh ; Singh, K. N. ; Thakur, Yamini ; Singh, Gurjaspreet ; Sharma, Samiksha

The increasing applications of aluminum metal have led to rising concerns regarding its adverse environmental impacts, particularly on marine life and human health, necessitating its efficient detection.Bis-organosilane compounds hold a pivotal position in organosilicon chem., contributing significantly to industrial processes and scientific research.In this study, a synthesized bis-1,2,3-triazole-linked bis-organosilane was employed as a sensor for the selective detection of Al³⁺ ions in a MeOH: H₂O (7:3, volume/volume) solvent system.This sensor demonstrated high selectivity and strong anti-interference capabilities, even in the presence of other metal ions.The detection limit for Al³⁺ was found to be significantly lower than the WHO-prescribed limits for drinking water.Using an actual water sample anal. experiment, its practical utility was also investigated.Addnl., bis-organosilane (6) capability as an antioxidant to stabilize free radicals was also tested.Given the biol. significance of triazoles, compound (6) was evaluated for its inhibitory activity against HIV-1 protease using mol. docking tools. the current study emphasizes bis-organosilane (6) as an Al³⁺ sensor with dual activity as a possible HIV medication and a significant antioxidant.

100 Deals associated with Punjabi University

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100 Translational Medicine associated with Punjabi University

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Pipeline

Pipeline Snapshot as of 07 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

Discovery

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3

Preclinical

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Bis-naphthalimides-5o ( DNA )	Bacterial Infections More	Preclinical
TLR7 agonists(Punjabi University) ( TLR7 )	Drug adjuvant More	Preclinical
Bis-naphthalimides-5d ( DNA )	Bacterial Infections More	Preclinical
Bile Acid Oligomers(Panjab University)	Staphylococcus Aureus Infections More	Discovery