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Idhayadhulla Akbar,1 Surendrakumar Radhakrishnan,1 Karpakavalli Meenakshisundaram,2 Aseer Manilal,3 Ashraf Atef Hatamleh,4 Bassam Khalid Alnafisi,4 Anis Ahamed,4 Ravindran Balasubramani5 1Research Department of Chemistry, Nehru Memorial College (Affiliated Bharathidasan University), Puthanamapatti, Tamilnadu, 621007, India; 2Department of Pharmaceutical Chemistry, Karpagam College of Pharmacy, Othakalmandapam, Coimbatore, 641032, India; 3Department of Medical Laboratory Science, College of Medicine and Health Sciences, Arba Minch University, Arba Minch, Ethiopia; 4Department of Botany and Microbiology, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia; 5Department of Environmental Energy and Engineering, Kyonggi University, Suwon, 16227, Republic of KoreaCorrespondence: Idhayadhulla Akbar, Email a.idhayadhulla@gmail.comPurpose: This study aims to determine the analgesic activity of 1,4-dihydropyridine hybrid benzamide derivatives. These hybrid derivatives were synthesized, and their analgesic activity was studied. The synthesis method applied was a one-step reaction involving a green chemistry approach.Methods: The compounds were prepared via the amination method with a yield ranging between 82% and 93%. The title compounds were confirmed by means of IR, 1H and 13C NMR, and mass spectral analyses. The pharmacological activity of all the synthesized compounds was evaluated, and the analgesic activities were monitored in vivo (by tail immersion methods), with a digital analgesiometer. The drug response and damage of tail ata concentration of 10 mg/kg were measured by tail-flicking latency.Results: The activity of compound 2c (81.35% activity at 5mg/kg) can be correlated with its salicylamidemoiety (13.99% activity at 5mg/kg), and diclofenac showed comparable activity (79.21% activity at 5mg/kg reference drugs). Compound 2c has a higher potential to inhibit COX proteins compared to diclofenac. The drug-like nature of the molecule 2c corresponds to i

Ashraf Atef Hatamleh,1 Dunia Al Farraj,1 Sarah Salah Al-Saif,1 SathishKumar Chidambaram,2 Surendrakumar Radhakrishnan,2 Idhayadhulla Akbar2 1Botany and Microbiology Department, College of Science, King Saud University, Riyadh, Kingdom of Saudi Arabia; 2Research Department of Chemistry, Nehru Memorial College (Affiliated with the Bharathidasan University), Puthanampatti, Tiruchirappalli District, Tamil Nadu, South IndiaCorrespondence: Idhayadhulla Akbar Email a.idhayadhulla@gmail.comPurpose: A new series of tetrazole derivatives, which are renowned antimicrobials possessing a five-membered aromatic heterocyclic group, are synthesized herein and subjected to antimicrobial and cytotoxicity screening.Methods: The tetrazole derivatives were synthesized via ultrasonication using Mannich base condensation. Structural verification of the products was performed using IR, 1H NMR, and 13C NMR spectroscopy, as well as mass spectroscopic and elemental analyses. The compounds were then screened for antimicrobial and cytotoxic activity against HepG2 (liver), MCF-7 (breast), and HeLa (cervical) cell lines. Inter- and intra-molecular binding interactions were determined using molecular docking studies. The exact binding mode between the most active tetrazole derivatives (ie, 1b, 2a, and 2b) and the proteins (ie, 4OR7, 1AI9, and 4FM9) was established using Autodock Vina 1.1.2 software and compared to the binding mode of the reference compounds (ie, cefazolin, clotrimazole, and fluorouracil).Results: Compound 1b was extremely active against Enterococcus faecalis relative to the positive control cefazolin. Compounds 1b and 1e were active against Candida albicans and Microsporum audouinii compared to the positive control clotrimazole in antifungal screening. The HepG2 (liver) and MCF-7 (breast) cancer cell lines were particularly susceptible to the synthesized compounds. Compared to the control compound fluorouracil, 2a and 2b were extremely active against all three cancer cell lines. M