Open AccessAnti-HIV activity of new pyrazolobenzothiazine 5,5-dioxide-based acetohydrazides
Author(s) -
Zunera Khalid,
Sana Aslam,
Matloob Ahmad,
Munawar Ali Munawar,
Catherine Montero,
Mervi Detorio,
Masood Parvez,
Raymond F. Schinazi
Publication year - 2015
Publication title -
medicinal chemistry research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.352
H-Index - 45
eISSN - 1554-8120
pISSN - 1054-2523
DOI - 10.1007/s00044-015-1411-z
Subject(s) - cytotoxicity , chemistry , vero cell , human immunodeficiency virus (hiv) , ec50 , stereochemistry , combinatorial chemistry , in vitro , virology , biochemistry , medicine
A series of fifteen new 2-[3-(3-chlorophenyl)-5,5-dioxidobenzo[e]pyrazolo[4,3-c][1,2]thiazin-4(2H)-yl]- N '-arylmethyleneacetohydrazides ( 5a-o ) were synthesized and screened for their anti-HIV-1 and cytotoxicity activity. Out of fifteen pyrazolobenzothiazine-based hydrazones, thirteen were found to be active inhibitors of HIV with EC 50 values <20 μM. Moreover, the cytotoxicity results showed that most of the compounds were toxic to PBM, CEM and Vero cell lines. This information could be used for structural modifications to acquire good candidates of HIV drugs.